Compounds > fosbretabulin
Page last updated: 2024-12-11

fosbretabulin

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Description

fosbretabulin: a microtubule destabilizing agent isolated from Combretum caffrum; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5351387
CHEMBL ID1206232
SCHEMBL ID66079
MeSH IDM0163664
PubMed CID5351344
CHEMBL ID67
CHEBI ID181391
SCHEMBL ID18945
MeSH IDM0163664

Synonyms (109)

Synonym
i5590es2qz ,
222030-63-9
2-methoxy-5-((1z)-2-(3,4,5-trimethoxyphenyl)ethenyl)phenyl phosphate
unii-i5590es2qz
fosbretabulin [inn]
fosbretabulin disodium
combretastatin a-4 phosphate
phenol, 2-methoxy-5-((1z)-2-(3,4,5-trimethoxyphenyl)ethenyl)-, dihydrogen phosphate
[2-methoxy-5-[(z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenyl] dihydrogen phosphate
combretastatin a4 phosphate
phenol, 2-methoxy-5-((1z)-2-(3,4,5-trimethoxyphenyl)ethenyl)-,1-(dihydrogen phosphate)
2-methoxy-5-((z)-2-(3,4,5-trimethoxyphenyl)vinyl)phenyl dihydrogen phosphate
phenol, 2-methoxy-5-((z)-2-(3,4,5-trimethoxyphenyl)ethenyl)-, dihydrogen phosphate
fosbretabulin
phosbretabulin
CHEMBL1206232
(z)-2-methoxy-5-(3,4,5-trimethoxystyryl)phenyl dihydrogen phosphate
combretastatin a-4 phosphate [mi]
fosbretabulin [mart.]
fosbretabulin [who-dd]
zybrestat (fosbretabulin disodium)
gtpl8857
SCHEMBL66079
AKOS022175199
fosbretabulin [free base]
ca 4dp
DB12577
Q5150956
A851726
fosbretabulin free acid
222030-63-9 (free acid)
phenol, 2-methoxy-5-[(1z)-2-(3,4,5-trimethoxyphenyl)ethenyl]-,dihydrogen phosphate
[2-methoxy-5-[(z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenoxy]phosphonic acid
DTXSID401028843
(z)-2-methoxy-5-(3,4,5-trimethoxystyryl)phenyldihydrogenphosphate
AC-5280
2-methoxy-5-[(z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenol
CHEBI:181391
nsc-613729
phenol,4,5-trimethoxyphenyl)ethenyl]-
combretastatin a-4
ca-4
st-1986 ,
CA4 ,
combretastatin a4
117048-59-6
3,4,5-trimethoxy-3'-hydroxy-4'-methoxystilbene
nsc 613729
nsc 817373
phenol, 2-methoxy-5-(2-(3,4,5-trimethoxyphenyl)ethenyl)-, (z)-
crc 87-09
1-(3,4,5-trimethoxyphenyl)-2-(3'-hydroxy-4'-methoxyphenyl)ethene
crc-98-09
nsc 609397
combretastatin 4
combrestatin a4
nsc-817373
CHEMBL67 ,
2'-deoxycombretastatin a1
2-methoxy-5-[(z)-2-(3,4,5-trimethoxy-phenyl)-vinyl]-phenol
combretastin a-4
5-(3,4,5-trimethoxystyryl)-2-methoxyphenol
combrestatin a-4
combretastin a4
(combretastin a-4)2-methoxy-5-[2-(3,4,5-trimethoxy-phenyl)-vinyl]-phenol
(combretastatin a-4)2-methoxy-5-[2-(3,4,5-trimethoxy-phenyl)-vinyl]-phenol
combretastatin a-4, (csa4)
2-methoxy-5-[(z)-2-(3,4,5-trimethox y-phenyl)-vinyl]-phenol
2-methoxy-5-[(z)-2-(3,4,5-trimethoxyphenyl)vinyl]phenol
5-[(s)-2-hydroxy-2-(3,4,5-trimethoxy-phenyl)-ethyl]-2-methoxy-phenol
(z)-5-(3,4,5-trimethoxystyryl)-2-methoxyphenol
(z)-3''-hydroxy-3,4,4'',5-tetramethoxystilbene
combretastastin a-4
z-combretastatin a-4
combretastatin-a4
bdbm50005480
C20268
AKOS015950727
16u6op69rq ,
unii-16u6op69rq
phenol, 2-methoxy-5-[(1z)-2-(3,4,5-trimethoxyphenyl)ethenyl]-
2-methoxy-5-[(1z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenol
S7783
(z)-2-methoxy-5-(3,4,5-trimethoxystyryl)phenol
gtpl8854
SCHEMBL18945
combretastatin a4 [who-dd]
combretastatin a-4 [mi]
ca 4
HMS3650G11
3'-hydroxy-3,4,4',5-tetramethoxy-cis-stilbene
C2520
mfcd03453309
combretastatin a4, >=98% (hplc), powder
HY-N2146
CS-6023
[3,4,5-trimethoxy-3'-hydroxy-4'-methoxy-(z)-stilbene]
DS-5860
Q5150955
DB14680
sr-01000946784
SR-01000946784-1
AMY24892
combretastatin-a-4
CCG-265026
EX-A4207
DTXSID101025983
EN300-1587417
Z2312943638

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"Anthracyclines are a well-known cause of cardiotoxicity, but a number of other drugs used to treat cancer can also result in cardiac and cardiovascular adverse effects."( Cardiac and cardiovascular toxicity of nonanthracycline anticancer drugs.
Ewer, MS; Jones, RL, 2006)		0.33
" • CA4P-related grade 3 or 4 adverse events were tumour pain, dyspnoea, hypoxia and syncope in patients who received doses ≥ 50 mg m(-2)."( A pharmacokinetic and safety study of single dose intravenous combretastatin A4 phosphate in Chinese patients with refractory solid tumours.
Chen, L; He, X; Huang, H; Huang, J; Li, S; Li, Z; Lin, T; Ye, S; Zhan, J, 2011)		0.37
" Safety was monitored by vital signs, ocular and physical examinations, electrocardiogram, routine laboratory tests, and collection of adverse events."( Vascular disrupting agent for neovascular age related macular degeneration: a pilot study of the safety and efficacy of intravenous combretastatin A-4 phosphate.
Balkissoon, J; Campochiaro, PA; Do, DV; Donahue, JK; Hafiz, G; Handa, JT; Ibrahim, MA; Nguyen, QD; Rivers, R; Sepah, YJ; Shah, SM; Van Anden, E, 2013)		0.39
"The most common adverse events were elevated blood pressure (46."( Vascular disrupting agent for neovascular age related macular degeneration: a pilot study of the safety and efficacy of intravenous combretastatin A-4 phosphate.
Balkissoon, J; Campochiaro, PA; Do, DV; Donahue, JK; Hafiz, G; Handa, JT; Ibrahim, MA; Nguyen, QD; Rivers, R; Sepah, YJ; Shah, SM; Van Anden, E, 2013)		0.39
"The safety profile of intravenous CA4P was consistent with that reported in oncology trials of CA4P and with the class effects of vascular disruptive agents; however, the frequency of adverse events was different."( Vascular disrupting agent for neovascular age related macular degeneration: a pilot study of the safety and efficacy of intravenous combretastatin A-4 phosphate.
Balkissoon, J; Campochiaro, PA; Do, DV; Donahue, JK; Hafiz, G; Handa, JT; Ibrahim, MA; Nguyen, QD; Rivers, R; Sepah, YJ; Shah, SM; Van Anden, E, 2013)		0.39
" There were no significant adverse cardiovascular side effects."( Randomized safety and efficacy study of fosbretabulin with paclitaxel/carboplatin against anaplastic thyroid carcinoma.
Bal, C; Balkissoon, J; Elisei, R; Gitlitz, B; Gramza, A; Haugen, BR; Jarzab, B; Karandikar, SM; Khuri, F; Licitra, L; Lu, C; Lu, SP; Marur, S; Ondrey, F; Remick, SC; Sosa, JA; Yosef, RB, 2014)		0.4
" Adverse events (AE), cardiovascular parameters, and biochemical investigations were studied, and the maximum tolerated dose was determined."( A phase I clinical trial assessing the safety and tolerability of combretastatin A4 phosphate injections.
Han, X; Li, N; Liu, P; Qin, Y; Shi, Y; Sun, K; Sun, Y; Wang, H; Wu, L; Xu, H; Yang, S; Zhang, S, 2014)		0.4

Pharmacokinetics

ExcerptReferenceRelevance
"Clinical evaluation of novel agents that target tumor blood vessels requires pharmacodynamic end points that measure vascular damage."( Assessment of pharmacodynamic vascular response in a phase I trial of combretastatin A4 phosphate.
Anderson, HL; Jones, T; Miller, MP; Price, PM; Robbins, A; Yap, JT, 2003)		0.32
"Although in vitro studies suggest that variable rates of tumor-specific prodrug dephosphorylation may explain these differences in pharmacokinetics profiles, the improved antitumor activity and altered pharmacokinetic profile of CA1 may be due to the formation of a more reactive metabolite."( Comparative preclinical pharmacokinetic and metabolic studies of the combretastatin prodrugs combretastatin A4 phosphate and A1 phosphate.
Anthoney, DA; Bibby, MC; Cooper, PA; Kirwan, IG; Lippert, JW; Loadman, PM; Pettit, GR; Shnyder, SD; Swaine, DJ, 2004)		0.32
" The method was reliable and has been successfully applied to a pharmacokinetic study of CA4P in beagle dogs via intravenous drop infusion at dose rates of 1, 3 and 9mgkg(-1)."( Development of a rapid and sensitive LC-MS/MS assay for the determination of combretastatin A4 phosphate, combretastatin A4 and combretastatin A4 glucuronide in beagle dog plasma and its application to a pharmacokinetic study.
Chai, Y; Che, J; Chen, Z; Cheng, Y; Hou, Y; Liu, X; Meng, Q; Shan, C; Wang, X, 2009)		0.35
"• Three pharmacokinetic and safety studies for combretastatin A4 phosphate (CA4P), the first vascular disrupting agent, have been conducted in Western countries."( A pharmacokinetic and safety study of single dose intravenous combretastatin A4 phosphate in Chinese patients with refractory solid tumours.
Chen, L; He, X; Huang, H; Huang, J; Li, S; Li, Z; Lin, T; Ye, S; Zhan, J, 2011)		0.37
"• This is the first pharmacokinetic and safety study conducted in East Asian patients."( A pharmacokinetic and safety study of single dose intravenous combretastatin A4 phosphate in Chinese patients with refractory solid tumours.
Chen, L; He, X; Huang, H; Huang, J; Li, S; Li, Z; Lin, T; Ye, S; Zhan, J, 2011)		0.37
" For macromolecule conjugate nanomedicine, its pharmacology mechanism is closely related to the pharmacokinetic profiles in vivo."( A UHPLC-MS/MS method coupled with simple and efficient alkaline hydrolysis for free and total determination of conjugate nanomedicine: Pharmacokinetic and biodistribution study of poly (l-glutamic acid)-graft-methoxy poly (ethylene glycol)/combretastatin
Chen, L; Feng, B; Liao, Z; Liu, K; Liu, Y; Shan, B; Song, Y; Su, D; Xu, P; Zeng, Q; Zhong, Y, 2019)		0.51
" Therefore, this method was successfully applied to the pharmacokinetic study of CA4P in phase I clinical trial."( A high-throughput and simultaneous determination of combretastatin A-4 phosphate and its metabolites in human plasma using HPLC-MS/MS: Application to a clinical pharmacokinetic study.
Fang, Y; Huang, J; Sun, Y; Wang, Q; Wang, Y; Wu, F; Wu, Q; Wu, W; Yu, X, 2021)		0.62

Compound-Compound Interactions

ExcerptReferenceRelevance
" m When TNP-470 was combined with combreAp, no significant lengthening of the growth delay, irrespective of the tumor size, was present with the applied schedule."( In vivo antitumor effect of vascular targeting combined with either ionizing radiation or anti-angiogenesis treatment.
Ahmed, B; Anné, J; Lambin, P; Landuyt, W; Nuyts, S; Op de Beeck, M; Rijnders, A; Theys, J; van den Bogaert, W; van Oosterom, A, 2001)		0.31
" Thus, the use of angiogenesis inhibitors in combination with radiation therapy should help to overcome the limitations of each leading to enhanced efficacy and diminished toxicity."( Radiation combined with antiangiogenic and antivascular agents.
O'Reilly, MS, 2006)		0.33
" Changes in dynamic CT parameters of tumor blood volume (BV) and permeability surface area product (PS) were measured for the whole tumor volume, tumor rim, and center after radiotherapy alone and after radiotherapy in combination with CA4P."( Tumor antivascular effects of radiotherapy combined with combretastatin a4 phosphate in human non-small-cell lung cancer.
Carnell, D; Goh, V; Hoskin, PJ; Meer, K; Ng, QS; Padhani, AR; Saunders, MI, 2007)		0.34
"In preclinical models, radioimmunotherapy with (131)I-A5B7 anti-carcinoembryonic antigen (CEA) antibody ((131)I-A5B7) combined with the vascular disruptive agent combretastatin-A4-phosphate (CA4P) produced cures unlike either agent alone."( A phase I trial of radioimmunotherapy with 131I-A5B7 anti-CEA antibody in combination with combretastatin-A4-phosphate in advanced gastrointestinal carcinomas.
Begent, RH; Buscombe, J; Chan, PS; Chester, KA; Dancey, G; Folkes, LK; Gaya, AM; Green, AJ; Malaroda, A; Meyer, T; Othman, S; Owen, K; Padhani, AR; Pedley, RB; Poupard, L; Rustin, GJ; Sharma, SK; Stirling, JJ; Stratford, MR; Taylor, NJ; Violet, JA; Wellsted, D, 2009)		0.35
" The aim of this study was to use a mouse model to investigate whether hypertension or its modification influenced the treatment efficacy of CA4P in combination with other therapies."( Combretastatin-induced hypertension and the consequences for its combination with other therapies.
Bohn, AB; Busk, M; Horsman, MR; Skals, M; Wang, T, )		0.13
" The effects of CA4P alone or in combination with the antihypertensive drug hydralazine (HDZ) on mean arterial blood pressure (MABP), hematocrit (Hct) and hemoglobin concentration ([Hb]) were characterized in non-tumor-bearing animals."( Combretastatin-induced hypertension and the consequences for its combination with other therapies.
Bohn, AB; Busk, M; Horsman, MR; Skals, M; Wang, T, )		0.13
"The vascular disrupting agent combretastatin-A4-phosphate (CA4P) demonstrated antitumour activity in preclinical studies when combined with radiation."( Phase Ib trial of radiotherapy in combination with combretastatin-A4-phosphate in patients with non-small-cell lung cancer, prostate adenocarcinoma, and squamous cell carcinoma of the head and neck.
Alonzi, R; Carnell, D; Goh, V; Hoskin, PJ; Mandeville, H; Meer, K; Milner, J; Ng, QS; Padhani, AR; Saunders, MI, 2012)		0.38
" DLT of cardiac ischaemia occurred in two patients with SCCHN at a weekly dose of 50 mg/m2 in combination with cetuximab."( Phase Ib trial of radiotherapy in combination with combretastatin-A4-phosphate in patients with non-small-cell lung cancer, prostate adenocarcinoma, and squamous cell carcinoma of the head and neck.
Alonzi, R; Carnell, D; Goh, V; Hoskin, PJ; Mandeville, H; Meer, K; Milner, J; Ng, QS; Padhani, AR; Saunders, MI, 2012)		0.38
"CA4P in combination with bevacizumab appears safe and well tolerated in this dosing schedule."( Phase I trial of combretastatin A4 phosphate (CA4P) in combination with bevacizumab in patients with advanced cancer.
Carden, C; Collins, DJ; Fisher, N; Harris, A; Judson, I; Koh, DM; Leach, MO; Lu, SP; Nathan, P; Ng, M; Padhani, AR; Rustin, GJ; Smythe, J; Stirling, JJ; Taylor, NJ; Zweifel, M, 2012)		0.38
"This pre-clinical study was designed to investigate the effect of various vascular disrupting agents (VDAs) that have undergone or are in clinical evaluation, had on the oxygenation status of tumours and what effects that could have on the combination with radiation."( Induction of hypoxia by vascular disrupting agents and the significance for their combination with radiation therapy.
Busk, M; Horsman, MR; Iversen, AB, 2013)		0.39
"Polytherapy (or drug combination cancer therapy (DCCT)), targeting multiple mechanisms associated with tumor proliferation, can efficiently maximize therapeutic efficacy, decrease drug dosage, and reduce drug resistance."( Molecular Engineering-Based Aptamer-Drug Conjugates with Accurate Tunability of Drug Ratios for Drug Combination Targeted Cancer Therapy.
Fang, X; Fu, T; He, N; Huang, Q; Peng, Y; Sun, W; Tan, W; Wang, P; Zhang, P; Zhao, Z; Zhou, F, 2019)		0.51
" Third, the therapeutic effects and the mechanism of the drug combination in the inhibition of transplanted tumors was studied."( Synergistic Anticancer Effects of Cisplatin Combined with Combretastatin A4 Phosphate on Human Osteosarcoma-Xenografted Mice.
Dai, G; Liu, G; Song, Q; Zheng, D, 2021)		0.62
"This study aimed to investigate the effect of combretastatin A4 phosphate (CA4P) on proliferation, migration, and capillary tube formation of human umbilical vein endothelial cells (HUVECs) and the efficacy of transcatheter arterial embolization combined with CA4P in the treatment of rabbit VX2 liver tumor."( Transcatheter Arterial Embolization Combined with Anti-vascular Agent Combretastatin A4 Phosphate Inhibits Growth and Vascularization of Liver Tumor in an Animal Model.
Deng, Q; Feng, JW; Hu, HY; Rao, M; Ren, Q; Wang, Y; Wu, JJ; Wu, ZZ; Zhao, H, 2022)		0.72
"The study suggests that CA4P could inhibit the proliferation, migration, and capillary tube formation of HUVECs, and transcatheter arterial embolization combined with CA4P could inhibit the growth of VX2 tumor and obviously induce tumor necrosis."( Transcatheter Arterial Embolization Combined with Anti-vascular Agent Combretastatin A4 Phosphate Inhibits Growth and Vascularization of Liver Tumor in an Animal Model.
Deng, Q; Feng, JW; Hu, HY; Rao, M; Ren, Q; Wang, Y; Wu, JJ; Wu, ZZ; Zhao, H, 2022)		0.72

Bioavailability

ExcerptReferenceRelevance
" This suggests some bioavailability by this route."( Abilities of 3,4-diarylfuran-2-one analogs of combretastatin A-4 to inhibit both proliferation of tumor cell lines and growth of relevant tumors in nude mice.
Coy, DH; Fuselier, JA; Sun, L; Vasilevich, NI, )		0.13
" CA4P-NPs reached an absolute bioavailability of 77."( Water-Soluble Combretastatin A4 Phosphate Orally Delivered via Composite Nanoparticles With Improved Inhibition Effect Toward S180 Tumors.
Qiu, L; Shen, Y; Wu, L, 2017)		0.46
" Furthermore, its poor aqueous solubility and the resulting limited bioavailability hinder its antitumor activity in the clinic."( Combination drug delivery via multilamellar vesicles enables targeting of tumor cells and tumor vasculature.
Kim, YJ; Liu, Y; Rohrs, JA; Siriwon, N; Wanga, P; Yu, Z, 2018)		0.48
" We have used a lipid-based nanoemulsion termed Lipid-Oil-Nanodroplets (LONDs) for the encapsulation and in vivo delivery of the poorly bioavailable combretastatin A4 (CA4)."( Targeted microbubbles carrying lipid-oil-nanodroplets for ultrasound-triggered delivery of the hydrophobic drug, combretastatin A4.
Bushby, RJ; Charalambous, A; Coletta, PL; Evans, SD; Ingram, N; Loadman, PM; Markham, AF; Marston, G; McLaughlan, JR; McVeigh, LE; Mico, V; Peyman, SA; Volpato, M; Wierzbicki, A, 2021)		0.62

Dosage Studied

ExcerptRelevanceReference
" We have investigated the effects of multiple daily or twice daily dosing with CA4P on the vascular function, cell survival and growth of syngeneic and spontaneous breast cancers in mice."( Schedule dependence of combretastatin A4 phosphate in transplanted and spontaneous tumour models.
Chaplin, DJ; Hill, SA; Lewis, G; Tozer, GM, 2002)		0.31
" The growth delay results obtained with the in vivo rodent tumor models involving repeat dosing of combreAp can partly be explained by anti-angiogenic activity of the compound."( Vascular targeting effect of combretastatin A-4 phosphate dominates the inherent angiogenesis inhibitory activity.
Ahmed, B; Bouma-Ter Steege, JC; Griffioen, AW; Joosten-Achjanie, SR; Lambin, P; Landuyt, W; Van Der Schaft, DW; Van Eijk, LI; Van Esch, AM, 2003)		0.32
" every 21 days, and the maximal dosage was 90 mg/m(2)."( Cardiovascular safety profile of combretastatin a4 phosphate in a single-dose phase I study in patients with advanced cancer.
Buchter, C; Cooney, MM; DeCaro, K; Dowlati, A; Levine, SL; Levitan, N; Overmoyer, B; Radivoyevitch, T; Remick, SC; Robertson, K; Stambler, BS; Taylor, A, 2004)		0.32
"44 for QTc); blood pressure and uncorrected QTc interval dose-response correlations were not significant."( Cardiovascular safety profile of combretastatin a4 phosphate in a single-dose phase I study in patients with advanced cancer.
Buchter, C; Cooney, MM; DeCaro, K; Dowlati, A; Levine, SL; Levitan, N; Overmoyer, B; Radivoyevitch, T; Remick, SC; Robertson, K; Stambler, BS; Taylor, A, 2004)		0.32
" It was concluded that the targeting properties of the prepared delivery system would potentially improve the therapeutic benefits of combretastatin A4 compared with nontargeted liposomes or solution dosage forms."( A tumor vasculature targeted liposome delivery system for combretastatin A4: design, characterization, and in vitro evaluation.
Kiani, MF; Moore, BM; Nallamothu, R; Pattillo, CB; Scott, RC; Thoma, LA; Wood, GC, 2006)		0.33
" In this study we investigate the dose-response relationship of ultrasound contrast agent for a minimal exposure power Doppler technique (minexPD) in a murine melanoma model."( Dose-response relationship of ultrasound contrast agent in an in vivo murine melanoma model.
Lee, WM; Schultz, S; Sehgal, CM; Seiler, GS; Ziemer, LS, 2007)		0.34
" The drug dose-response curves for all post-treatment vascular DCE-MRI parameters showed a shape similar to that of the TCD(50) curve."( Preclinical studies to predict efficacy of vascular changes induced by combretastatin a-4 disodium phosphate in patients.
Horsman, MR; Maxwell, RJ; Murata, R; Nielsen, T; Ostergaard, L; Stødkilde-Jørgensen, H, 2008)		0.35
" Repeated dosing of l-NNA with CA-4-P produced enhanced growth delay over either treatment alone in P22, CaNT, and spontaneous T138 mouse mammary tumors, which represented a true therapeutic enhancement."( Nitric oxide synthase inhibition enhances the tumor vascular-damaging effects of combretastatin a-4 3-o-phosphate at clinically relevant doses.
Hill, SA; Lewis, G; Prise, VE; Tozer, GM; Wilson, I; Xie, S, 2009)		0.35
" Tumor response to repeated CA4P dosing (50 mg/kg/day, 5 days/week for 2 weeks) was examined through growth measurement, and ultimate tumor cell survival was studied by ex vivo clonogenic assay."( Vascular effects dominate solid tumor response to treatment with combretastatin A-4-phosphate.
Akerman, S; Fisher, M; Hill, SA; Kanthou, C; Lunt, SJ; Reyes-Aldasoro, CC; Tozer, GM; Wright, VJ, 2011)		0.37
"CA4P in combination with bevacizumab appears safe and well tolerated in this dosing schedule."( Phase I trial of combretastatin A4 phosphate (CA4P) in combination with bevacizumab in patients with advanced cancer.
Carden, C; Collins, DJ; Fisher, N; Harris, A; Judson, I; Koh, DM; Leach, MO; Lu, SP; Nathan, P; Ng, M; Padhani, AR; Rustin, GJ; Smythe, J; Stirling, JJ; Taylor, NJ; Zweifel, M, 2012)		0.38
"Potassium oxonate-induced hyperuricemic mice were dosed by gavage with eight stilbenes."( Antihyperuricemic and nephroprotective effects of resveratrol and its analogues in hyperuricemic mice.
Hong, Y; Kong, LD; Li, Z; Liu, L; Liu, YL; Shi, YW; Wang, CP; Wang, X, 2012)		0.38
" But the dosing schedules are essential to achieve a balance between vascular collapse and intratumoral uptake of chemotherapeutic agents."( Antimetastasis and antitumor efficacy promoted by sequential release of vascular disrupting and chemotherapeutic agents from electrospun fibers.
Chen, M; Li, X; Luo, X; Wei, J; Zhang, H; Zhang, Y, 2014)		0.4
" However, frequent dosing and negative patient compliance have been encountered over CA4P by injection administration due to its quite short-term action and acute side effects."( Water-Soluble Combretastatin A4 Phosphate Orally Delivered via Composite Nanoparticles With Improved Inhibition Effect Toward S180 Tumors.
Qiu, L; Shen, Y; Wu, L, 2017)		0.46
" The glycinamide analog 45 showed significant efficacy in the HCT-116 xenograft model, with 64% inhibition of tumor growth upon dosing at 20 mg/kg qd."( 1,1-Diarylalkenes as anticancer agents: dual inhibitors of tubulin polymerization and phosphodiesterase 4.
Cedzik, D; Chen, R; Collette, A; Leisten, J; Liu, W; Lu, L; Man, HW; Muller, GW; Narla, RK; Raymon, HK; Ruchelman, AL; Zhang, L, 2011)		0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
stilbenoidAny olefinic compound characterised by a 1,2-diphenylethylene backbone.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (46)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency0.00930.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency0.00930.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 2Homo sapiens (human)IC50 (µMol)61.94000.40003.10009.7000AID1411601
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)200.00000.21005.553710.0000AID1411600
Tubulin polymerization-promoting proteinHomo sapiens (human)IC50 (µMol)1.01600.03201.01602.0000AID1799503; AID1799504
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)IC50 (µMol)12.27000.55003.70836.1000AID1411599
Tyrosine-protein kinase ABL1Homo sapiens (human)IC50 (µMol)10.00000.00010.712810.0000AID1157569
Epidermal growth factor receptorHomo sapiens (human)IC50 (µMol)10.00000.00000.536910.0000AID1157567
Tubulin alpha-1A chainSus scrofa (pig)IC50 (µMol)1.82000.00672.160310.0000AID1057124; AID1158426; AID1285329; AID1517169; AID1517359; AID1518073; AID1533672; AID1534367; AID1586012; AID1612628; AID1613397; AID1628409; AID1637527; AID1865677; AID1906180; AID1917311; AID213846; AID214367; AID214539; AID214546; AID214556; AID228626; AID382330; AID502528; AID622612; AID635032; AID662352; AID691623; AID695148; AID769749
Tubulin beta chainSus scrofa (pig)IC50 (µMol)1.94280.00672.137410.0000AID1057124; AID1158426; AID1285329; AID1517169; AID1517359; AID1518073; AID1533672; AID1534367; AID1586012; AID1612628; AID1613397; AID1628409; AID1637527; AID1865677; AID1906180; AID1917311; AID214367; AID382330; AID502528; AID622612; AID635032; AID662352; AID691623; AID695148; AID769749
Tubulin beta-4A chainHomo sapiens (human)IC50 (µMol)10.77220.00051.968010.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin beta-4A chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Tubulin beta chainHomo sapiens (human)IC50 (µMol)10.77220.00052.052910.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin beta chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)0.00900.00022.318510.0000AID751512; AID769831
Tubulin alpha-3C chainHomo sapiens (human)IC50 (µMol)10.77220.00051.955510.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin alpha-3C chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Fibroblast growth factor receptor 1Homo sapiens (human)IC50 (µMol)10.00000.00020.942010.0000AID1157568
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)IC50 (µMol)10.00000.00020.533510.0000AID1157570
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC50 (µMol)10.00000.00001.068010.0000AID630730
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC50 (µMol)1.08000.00030.81978.4900AID1162828
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)1.00500.00010.729810.0000AID1240945; AID293336
Delta-type opioid receptorRattus norvegicus (Norway rat)IC50 (µMol)0.81000.00030.38877.0000AID293336
Mu-type opioid receptorMus musculus (house mouse)IC50 (µMol)1.20000.00081.699210.0000AID1240945
Tubulin alpha-1B chainHomo sapiens (human)IC50 (µMol)10.77220.00051.955510.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin alpha-1B chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Tubulin alpha-4A chainHomo sapiens (human)IC50 (µMol)10.77220.00051.955510.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin alpha-4A chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Tubulin beta-4B chainHomo sapiens (human)IC50 (µMol)10.77220.00051.968010.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin beta-4B chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Vesicular acetylcholine transporterTetronarce californica (Pacific electric ray)IC50 (µMol)1.80000.03401.12202.6200AID1233620
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)10.00000.00001.104010.0000AID630730
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)IC50 (µMol)10.00000.00001.465110.0000AID630730
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)10.00000.00001.146310.0000AID630730
Tubulin beta-3 chainHomo sapiens (human)IC50 (µMol)10.24270.00051.894510.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1693360; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID751509; AID761828; AID765489; AID769828; AID771205
Tubulin beta-3 chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Tubulin beta-2A chainHomo sapiens (human)IC50 (µMol)10.77220.00051.968010.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin beta-2A chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Beta-tubulin Leishmania donovaniIC50 (µMol)1.95001.00001.38002.0000AID247567; AID247822
Tubulin beta-8 chainHomo sapiens (human)IC50 (µMol)10.77220.00051.968010.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin beta-8 chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Solute carrier family 22 member 6Homo sapiens (human)IC50 (µMol)41.36000.27004.53069.9000AID1411596
Tubulin beta-2B chainBos taurus (cattle)IC50 (µMol)3.36120.25001.88388.7000AID1125809; AID1153044; AID1154741; AID1157571; AID1157572; AID1176811; AID1179508; AID1179657; AID1183667; AID1185191; AID1185192; AID1187065; AID1195357; AID1198456; AID1200592; AID1205517; AID1206088; AID1233620; AID1235363; AID1251950; AID1276335; AID1278670; AID1297648; AID1341363; AID1517174; AID1524339; AID1538716; AID1552971; AID1572259; AID1586074; AID1597717; AID1608962; AID213997; AID213999; AID214001; AID214002; AID214014; AID214015; AID214019; AID214021; AID214031; AID214033; AID214037; AID214039; AID214160; AID214555; AID214690; AID228453; AID228456; AID266932; AID54295
Tubulin beta-2B chainBos taurus (cattle)Ki0.90670.14001.34003.2000AID1341372; AID1517174; AID213853
Tubulin alpha-3E chainHomo sapiens (human)IC50 (µMol)10.77220.00051.955510.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin alpha-3E chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Tubulin alpha-1A chainHomo sapiens (human)IC50 (µMol)10.77220.00051.955510.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin alpha-1A chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)3.52420.25001.87798.7000AID1125809; AID1153044; AID1154741; AID1157571; AID1157572; AID1176811; AID1179508; AID1179657; AID1183667; AID1185191; AID1185192; AID1187065; AID1195357; AID1198456; AID1200592; AID1205517; AID1206088; AID1233620; AID1235363; AID1251950; AID1276335; AID1278670; AID1297648; AID1341363; AID1517174; AID1524339; AID1538716; AID1552971; AID1572259; AID1586074; AID1597717; AID1608962; AID213997; AID213999; AID214001; AID214002; AID214015; AID214019; AID214021; AID214031; AID214033; AID214037; AID214039; AID214160; AID214690; AID228456; AID266932; AID54295
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)Ki1.27000.14001.91333.2000AID1341372; AID1517174
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)3.62180.25001.86568.7000AID1125809; AID1153044; AID1154741; AID1157571; AID1157572; AID1176811; AID1179508; AID1179657; AID1183667; AID1185191; AID1185192; AID1187065; AID1195357; AID1198456; AID1200592; AID1205517; AID1206088; AID1276335; AID1278670; AID1297648; AID1341363; AID1517174; AID1524339; AID1538716; AID1552971; AID1572259; AID1586074; AID1597717; AID1608962; AID213997; AID213999; AID214001; AID214002; AID214015; AID214019; AID214021; AID214031; AID214033; AID214037; AID214039; AID214160; AID214690; AID228456; AID266932
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)Ki1.27000.14001.91333.2000AID1341372; AID1517174
Solute carrier family 22 member 8Homo sapiens (human)IC50 (µMol)16.39004.93007.39009.9200AID1411597
Tubulin alpha-1C chainHomo sapiens (human)IC50 (µMol)10.77220.00051.955510.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin alpha-1C chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Tubulin beta-6 chainHomo sapiens (human)IC50 (µMol)10.77220.00051.968010.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin beta-6 chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Tubulin beta-2B chainHomo sapiens (human)IC50 (µMol)10.77220.00051.968010.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin beta-2B chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Tubulin beta-1 chainHomo sapiens (human)IC50 (µMol)10.29830.00051.987010.0000AID1075759; AID1162828; AID1174857; AID1174858; AID1183705; AID1185443; AID1188096; AID1194523; AID1196870; AID1237706; AID1240945; AID1254255; AID1424776; AID1498594; AID1500305; AID1514444; AID1595695; AID1597924; AID1698447; AID1727329; AID1731557; AID1733033; AID1757887; AID1771468; AID1778220; AID1779198; AID1811164; AID1832110; AID1860528; AID1862628; AID1886188; AID1891191; AID214692; AID228457; AID240662; AID241079; AID241105; AID261211; AID261214; AID262911; AID265407; AID265408; AID271658; AID273280; AID273359; AID277283; AID281503; AID288667; AID293336; AID297425; AID310083; AID590529; AID590530; AID721885; AID722281; AID727482; AID729788; AID735009; AID761828; AID765489; AID771205
Tubulin beta-1 chainHomo sapiens (human)Ki0.06150.00301.00832.4000AID256882; AID780970
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC50 (µMol)194.54000.10472.71957.0795AID1411598
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Tubulin alpha-1A chainSus scrofa (pig)EC50 (µMol)0.00700.00700.26350.5200AID1158424
Tubulin beta chainSus scrofa (pig)EC50 (µMol)0.00700.00700.26350.5200AID1158424
Tubulin beta-4A chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin beta chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin alpha-3C chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin alpha-1B chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin alpha-4A chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin beta-4B chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin beta-3 chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin beta-2A chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin beta-8 chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin beta-2B chainBos taurus (cattle)Kd0.31000.31005.570010.0000AID1517174
Tubulin alpha-3E chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin alpha-1A chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)Kd0.31000.31005.570010.0000AID1517174
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)Kd0.31000.31005.570010.0000AID1517174
Tubulin alpha-1C chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin beta-6 chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin beta-2B chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
Tubulin beta-1 chainHomo sapiens (human)EC50 (µMol)0.00940.00900.36851.2300AID1267532; AID1635267
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (546)

Processvia Protein(s)Taxonomy
activation of cysteine-type endopeptidase activity involved in apoptotic processSolute carrier family 22 member 2Homo sapiens (human)
positive regulation of gene expressionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
monoatomic cation transportSolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin transportSolute carrier family 22 member 2Homo sapiens (human)
body fluid secretionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 2Homo sapiens (human)
amine transportSolute carrier family 22 member 2Homo sapiens (human)
putrescine transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transportSolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 2Homo sapiens (human)
choline transportSolute carrier family 22 member 2Homo sapiens (human)
dopamine transportSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 2Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
histamine transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 2Homo sapiens (human)
histamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
amino acid import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
L-arginine import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
export across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
L-alpha-amino acid transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
microtubule bundle formationTubulin polymerization-promoting proteinHomo sapiens (human)
oligodendrocyte developmentTubulin polymerization-promoting proteinHomo sapiens (human)
astral microtubule organizationTubulin polymerization-promoting proteinHomo sapiens (human)
positive regulation of protein-containing complex assemblyTubulin polymerization-promoting proteinHomo sapiens (human)
positive regulation of myelinationTubulin polymerization-promoting proteinHomo sapiens (human)
positive regulation of protein polymerizationTubulin polymerization-promoting proteinHomo sapiens (human)
myelin assemblyTubulin polymerization-promoting proteinHomo sapiens (human)
microtubule polymerizationTubulin polymerization-promoting proteinHomo sapiens (human)
oligodendrocyte differentiationTubulin polymerization-promoting proteinHomo sapiens (human)
cell divisionTubulin polymerization-promoting proteinHomo sapiens (human)
microtubule nucleation by microtubule organizing centerTubulin polymerization-promoting proteinHomo sapiens (human)
regulation of microtubule cytoskeleton organizationTubulin polymerization-promoting proteinHomo sapiens (human)
negative regulation of tubulin deacetylationTubulin polymerization-promoting proteinHomo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
prostaglandin transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
response to oxidative stressTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of ubiquitin-protein transferase activityTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of phospholipase C activityTyrosine-protein kinase ABL1Homo sapiens (human)
mitotic cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
neural tube closureTyrosine-protein kinase ABL1Homo sapiens (human)
B-1 B cell homeostasisTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of protein phosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
B cell proliferation involved in immune responseTyrosine-protein kinase ABL1Homo sapiens (human)
transitional one stage B cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
mismatch repairTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of DNA-templated transcriptionTyrosine-protein kinase ABL1Homo sapiens (human)
autophagyTyrosine-protein kinase ABL1Homo sapiens (human)
DNA damage responseTyrosine-protein kinase ABL1Homo sapiens (human)
integrin-mediated signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
canonical NF-kappaB signal transductionTyrosine-protein kinase ABL1Homo sapiens (human)
associative learningTyrosine-protein kinase ABL1Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageTyrosine-protein kinase ABL1Homo sapiens (human)
response to xenobiotic stimulusTyrosine-protein kinase ABL1Homo sapiens (human)
post-embryonic developmentTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of autophagyTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of endothelial cell migrationTyrosine-protein kinase ABL1Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
cerebellum morphogenesisTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of cell-cell adhesionTyrosine-protein kinase ABL1Homo sapiens (human)
microspike assemblyTyrosine-protein kinase ABL1Homo sapiens (human)
actin cytoskeleton organizationTyrosine-protein kinase ABL1Homo sapiens (human)
actin filament polymerizationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of endocytosisTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of cell adhesionTyrosine-protein kinase ABL1Homo sapiens (human)
neuron differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
BMP signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of BMP signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of axon extensionTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of microtubule polymerizationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of Cdc42 protein signal transductionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of type II interferon productionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of interleukin-2 productionTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of actin cytoskeleton organizationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of osteoblast proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
substrate adhesion-dependent cell spreadingTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to oxidative stressTyrosine-protein kinase ABL1Homo sapiens (human)
response to endoplasmic reticulum stressTyrosine-protein kinase ABL1Homo sapiens (human)
platelet-derived growth factor receptor-beta signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
protein modification processTyrosine-protein kinase ABL1Homo sapiens (human)
peptidyl-tyrosine autophosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisTyrosine-protein kinase ABL1Homo sapiens (human)
neuropilin signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
signal transduction in response to DNA damageTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of neuron apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
endothelial cell migrationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of T cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of vasoconstrictionTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of mitotic cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of mitotic cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IITyrosine-protein kinase ABL1Homo sapiens (human)
alpha-beta T cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
protein autophosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of fibroblast proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
spleen developmentTyrosine-protein kinase ABL1Homo sapiens (human)
thymus developmentTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
activated T cell proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
B cell receptor signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
neuromuscular process controlling balanceTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of oxidoreductase activityTyrosine-protein kinase ABL1Homo sapiens (human)
neuron apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of ubiquitin-protein transferase activityTyrosine-protein kinase ABL1Homo sapiens (human)
myoblast proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of stress fiber assemblyTyrosine-protein kinase ABL1Homo sapiens (human)
establishment of localization in cellTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
mitochondrial depolarizationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of focal adhesion assemblyTyrosine-protein kinase ABL1Homo sapiens (human)
Bergmann glial cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
cardiac muscle cell proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
neuroepithelial cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to hydrogen peroxideTyrosine-protein kinase ABL1Homo sapiens (human)
ERK1 and ERK2 cascadeTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeTyrosine-protein kinase ABL1Homo sapiens (human)
DNA conformation changeTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to lipopolysaccharideTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to transforming growth factor beta stimulusTyrosine-protein kinase ABL1Homo sapiens (human)
response to epinephrineTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of protein serine/threonine kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisTyrosine-protein kinase ABL1Homo sapiens (human)
cellular senescenceTyrosine-protein kinase ABL1Homo sapiens (human)
cell-cell adhesionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of dendrite developmentTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of long-term synaptic potentiationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of hematopoietic stem cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of extracellular matrix organizationTyrosine-protein kinase ABL1Homo sapiens (human)
podocyte apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to dopamineTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of establishment of T cell polarityTyrosine-protein kinase ABL1Homo sapiens (human)
DN4 thymocyte differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
protein localization to cytoplasmic microtubule plus-endTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of microtubule bindingTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of actin filament bindingTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of modification of synaptic structureTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of blood vessel branchingTyrosine-protein kinase ABL1Homo sapiens (human)
activation of protein kinase C activityTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of double-strand break repair via homologous recombinationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of Wnt signaling pathway, planar cell polarity pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of cell motilityTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of endothelial cell apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of T cell migrationTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of cellular senescenceTyrosine-protein kinase ABL1Homo sapiens (human)
epidermal growth factor receptor signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
cell surface receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
MAPK cascadeEpidermal growth factor receptorHomo sapiens (human)
ossificationEpidermal growth factor receptorHomo sapiens (human)
embryonic placenta developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein phosphorylationEpidermal growth factor receptorHomo sapiens (human)
hair follicle developmentEpidermal growth factor receptorHomo sapiens (human)
translationEpidermal growth factor receptorHomo sapiens (human)
signal transductionEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
activation of phospholipase C activityEpidermal growth factor receptorHomo sapiens (human)
salivary gland morphogenesisEpidermal growth factor receptorHomo sapiens (human)
midgut developmentEpidermal growth factor receptorHomo sapiens (human)
learning or memoryEpidermal growth factor receptorHomo sapiens (human)
circadian rhythmEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
diterpenoid metabolic processEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
cerebral cortex cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell growthEpidermal growth factor receptorHomo sapiens (human)
lung developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of superoxide anion generationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
response to cobalaminEpidermal growth factor receptorHomo sapiens (human)
response to hydroxyisoflavoneEpidermal growth factor receptorHomo sapiens (human)
cellular response to reactive oxygen speciesEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
ERBB2-EGFR signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of protein catabolic processEpidermal growth factor receptorHomo sapiens (human)
vasodilationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphorylationEpidermal growth factor receptorHomo sapiens (human)
ovulation cycleEpidermal growth factor receptorHomo sapiens (human)
hydrogen peroxide metabolic processEpidermal growth factor receptorHomo sapiens (human)
negative regulation of apoptotic processEpidermal growth factor receptorHomo sapiens (human)
positive regulation of MAP kinase activityEpidermal growth factor receptorHomo sapiens (human)
tongue developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA repairEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA replicationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of bone resorptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of vasoconstrictionEpidermal growth factor receptorHomo sapiens (human)
negative regulation of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEpidermal growth factor receptorHomo sapiens (human)
regulation of JNK cascadeEpidermal growth factor receptorHomo sapiens (human)
symbiont entry into host cellEpidermal growth factor receptorHomo sapiens (human)
protein autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
astrocyte activationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEpidermal growth factor receptorHomo sapiens (human)
digestive tract morphogenesisEpidermal growth factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationEpidermal growth factor receptorHomo sapiens (human)
neuron projection morphogenesisEpidermal growth factor receptorHomo sapiens (human)
epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
protein insertion into membraneEpidermal growth factor receptorHomo sapiens (human)
response to calcium ionEpidermal growth factor receptorHomo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicEpidermal growth factor receptorHomo sapiens (human)
positive regulation of glial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
morphogenesis of an epithelial foldEpidermal growth factor receptorHomo sapiens (human)
eyelid development in camera-type eyeEpidermal growth factor receptorHomo sapiens (human)
response to UV-AEpidermal growth factor receptorHomo sapiens (human)
positive regulation of mucus secretionEpidermal growth factor receptorHomo sapiens (human)
regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
cellular response to amino acid stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to mechanical stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to cadmium ionEpidermal growth factor receptorHomo sapiens (human)
cellular response to epidermal growth factor stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to estradiol stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to xenobiotic stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to dexamethasone stimulusEpidermal growth factor receptorHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
liver regenerationEpidermal growth factor receptorHomo sapiens (human)
cell-cell adhesionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein kinase C activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of prolactin secretionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of miRNA transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein localization to plasma membraneEpidermal growth factor receptorHomo sapiens (human)
negative regulation of cardiocyte differentiationEpidermal growth factor receptorHomo sapiens (human)
neurogenesisEpidermal growth factor receptorHomo sapiens (human)
multicellular organism developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of kinase activityEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
negative regulation of microtubule polymerizationTubulin beta-4A chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-4A chainHomo sapiens (human)
mitotic cell cycleTubulin beta-4A chainHomo sapiens (human)
odontoblast differentiationTubulin beta chainHomo sapiens (human)
microtubule-based processTubulin beta chainHomo sapiens (human)
cytoskeleton-dependent intracellular transportTubulin beta chainHomo sapiens (human)
natural killer cell mediated cytotoxicityTubulin beta chainHomo sapiens (human)
regulation of synapse organizationTubulin beta chainHomo sapiens (human)
spindle assemblyTubulin beta chainHomo sapiens (human)
cell divisionTubulin beta chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta chainHomo sapiens (human)
mitotic cell cycleTubulin beta chainHomo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-3C chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-3C chainHomo sapiens (human)
positive regulation of cell population proliferationFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIFibroblast growth factor receptor 1Homo sapiens (human)
MAPK cascadeFibroblast growth factor receptor 1Homo sapiens (human)
skeletal system developmentFibroblast growth factor receptor 1Homo sapiens (human)
angiogenesisFibroblast growth factor receptor 1Homo sapiens (human)
ureteric bud developmentFibroblast growth factor receptor 1Homo sapiens (human)
in utero embryonic developmentFibroblast growth factor receptor 1Homo sapiens (human)
organ inductionFibroblast growth factor receptor 1Homo sapiens (human)
neuron migrationFibroblast growth factor receptor 1Homo sapiens (human)
epithelial to mesenchymal transitionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of mesenchymal cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
chondrocyte differentiationFibroblast growth factor receptor 1Homo sapiens (human)
protein phosphorylationFibroblast growth factor receptor 1Homo sapiens (human)
sensory perception of soundFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of cell population proliferationFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
mesenchymal cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
gene expressionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of phospholipase activityFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of phospholipase C activityFibroblast growth factor receptor 1Homo sapiens (human)
regulation of phosphate transportFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of neuron projection developmentFibroblast growth factor receptor 1Homo sapiens (human)
cell migrationFibroblast growth factor receptor 1Homo sapiens (human)
peptidyl-tyrosine phosphorylationFibroblast growth factor receptor 1Homo sapiens (human)
ventricular zone neuroblast divisionFibroblast growth factor receptor 1Homo sapiens (human)
cell projection assemblyFibroblast growth factor receptor 1Homo sapiens (human)
embryonic limb morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
midbrain developmentFibroblast growth factor receptor 1Homo sapiens (human)
neuron projection developmentFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor signaling pathway involved in orbitofrontal cortex developmentFibroblast growth factor receptor 1Homo sapiens (human)
inner ear morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
outer ear morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
middle ear morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
chordate embryonic developmentFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of MAP kinase activityFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of MAPK cascadeFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationFibroblast growth factor receptor 1Homo sapiens (human)
cellular response to fibroblast growth factor stimulusFibroblast growth factor receptor 1Homo sapiens (human)
regulation of cell differentiationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of neuron differentiationFibroblast growth factor receptor 1Homo sapiens (human)
protein autophosphorylationFibroblast growth factor receptor 1Homo sapiens (human)
phosphatidylinositol-mediated signalingFibroblast growth factor receptor 1Homo sapiens (human)
paraxial mesoderm developmentFibroblast growth factor receptor 1Homo sapiens (human)
regulation of lateral mesodermal cell fate specificationFibroblast growth factor receptor 1Homo sapiens (human)
cell maturationFibroblast growth factor receptor 1Homo sapiens (human)
skeletal system morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
stem cell differentiationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionFibroblast growth factor receptor 1Homo sapiens (human)
calcium ion homeostasisFibroblast growth factor receptor 1Homo sapiens (human)
cardiac muscle cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
auditory receptor cell developmentFibroblast growth factor receptor 1Homo sapiens (human)
branching involved in salivary gland morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
lung-associated mesenchyme developmentFibroblast growth factor receptor 1Homo sapiens (human)
regulation of branching involved in salivary gland morphogenesis by mesenchymal-epithelial signalingFibroblast growth factor receptor 1Homo sapiens (human)
vitamin D3 metabolic processFibroblast growth factor receptor 1Homo sapiens (human)
diphosphate metabolic processFibroblast growth factor receptor 1Homo sapiens (human)
cementum mineralizationFibroblast growth factor receptor 1Homo sapiens (human)
stem cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of MAPKKK cascade by fibroblast growth factor receptor signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
negative regulation of fibroblast growth factor productionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of mitotic cell cycle DNA replicationFibroblast growth factor receptor 1Homo sapiens (human)
response to sodium phosphateFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of stem cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of parathyroid hormone secretionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of endothelial cell chemotaxisFibroblast growth factor receptor 1Homo sapiens (human)
regulation of extrinsic apoptotic signaling pathway in absence of ligandFibroblast growth factor receptor 1Homo sapiens (human)
multicellular organism developmentFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of cell differentiationFibroblast growth factor receptor 1Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of kinase activityFibroblast growth factor receptor 1Homo sapiens (human)
peptidyl-tyrosine phosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
primary ovarian follicle growthProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of cytokine productionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
stimulatory C-type lectin receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
signal transductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
signal complex assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
epidermal growth factor receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
transforming growth factor beta receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
integrin-mediated signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
spermatogenesisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
learning or memoryProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to xenobiotic stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to mechanical stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to acidic pHProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of gene expressionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of epithelial cell migrationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of epithelial cell migrationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of glucose metabolic processProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of protein processingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
skeletal muscle cell proliferationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of smooth muscle cell migrationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
macroautophagyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
peptidyl-tyrosine phosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of cell-cell adhesionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
platelet activationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
forebrain developmentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
T cell costimulationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of protein-containing complex assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein destabilizationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to nutrient levelsProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of telomere maintenance via telomeraseProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to insulin stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of intracellular estrogen receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of integrin activationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of toll-like receptor 3 signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
adherens junction organizationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
substrate adhesion-dependent cell spreadingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of dephosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of hippo signalingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
intracellular signal transductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
entry of bacterium into host cellProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
osteoclast developmentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to platelet-derived growth factor stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ERBB2 signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
angiotensin-activated signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
odontogenesisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of apoptotic processProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of apoptotic processProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of vascular permeabilityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
stress fiber assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
transcytosisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of bone resorptionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
bone resorptionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of Notch signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of bone resorptionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of Ras protein signal transductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of insulin receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein autophosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
platelet-derived growth factor receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
neurotrophin TRK receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ephrin receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
focal adhesion assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
oogenesisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
progesterone receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
leukocyte migrationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of small GTPase mediated signal transductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of protein transportProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to mineralocorticoidProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
myoblast proliferationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to electrical stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of focal adhesion assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of mitochondrial depolarizationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of telomerase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
uterus developmentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
branching involved in mammary gland duct morphogenesisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of cell projection assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
intestinal epithelial cell developmentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
interleukin-6-mediated signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to hydrogen peroxideProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to interleukin-1Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to lipopolysaccharideProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to peptide hormone stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to progesterone stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to fatty acidProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to hypoxiaProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to fluid shear stressProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of podosome assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
DNA biosynthetic processProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of heart rate by cardiac conductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cell-cell adhesionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of protein localization to nucleusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of non-membrane spanning protein tyrosine kinase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of TORC1 signalingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to prolactinProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of male germ cell proliferationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of ovarian follicle developmentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of lamellipodium morphogenesisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor-beta signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of early endosome to late endosome transportProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of anoikisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of caveolin-mediated endocytosisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cell differentiationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cell adhesionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
innate immune responseProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein phosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
symbiont entry into host cellProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
signal transductioncAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
sensory perception of smellcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
regulation of protein kinase A signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cellular response to xenobiotic stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-1B chainHomo sapiens (human)
microtubule-based processTubulin alpha-1B chainHomo sapiens (human)
cytoskeleton-dependent intracellular transportTubulin alpha-1B chainHomo sapiens (human)
cell divisionTubulin alpha-1B chainHomo sapiens (human)
cellular response to interleukin-4Tubulin alpha-1B chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-1B chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-4A chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-4A chainHomo sapiens (human)
natural killer cell mediated cytotoxicityTubulin beta-4B chainHomo sapiens (human)
mitotic cell cycleTubulin beta-4B chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-4B chainHomo sapiens (human)
neutrophil homeostasiscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
neutrophil chemotaxiscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
positive regulation of type II interferon productioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
positive regulation of interleukin-2 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
T cell receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
leukocyte migrationcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to lipopolysaccharidecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to xenobiotic stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to epinephrine stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
negative regulation of adenylate cyclase-activating adrenergic receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
regulation of cardiac muscle cell contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
negative regulation of relaxation of cardiac musclecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
regulation of heart ratecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of heart ratecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulumcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of type II interferon productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of interleukin-2 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of interleukin-5 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of peptidyl-serine phosphorylationcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of heart contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
T cell receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
establishment of endothelial barriercAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
adrenergic receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of cardiac muscle cell contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of cell communication by electrical coupling involved in cardiac conductioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of relaxation of cardiac musclecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-3 chainHomo sapiens (human)
axon guidanceTubulin beta-3 chainHomo sapiens (human)
netrin-activated signaling pathwayTubulin beta-3 chainHomo sapiens (human)
dorsal root ganglion developmentTubulin beta-3 chainHomo sapiens (human)
mitotic cell cycleTubulin beta-3 chainHomo sapiens (human)
cerebral cortex developmentTubulin beta-2A chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-2A chainHomo sapiens (human)
mitotic cell cycleTubulin beta-2A chainHomo sapiens (human)
B cell apoptotic processProgrammed cell death protein 1Homo sapiens (human)
adaptive immune responseProgrammed cell death protein 1Homo sapiens (human)
negative regulation of tolerance inductionProgrammed cell death protein 1Homo sapiens (human)
negative regulation of T cell mediated immune response to tumor cellProgrammed cell death protein 1Homo sapiens (human)
negative regulation of B cell apoptotic processProgrammed cell death protein 1Homo sapiens (human)
apoptotic processProgrammed cell death protein 1Homo sapiens (human)
humoral immune responseProgrammed cell death protein 1Homo sapiens (human)
negative regulation of immune responseProgrammed cell death protein 1Homo sapiens (human)
negative regulation of T cell activationProgrammed cell death protein 1Homo sapiens (human)
regulatory T cell apoptotic processProgrammed cell death protein 1Homo sapiens (human)
regulation of immune responseProgrammed cell death protein 1Homo sapiens (human)
positive regulation of T cell apoptotic processProgrammed cell death protein 1Homo sapiens (human)
oocyte maturationTubulin beta-8 chainHomo sapiens (human)
spindle assembly involved in female meiosisTubulin beta-8 chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-8 chainHomo sapiens (human)
mitotic cell cycleTubulin beta-8 chainHomo sapiens (human)
monoatomic anion transportSolute carrier family 22 member 6Homo sapiens (human)
response to organic cyclic compoundSolute carrier family 22 member 6Homo sapiens (human)
inorganic anion transportSolute carrier family 22 member 6Homo sapiens (human)
organic anion transportSolute carrier family 22 member 6Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 6Homo sapiens (human)
alpha-ketoglutarate transportSolute carrier family 22 member 6Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 6Homo sapiens (human)
sodium-independent organic anion transportSolute carrier family 22 member 6Homo sapiens (human)
transmembrane transportSolute carrier family 22 member 6Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 6Homo sapiens (human)
renal tubular secretionSolute carrier family 22 member 6Homo sapiens (human)
microtubule-based processTubulin beta-2B chainBos taurus (cattle)
nervous system developmentTubulin beta-2B chainBos taurus (cattle)
positive regulation of axon guidanceTubulin beta-2B chainBos taurus (cattle)
biological_processTubulin alpha-3E chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-3E chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-3E chainHomo sapiens (human)
neuron migrationTubulin alpha-1A chainHomo sapiens (human)
startle responseTubulin alpha-1A chainHomo sapiens (human)
intracellular protein transportTubulin alpha-1A chainHomo sapiens (human)
microtubule-based processTubulin alpha-1A chainHomo sapiens (human)
centrosome cycleTubulin alpha-1A chainHomo sapiens (human)
smoothened signaling pathwayTubulin alpha-1A chainHomo sapiens (human)
memoryTubulin alpha-1A chainHomo sapiens (human)
adult locomotory behaviorTubulin alpha-1A chainHomo sapiens (human)
visual learningTubulin alpha-1A chainHomo sapiens (human)
response to mechanical stimulusTubulin alpha-1A chainHomo sapiens (human)
glial cell differentiationTubulin alpha-1A chainHomo sapiens (human)
gene expressionTubulin alpha-1A chainHomo sapiens (human)
dentate gyrus developmentTubulin alpha-1A chainHomo sapiens (human)
cerebellar cortex morphogenesisTubulin alpha-1A chainHomo sapiens (human)
pyramidal neuron differentiationTubulin alpha-1A chainHomo sapiens (human)
cerebral cortex developmentTubulin alpha-1A chainHomo sapiens (human)
cytoskeleton-dependent intracellular transportTubulin alpha-1A chainHomo sapiens (human)
response to tumor necrosis factorTubulin alpha-1A chainHomo sapiens (human)
locomotory exploration behaviorTubulin alpha-1A chainHomo sapiens (human)
microtubule polymerizationTubulin alpha-1A chainHomo sapiens (human)
forebrain morphogenesisTubulin alpha-1A chainHomo sapiens (human)
homeostasis of number of cells within a tissueTubulin alpha-1A chainHomo sapiens (human)
regulation of synapse organizationTubulin alpha-1A chainHomo sapiens (human)
synapse organizationTubulin alpha-1A chainHomo sapiens (human)
cell divisionTubulin alpha-1A chainHomo sapiens (human)
neuron apoptotic processTubulin alpha-1A chainHomo sapiens (human)
motor behaviorTubulin alpha-1A chainHomo sapiens (human)
cellular response to calcium ionTubulin alpha-1A chainHomo sapiens (human)
organelle transport along microtubuleTubulin alpha-1A chainHomo sapiens (human)
neuron projection arborizationTubulin alpha-1A chainHomo sapiens (human)
response to L-glutamateTubulin alpha-1A chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-1A chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-1A chainHomo sapiens (human)
monoatomic ion transportSolute carrier family 22 member 8Homo sapiens (human)
response to toxic substanceSolute carrier family 22 member 8Homo sapiens (human)
inorganic anion transportSolute carrier family 22 member 8Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 8Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 8Homo sapiens (human)
transmembrane transportSolute carrier family 22 member 8Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 8Homo sapiens (human)
microtubule-based processTubulin alpha-1C chainHomo sapiens (human)
cytoskeleton-dependent intracellular transportTubulin alpha-1C chainHomo sapiens (human)
cell divisionTubulin alpha-1C chainHomo sapiens (human)
mitotic cell cycleTubulin alpha-1C chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin alpha-1C chainHomo sapiens (human)
mitotic cell cycleTubulin beta-6 chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-6 chainHomo sapiens (human)
neuron migrationTubulin beta-2B chainHomo sapiens (human)
microtubule-based processTubulin beta-2B chainHomo sapiens (human)
cerebral cortex developmentTubulin beta-2B chainHomo sapiens (human)
modulation of chemical synaptic transmissionTubulin beta-2B chainHomo sapiens (human)
positive regulation of axon guidanceTubulin beta-2B chainHomo sapiens (human)
embryonic brain developmentTubulin beta-2B chainHomo sapiens (human)
mitotic cell cycleTubulin beta-2B chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-2B chainHomo sapiens (human)
platelet formationTubulin beta-1 chainHomo sapiens (human)
thyroid gland developmentTubulin beta-1 chainHomo sapiens (human)
microtubule polymerizationTubulin beta-1 chainHomo sapiens (human)
spindle assemblyTubulin beta-1 chainHomo sapiens (human)
thyroid hormone transportTubulin beta-1 chainHomo sapiens (human)
platelet aggregationTubulin beta-1 chainHomo sapiens (human)
mitotic cell cycleTubulin beta-1 chainHomo sapiens (human)
microtubule cytoskeleton organizationTubulin beta-1 chainHomo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
regulation of activated T cell proliferationProgrammed cell death 1 ligand 1Homo sapiens (human)
regulation of T cell apoptotic processProgrammed cell death 1 ligand 1Homo sapiens (human)
regulation of activated CD4-positive, alpha-beta T cell apoptotic processProgrammed cell death 1 ligand 1Homo sapiens (human)
adaptive immune responseProgrammed cell death 1 ligand 1Homo sapiens (human)
negative regulation of T cell mediated immune response to tumor cellProgrammed cell death 1 ligand 1Homo sapiens (human)
immune responseProgrammed cell death 1 ligand 1Homo sapiens (human)
signal transductionProgrammed cell death 1 ligand 1Homo sapiens (human)
cell surface receptor signaling pathwayProgrammed cell death 1 ligand 1Homo sapiens (human)
positive regulation of cell migrationProgrammed cell death 1 ligand 1Homo sapiens (human)
T cell costimulationProgrammed cell death 1 ligand 1Homo sapiens (human)
negative regulation of type II interferon productionProgrammed cell death 1 ligand 1Homo sapiens (human)
negative regulation of interleukin-10 productionProgrammed cell death 1 ligand 1Homo sapiens (human)
positive regulation of interleukin-10 productionProgrammed cell death 1 ligand 1Homo sapiens (human)
response to cytokineProgrammed cell death 1 ligand 1Homo sapiens (human)
TRIF-dependent toll-like receptor signaling pathwayProgrammed cell death 1 ligand 1Homo sapiens (human)
positive regulation of T cell proliferationProgrammed cell death 1 ligand 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionProgrammed cell death 1 ligand 1Homo sapiens (human)
negative regulation of activated T cell proliferationProgrammed cell death 1 ligand 1Homo sapiens (human)
negative regulation of tumor necrosis factor superfamily cytokine productionProgrammed cell death 1 ligand 1Homo sapiens (human)
positive regulation of activated CD8-positive, alpha-beta T cell apoptotic processProgrammed cell death 1 ligand 1Homo sapiens (human)
negative regulation of CD4-positive, alpha-beta T cell proliferationProgrammed cell death 1 ligand 1Homo sapiens (human)
negative regulation of CD8-positive, alpha-beta T cell activationProgrammed cell death 1 ligand 1Homo sapiens (human)
cellular response to lipopolysaccharideProgrammed cell death 1 ligand 1Homo sapiens (human)
negative regulation of T cell proliferationProgrammed cell death 1 ligand 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (137)

Processvia Protein(s)Taxonomy
amine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-amino acid transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
choline transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
efflux transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
magnesium ion bindingTubulin polymerization-promoting proteinHomo sapiens (human)
GTPase activityTubulin polymerization-promoting proteinHomo sapiens (human)
protein bindingTubulin polymerization-promoting proteinHomo sapiens (human)
microtubule bindingTubulin polymerization-promoting proteinHomo sapiens (human)
tubulin bindingTubulin polymerization-promoting proteinHomo sapiens (human)
protein homodimerization activityTubulin polymerization-promoting proteinHomo sapiens (human)
protein dimerization activityTubulin polymerization-promoting proteinHomo sapiens (human)
microtubule nucleator activityTubulin polymerization-promoting proteinHomo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
supercoiled DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
magnesium ion bindingTyrosine-protein kinase ABL1Homo sapiens (human)
four-way junction DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
bubble DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
phosphotyrosine residue bindingTyrosine-protein kinase ABL1Homo sapiens (human)
DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
transcription coactivator activityTyrosine-protein kinase ABL1Homo sapiens (human)
actin monomer bindingTyrosine-protein kinase ABL1Homo sapiens (human)
nicotinate-nucleotide adenylyltransferase activityTyrosine-protein kinase ABL1Homo sapiens (human)
protein kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
protein kinase C bindingTyrosine-protein kinase ABL1Homo sapiens (human)
protein bindingTyrosine-protein kinase ABL1Homo sapiens (human)
ATP bindingTyrosine-protein kinase ABL1Homo sapiens (human)
kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
SH3 domain bindingTyrosine-protein kinase ABL1Homo sapiens (human)
syntaxin bindingTyrosine-protein kinase ABL1Homo sapiens (human)
manganese ion bindingTyrosine-protein kinase ABL1Homo sapiens (human)
neuropilin bindingTyrosine-protein kinase ABL1Homo sapiens (human)
SH2 domain bindingTyrosine-protein kinase ABL1Homo sapiens (human)
ephrin receptor bindingTyrosine-protein kinase ABL1Homo sapiens (human)
actin filament bindingTyrosine-protein kinase ABL1Homo sapiens (human)
mitogen-activated protein kinase bindingTyrosine-protein kinase ABL1Homo sapiens (human)
proline-rich region bindingTyrosine-protein kinase ABL1Homo sapiens (human)
delta-catenin bindingTyrosine-protein kinase ABL1Homo sapiens (human)
sequence-specific double-stranded DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
virus receptor activityEpidermal growth factor receptorHomo sapiens (human)
chromatin bindingEpidermal growth factor receptorHomo sapiens (human)
double-stranded DNA bindingEpidermal growth factor receptorHomo sapiens (human)
MAP kinase kinase kinase activityEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane signaling receptor activityEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
integrin bindingEpidermal growth factor receptorHomo sapiens (human)
protein bindingEpidermal growth factor receptorHomo sapiens (human)
calmodulin bindingEpidermal growth factor receptorHomo sapiens (human)
ATP bindingEpidermal growth factor receptorHomo sapiens (human)
enzyme bindingEpidermal growth factor receptorHomo sapiens (human)
kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein phosphatase bindingEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
ubiquitin protein ligase bindingEpidermal growth factor receptorHomo sapiens (human)
identical protein bindingEpidermal growth factor receptorHomo sapiens (human)
cadherin bindingEpidermal growth factor receptorHomo sapiens (human)
actin filament bindingEpidermal growth factor receptorHomo sapiens (human)
ATPase bindingEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor bindingEpidermal growth factor receptorHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
GTPase activityTubulin beta-4A chainHomo sapiens (human)
calcium ion bindingTubulin beta-4A chainHomo sapiens (human)
protein bindingTubulin beta-4A chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-4A chainHomo sapiens (human)
GTP bindingTubulin beta-4A chainHomo sapiens (human)
GTPase activityTubulin beta chainHomo sapiens (human)
structural molecule activityTubulin beta chainHomo sapiens (human)
protein bindingTubulin beta chainHomo sapiens (human)
protein domain specific bindingTubulin beta chainHomo sapiens (human)
ubiquitin protein ligase bindingTubulin beta chainHomo sapiens (human)
GTPase activating protein bindingTubulin beta chainHomo sapiens (human)
MHC class I protein bindingTubulin beta chainHomo sapiens (human)
protein-containing complex bindingTubulin beta chainHomo sapiens (human)
metal ion bindingTubulin beta chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta chainHomo sapiens (human)
GTP bindingTubulin beta chainHomo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
hydrolase activityTubulin alpha-3C chainHomo sapiens (human)
metal ion bindingTubulin alpha-3C chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-3C chainHomo sapiens (human)
GTP bindingTubulin alpha-3C chainHomo sapiens (human)
protein tyrosine kinase activityFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor activityFibroblast growth factor receptor 1Homo sapiens (human)
protein bindingFibroblast growth factor receptor 1Homo sapiens (human)
ATP bindingFibroblast growth factor receptor 1Homo sapiens (human)
heparin bindingFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor bindingFibroblast growth factor receptor 1Homo sapiens (human)
SH2 domain bindingFibroblast growth factor receptor 1Homo sapiens (human)
identical protein bindingFibroblast growth factor receptor 1Homo sapiens (human)
protein homodimerization activityFibroblast growth factor receptor 1Homo sapiens (human)
receptor-receptor interactionFibroblast growth factor receptor 1Homo sapiens (human)
protein kinase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein tyrosine kinase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein kinase C bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
signaling receptor bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
insulin receptor bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
integrin bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ATP bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
phospholipase activator activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
enzyme bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
heme bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
nuclear estrogen receptor bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
SH2 domain bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
phospholipase bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
transmembrane transporter bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cadherin bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ephrin receptor bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ATPase bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
phosphoprotein bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
BMP receptor bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
connexin bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
scaffold protein bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
double-stranded RNA bindingTubulin alpha-1B chainHomo sapiens (human)
GTPase activityTubulin alpha-1B chainHomo sapiens (human)
structural molecule activityTubulin alpha-1B chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-1B chainHomo sapiens (human)
protein bindingTubulin alpha-1B chainHomo sapiens (human)
GTP bindingTubulin alpha-1B chainHomo sapiens (human)
ubiquitin protein ligase bindingTubulin alpha-1B chainHomo sapiens (human)
protein bindingTubulin alpha-4A chainHomo sapiens (human)
hydrolase activityTubulin alpha-4A chainHomo sapiens (human)
protein kinase bindingTubulin alpha-4A chainHomo sapiens (human)
metal ion bindingTubulin alpha-4A chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-4A chainHomo sapiens (human)
GTP bindingTubulin alpha-4A chainHomo sapiens (human)
double-stranded RNA bindingTubulin beta-4B chainHomo sapiens (human)
GTPase activityTubulin beta-4B chainHomo sapiens (human)
protein bindingTubulin beta-4B chainHomo sapiens (human)
MHC class I protein bindingTubulin beta-4B chainHomo sapiens (human)
metal ion bindingTubulin beta-4B chainHomo sapiens (human)
unfolded protein bindingTubulin beta-4B chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-4B chainHomo sapiens (human)
GTP bindingTubulin beta-4B chainHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
calcium channel regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
gamma-tubulin bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
transmembrane transporter bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
calcium channel regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
enzyme bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
signaling receptor regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
beta-2 adrenergic receptor bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
transmembrane transporter bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
ATPase bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
scaffold protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
heterocyclic compound bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
GTPase activityTubulin beta-3 chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-3 chainHomo sapiens (human)
protein bindingTubulin beta-3 chainHomo sapiens (human)
GTP bindingTubulin beta-3 chainHomo sapiens (human)
peptide bindingTubulin beta-3 chainHomo sapiens (human)
metal ion bindingTubulin beta-3 chainHomo sapiens (human)
netrin receptor bindingTubulin beta-3 chainHomo sapiens (human)
GTPase activityTubulin beta-2A chainHomo sapiens (human)
protein bindingTubulin beta-2A chainHomo sapiens (human)
metal ion bindingTubulin beta-2A chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-2A chainHomo sapiens (human)
GTP bindingTubulin beta-2A chainHomo sapiens (human)
protein bindingProgrammed cell death protein 1Homo sapiens (human)
signaling receptor activityProgrammed cell death protein 1Homo sapiens (human)
molecular_functionTubulin beta-8 chainHomo sapiens (human)
GTPase activityTubulin beta-8 chainHomo sapiens (human)
metal ion bindingTubulin beta-8 chainHomo sapiens (human)
GTP bindingTubulin beta-8 chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-8 chainHomo sapiens (human)
solute:inorganic anion antiporter activitySolute carrier family 22 member 6Homo sapiens (human)
protein bindingSolute carrier family 22 member 6Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
alpha-ketoglutarate transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
antiporter activitySolute carrier family 22 member 6Homo sapiens (human)
transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
chloride ion bindingSolute carrier family 22 member 6Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 6Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier family 22 member 6Homo sapiens (human)
GTPase activityTubulin beta-2B chainBos taurus (cattle)
metal ion bindingTubulin beta-2B chainBos taurus (cattle)
protein heterodimerization activityTubulin beta-2B chainBos taurus (cattle)
molecular_functionTubulin alpha-3E chainHomo sapiens (human)
protein bindingTubulin alpha-3E chainHomo sapiens (human)
hydrolase activityTubulin alpha-3E chainHomo sapiens (human)
metal ion bindingTubulin alpha-3E chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-3E chainHomo sapiens (human)
GTP bindingTubulin alpha-3E chainHomo sapiens (human)
structural molecule activityTubulin alpha-1A chainHomo sapiens (human)
protein bindingTubulin alpha-1A chainHomo sapiens (human)
hydrolase activityTubulin alpha-1A chainHomo sapiens (human)
identical protein bindingTubulin alpha-1A chainHomo sapiens (human)
protein-containing complex bindingTubulin alpha-1A chainHomo sapiens (human)
metal ion bindingTubulin alpha-1A chainHomo sapiens (human)
protein heterodimerization activityTubulin alpha-1A chainHomo sapiens (human)
GTP bindingTubulin alpha-1A chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-1A chainHomo sapiens (human)
solute:inorganic anion antiporter activitySolute carrier family 22 member 8Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 8Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 8Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 8Homo sapiens (human)
structural molecule activityTubulin alpha-1C chainHomo sapiens (human)
protein bindingTubulin alpha-1C chainHomo sapiens (human)
hydrolase activityTubulin alpha-1C chainHomo sapiens (human)
metal ion bindingTubulin alpha-1C chainHomo sapiens (human)
GTP bindingTubulin alpha-1C chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin alpha-1C chainHomo sapiens (human)
molecular_functionTubulin beta-6 chainHomo sapiens (human)
GTPase activityTubulin beta-6 chainHomo sapiens (human)
protein bindingTubulin beta-6 chainHomo sapiens (human)
metal ion bindingTubulin beta-6 chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-6 chainHomo sapiens (human)
GTP bindingTubulin beta-6 chainHomo sapiens (human)
GTPase activityTubulin beta-2B chainHomo sapiens (human)
protein bindingTubulin beta-2B chainHomo sapiens (human)
metal ion bindingTubulin beta-2B chainHomo sapiens (human)
protein heterodimerization activityTubulin beta-2B chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-2B chainHomo sapiens (human)
GTP bindingTubulin beta-2B chainHomo sapiens (human)
GTPase activityTubulin beta-1 chainHomo sapiens (human)
metal ion bindingTubulin beta-1 chainHomo sapiens (human)
structural constituent of cytoskeletonTubulin beta-1 chainHomo sapiens (human)
GTP bindingTubulin beta-1 chainHomo sapiens (human)
serine-type endopeptidase inhibitor activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
transcription coactivator activityProgrammed cell death 1 ligand 1Homo sapiens (human)
protein bindingProgrammed cell death 1 ligand 1Homo sapiens (human)
receptor ligand activityProgrammed cell death 1 ligand 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (95)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
membraneSolute carrier family 22 member 2Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 2Homo sapiens (human)
presynapseSolute carrier family 22 member 2Homo sapiens (human)
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
microtubuleTubulin polymerization-promoting proteinHomo sapiens (human)
microtubule bundleTubulin polymerization-promoting proteinHomo sapiens (human)
Golgi apparatusTubulin polymerization-promoting proteinHomo sapiens (human)
nucleusTubulin polymerization-promoting proteinHomo sapiens (human)
cytoplasmTubulin polymerization-promoting proteinHomo sapiens (human)
mitochondrionTubulin polymerization-promoting proteinHomo sapiens (human)
microtubule organizing centerTubulin polymerization-promoting proteinHomo sapiens (human)
cytosolTubulin polymerization-promoting proteinHomo sapiens (human)
perinuclear region of cytoplasmTubulin polymerization-promoting proteinHomo sapiens (human)
mitotic spindleTubulin polymerization-promoting proteinHomo sapiens (human)
postsynaptic Golgi apparatusTubulin polymerization-promoting proteinHomo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
apical plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
apical plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
ruffleTyrosine-protein kinase ABL1Homo sapiens (human)
nucleusTyrosine-protein kinase ABL1Homo sapiens (human)
nucleoplasmTyrosine-protein kinase ABL1Homo sapiens (human)
nucleolusTyrosine-protein kinase ABL1Homo sapiens (human)
cytoplasmTyrosine-protein kinase ABL1Homo sapiens (human)
mitochondrionTyrosine-protein kinase ABL1Homo sapiens (human)
cytosolTyrosine-protein kinase ABL1Homo sapiens (human)
actin cytoskeletonTyrosine-protein kinase ABL1Homo sapiens (human)
nuclear bodyTyrosine-protein kinase ABL1Homo sapiens (human)
dendriteTyrosine-protein kinase ABL1Homo sapiens (human)
growth coneTyrosine-protein kinase ABL1Homo sapiens (human)
nuclear membraneTyrosine-protein kinase ABL1Homo sapiens (human)
neuronal cell bodyTyrosine-protein kinase ABL1Homo sapiens (human)
perinuclear region of cytoplasmTyrosine-protein kinase ABL1Homo sapiens (human)
postsynapseTyrosine-protein kinase ABL1Homo sapiens (human)
protein-containing complexTyrosine-protein kinase ABL1Homo sapiens (human)
plasma membraneTyrosine-protein kinase ABL1Homo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
ruffle membraneEpidermal growth factor receptorHomo sapiens (human)
Golgi membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceEpidermal growth factor receptorHomo sapiens (human)
nucleusEpidermal growth factor receptorHomo sapiens (human)
cytoplasmEpidermal growth factor receptorHomo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
endoplasmic reticulum membraneEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
focal adhesionEpidermal growth factor receptorHomo sapiens (human)
cell surfaceEpidermal growth factor receptorHomo sapiens (human)
endosome membraneEpidermal growth factor receptorHomo sapiens (human)
membraneEpidermal growth factor receptorHomo sapiens (human)
basolateral plasma membraneEpidermal growth factor receptorHomo sapiens (human)
apical plasma membraneEpidermal growth factor receptorHomo sapiens (human)
cell junctionEpidermal growth factor receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneEpidermal growth factor receptorHomo sapiens (human)
early endosome membraneEpidermal growth factor receptorHomo sapiens (human)
nuclear membraneEpidermal growth factor receptorHomo sapiens (human)
membrane raftEpidermal growth factor receptorHomo sapiens (human)
perinuclear region of cytoplasmEpidermal growth factor receptorHomo sapiens (human)
multivesicular body, internal vesicle lumenEpidermal growth factor receptorHomo sapiens (human)
intracellular vesicleEpidermal growth factor receptorHomo sapiens (human)
protein-containing complexEpidermal growth factor receptorHomo sapiens (human)
receptor complexEpidermal growth factor receptorHomo sapiens (human)
Shc-EGFR complexEpidermal growth factor receptorHomo sapiens (human)
basal plasma membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
nucleusTubulin beta-4A chainHomo sapiens (human)
cytosolTubulin beta-4A chainHomo sapiens (human)
microtubuleTubulin beta-4A chainHomo sapiens (human)
axonemeTubulin beta-4A chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-4A chainHomo sapiens (human)
internode region of axonTubulin beta-4A chainHomo sapiens (human)
neuronal cell bodyTubulin beta-4A chainHomo sapiens (human)
myelin sheathTubulin beta-4A chainHomo sapiens (human)
intercellular bridgeTubulin beta-4A chainHomo sapiens (human)
extracellular exosomeTubulin beta-4A chainHomo sapiens (human)
mitotic spindleTubulin beta-4A chainHomo sapiens (human)
microtubuleTubulin beta-4A chainHomo sapiens (human)
cytoplasmTubulin beta-4A chainHomo sapiens (human)
extracellular regionTubulin beta chainHomo sapiens (human)
nucleusTubulin beta chainHomo sapiens (human)
nuclear envelope lumenTubulin beta chainHomo sapiens (human)
cytoplasmTubulin beta chainHomo sapiens (human)
cytosolTubulin beta chainHomo sapiens (human)
cytoskeletonTubulin beta chainHomo sapiens (human)
microtubuleTubulin beta chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta chainHomo sapiens (human)
azurophil granule lumenTubulin beta chainHomo sapiens (human)
cytoplasmic ribonucleoprotein granuleTubulin beta chainHomo sapiens (human)
cell bodyTubulin beta chainHomo sapiens (human)
membrane raftTubulin beta chainHomo sapiens (human)
intercellular bridgeTubulin beta chainHomo sapiens (human)
extracellular exosomeTubulin beta chainHomo sapiens (human)
mitotic spindleTubulin beta chainHomo sapiens (human)
protein-containing complexTubulin beta chainHomo sapiens (human)
cytoplasmTubulin beta chainHomo sapiens (human)
microtubuleTubulin beta chainHomo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
nucleusTubulin alpha-3C chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-3C chainHomo sapiens (human)
microtubuleTubulin alpha-3C chainHomo sapiens (human)
cytoplasmTubulin alpha-3C chainHomo sapiens (human)
extracellular regionFibroblast growth factor receptor 1Homo sapiens (human)
nucleusFibroblast growth factor receptor 1Homo sapiens (human)
cytosolFibroblast growth factor receptor 1Homo sapiens (human)
plasma membraneFibroblast growth factor receptor 1Homo sapiens (human)
membraneFibroblast growth factor receptor 1Homo sapiens (human)
cytoplasmic vesicleFibroblast growth factor receptor 1Homo sapiens (human)
receptor complexFibroblast growth factor receptor 1Homo sapiens (human)
plasma membraneFibroblast growth factor receptor 1Homo sapiens (human)
podosomeProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
nucleoplasmProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cytoplasmProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
mitochondrionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
mitochondrial inner membraneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
lysosomeProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
late endosomeProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cytosolProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
actin filamentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
plasma membraneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
caveolaProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
focal adhesionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cell junctionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ruffle membraneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
neuronal cell bodyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
dendritic growth coneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
membrane raftProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
perinuclear region of cytoplasmProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
extracellular exosomeProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
synaptic membraneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
glutamatergic synapseProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
postsynaptic specialization, intracellular componentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
dendritic filopodiumProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
plasma membraneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
nucleoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
ruffle membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
plasma membraneMu-type opioid receptorMus musculus (house mouse)
microtubule cytoskeletonTubulin alpha-1B chainHomo sapiens (human)
microtubuleTubulin alpha-1B chainHomo sapiens (human)
cytoplasmic microtubuleTubulin alpha-1B chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-1B chainHomo sapiens (human)
microtubuleTubulin alpha-1B chainHomo sapiens (human)
cytoplasmTubulin alpha-1B chainHomo sapiens (human)
extracellular regionTubulin alpha-4A chainHomo sapiens (human)
cytosolTubulin alpha-4A chainHomo sapiens (human)
cytoskeletonTubulin alpha-4A chainHomo sapiens (human)
microtubuleTubulin alpha-4A chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-4A chainHomo sapiens (human)
extracellular exosomeTubulin alpha-4A chainHomo sapiens (human)
cytoplasmTubulin alpha-4A chainHomo sapiens (human)
microtubuleTubulin alpha-4A chainHomo sapiens (human)
extracellular regionTubulin beta-4B chainHomo sapiens (human)
nucleusTubulin beta-4B chainHomo sapiens (human)
cytosolTubulin beta-4B chainHomo sapiens (human)
cytoskeletonTubulin beta-4B chainHomo sapiens (human)
microtubuleTubulin beta-4B chainHomo sapiens (human)
axonemal microtubuleTubulin beta-4B chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-4B chainHomo sapiens (human)
azurophil granule lumenTubulin beta-4B chainHomo sapiens (human)
intercellular bridgeTubulin beta-4B chainHomo sapiens (human)
extracellular exosomeTubulin beta-4B chainHomo sapiens (human)
mitotic spindleTubulin beta-4B chainHomo sapiens (human)
extracellular vesicleTubulin beta-4B chainHomo sapiens (human)
microtubuleTubulin beta-4B chainHomo sapiens (human)
cytoplasmTubulin beta-4B chainHomo sapiens (human)
centrosomecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
synaptic vesiclecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
postsynaptic densitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
Z disccAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
dendritic spinecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
excitatory synapsecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
gamma-tubulin complexcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
voltage-gated calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
extracellular spacecAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
ciliumcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
centrosomecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
apical plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
voltage-gated calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
microtubule cytoskeletonTubulin beta-3 chainHomo sapiens (human)
nucleusTubulin beta-3 chainHomo sapiens (human)
microtubuleTubulin beta-3 chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-3 chainHomo sapiens (human)
lamellipodiumTubulin beta-3 chainHomo sapiens (human)
filopodiumTubulin beta-3 chainHomo sapiens (human)
axonTubulin beta-3 chainHomo sapiens (human)
dendriteTubulin beta-3 chainHomo sapiens (human)
growth coneTubulin beta-3 chainHomo sapiens (human)
neuronal cell bodyTubulin beta-3 chainHomo sapiens (human)
intercellular bridgeTubulin beta-3 chainHomo sapiens (human)
extracellular exosomeTubulin beta-3 chainHomo sapiens (human)
cell peripheryTubulin beta-3 chainHomo sapiens (human)
mitotic spindleTubulin beta-3 chainHomo sapiens (human)
microtubuleTubulin beta-3 chainHomo sapiens (human)
cytoplasmTubulin beta-3 chainHomo sapiens (human)
nucleusTubulin beta-2A chainHomo sapiens (human)
microtubuleTubulin beta-2A chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-2A chainHomo sapiens (human)
intercellular bridgeTubulin beta-2A chainHomo sapiens (human)
extracellular exosomeTubulin beta-2A chainHomo sapiens (human)
mitotic spindleTubulin beta-2A chainHomo sapiens (human)
extracellular vesicleTubulin beta-2A chainHomo sapiens (human)
cytoplasmTubulin beta-2A chainHomo sapiens (human)
microtubuleTubulin beta-2A chainHomo sapiens (human)
plasma membraneProgrammed cell death protein 1Homo sapiens (human)
external side of plasma membraneProgrammed cell death protein 1Homo sapiens (human)
microtubule cytoskeletonTubulin beta-8 chainHomo sapiens (human)
intercellular bridgeTubulin beta-8 chainHomo sapiens (human)
extracellular exosomeTubulin beta-8 chainHomo sapiens (human)
mitotic spindleTubulin beta-8 chainHomo sapiens (human)
meiotic spindleTubulin beta-8 chainHomo sapiens (human)
microtubuleTubulin beta-8 chainHomo sapiens (human)
cytoplasmTubulin beta-8 chainHomo sapiens (human)
plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
caveolaSolute carrier family 22 member 6Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 6Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 6Homo sapiens (human)
protein-containing complexSolute carrier family 22 member 6Homo sapiens (human)
microtubule cytoskeletonTubulin beta-2B chainBos taurus (cattle)
nucleusTubulin alpha-3E chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-3E chainHomo sapiens (human)
microtubuleTubulin alpha-3E chainHomo sapiens (human)
cytoplasmTubulin alpha-3E chainHomo sapiens (human)
condensed chromosomeTubulin alpha-1A chainHomo sapiens (human)
nucleusTubulin alpha-1A chainHomo sapiens (human)
cytosolTubulin alpha-1A chainHomo sapiens (human)
microtubuleTubulin alpha-1A chainHomo sapiens (human)
axonemal microtubuleTubulin alpha-1A chainHomo sapiens (human)
plasma membraneTubulin alpha-1A chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-1A chainHomo sapiens (human)
neuromuscular junctionTubulin alpha-1A chainHomo sapiens (human)
cytoplasmic ribonucleoprotein granuleTubulin alpha-1A chainHomo sapiens (human)
recycling endosomeTubulin alpha-1A chainHomo sapiens (human)
extracellular exosomeTubulin alpha-1A chainHomo sapiens (human)
microtubuleTubulin alpha-1A chainHomo sapiens (human)
cytoplasmTubulin alpha-1A chainHomo sapiens (human)
plasma membraneSolute carrier family 22 member 8Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 8Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 8Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 8Homo sapiens (human)
nucleusTubulin alpha-1C chainHomo sapiens (human)
microtubuleTubulin alpha-1C chainHomo sapiens (human)
cytoplasmic microtubuleTubulin alpha-1C chainHomo sapiens (human)
microtubule cytoskeletonTubulin alpha-1C chainHomo sapiens (human)
vesicleTubulin alpha-1C chainHomo sapiens (human)
membrane raftTubulin alpha-1C chainHomo sapiens (human)
microtubuleTubulin alpha-1C chainHomo sapiens (human)
cytoplasmTubulin alpha-1C chainHomo sapiens (human)
nucleusTubulin beta-6 chainHomo sapiens (human)
microtubuleTubulin beta-6 chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-6 chainHomo sapiens (human)
intercellular bridgeTubulin beta-6 chainHomo sapiens (human)
extracellular exosomeTubulin beta-6 chainHomo sapiens (human)
mitotic spindleTubulin beta-6 chainHomo sapiens (human)
cytoplasmTubulin beta-6 chainHomo sapiens (human)
microtubuleTubulin beta-6 chainHomo sapiens (human)
nucleusTubulin beta-2B chainHomo sapiens (human)
microtubuleTubulin beta-2B chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-2B chainHomo sapiens (human)
intercellular bridgeTubulin beta-2B chainHomo sapiens (human)
mitotic spindleTubulin beta-2B chainHomo sapiens (human)
Schaffer collateral - CA1 synapseTubulin beta-2B chainHomo sapiens (human)
microtubuleTubulin beta-2B chainHomo sapiens (human)
cytoplasmTubulin beta-2B chainHomo sapiens (human)
cytoplasmTubulin beta-1 chainHomo sapiens (human)
microtubule cytoskeletonTubulin beta-1 chainHomo sapiens (human)
intercellular bridgeTubulin beta-1 chainHomo sapiens (human)
extracellular exosomeTubulin beta-1 chainHomo sapiens (human)
mitotic spindleTubulin beta-1 chainHomo sapiens (human)
microtubuleTubulin beta-1 chainHomo sapiens (human)
cytoplasmTubulin beta-1 chainHomo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
nucleusProgrammed cell death 1 ligand 1Homo sapiens (human)
nucleoplasmProgrammed cell death 1 ligand 1Homo sapiens (human)
plasma membraneProgrammed cell death 1 ligand 1Homo sapiens (human)
actin cytoskeletonProgrammed cell death 1 ligand 1Homo sapiens (human)
early endosome membraneProgrammed cell death 1 ligand 1Homo sapiens (human)
recycling endosome membraneProgrammed cell death 1 ligand 1Homo sapiens (human)
extracellular exosomeProgrammed cell death 1 ligand 1Homo sapiens (human)
external side of plasma membraneProgrammed cell death 1 ligand 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (3689)

Assay IDTitleYearJournalArticle
AID1376372Induction of necrosis in human luc-GFP-mCherry-tagged MCF7 cells implanted in SCID-NOD mouse at 120 mg/kg, ip administered as single dose measured after 48 hrs by haematoxylin and eosin staining based microscopy
AID1353848In vivo antiangiogenic activity in chicken embryo chorioallantoic membrane at 50 uM/disc after 48 hrs by microscopic method2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and structure-activity relationships of asymmetric dimeric β-carboline derivatives as potential antitumor agents.
AID536412Relative resistance, ratio of IC50 for human SKOV3 cells expressing MDR1-6/6 to IC50 for human SKOV3 cells2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.
AID1871665Antitumor activity against human HepG2 xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 50 mg/kg, iv administered every 2 days and measured upto 30 days relative to control2022European journal of medicinal chemistry, Feb-05, Volume: 229Current status of carbazole hybrids as anticancer agents.
AID1376369Growth inhibition of human SKOV3 cells after 48 hrs by SRB assay
AID1308612Antitumor activity against human A549 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 30 mg/kg, ip administered every other day for 1 month measured every other day post dose relative to vehicle-treated control2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID536414Antiproliferative activity against human HeLa cells expressing tubulin 3beta by sulforhodamine B assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.
AID536415Relative resistance, ratio of IC50 for human HeLa cells expressing tubulin 3beta to IC50 for human HeLa cells2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.
AID1740977Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Oct-01, Volume: 203Discovery of tertiary amide derivatives incorporating benzothiazole moiety as anti-gastric cancer agents in vitro via inhibiting tubulin polymerization and activating the Hippo signaling pathway.
AID1376370Induction of vascular disruption in human luc-GFP-mCherry-tagged MCF7 cells implanted in SCID-NOD mouse assessed as reduction in bioluminescence at 120 mg/kg, ip administered as single dose measured at 4 hrs post dose by luciferase reporter gene based ima
AID1887895Antitumor activity against human MHCC97H cells xenografted in BALB/c mouse assessed as tumor weight at 30 mg/kg, ip administered every other day for 30 days2022European journal of medicinal chemistry, Jan-05, Volume: 227Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR.
AID1376365Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured after 20 mins by spectrophotometric method
AID1376367Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
AID536404Inhibition of microtubule depolymerization in rat A10 cells assessed as reorganization of interphase microtubule network by indirect immunofluorescence technique2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.
AID536410Antiproliferative activity against human SKOV3 cells by sulforhodamine B assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.
AID1335310Antiproliferative activity against human EAhy926 cells measured after 48 hrs by MTT assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Synthesis and biological evaluation of novel alkyl diamine linked bivalent β-carbolines as angiogenesis inhibitors.
AID1740978Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Oct-01, Volume: 203Discovery of tertiary amide derivatives incorporating benzothiazole moiety as anti-gastric cancer agents in vitro via inhibiting tubulin polymerization and activating the Hippo signaling pathway.
AID1376368Growth inhibition of human DU145 cells after 48 hrs by SRB assay
AID1887892Antitumor activity against human MHCC97H cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 30 mg/kg, ip administered every other day for 30 days2022European journal of medicinal chemistry, Jan-05, Volume: 227Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR.
AID1740976Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Oct-01, Volume: 203Discovery of tertiary amide derivatives incorporating benzothiazole moiety as anti-gastric cancer agents in vitro via inhibiting tubulin polymerization and activating the Hippo signaling pathway.
AID1321614Antiproliferative activity against human EAhy926 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Design, synthesis and biological evaluation of novel alkyl diamine linked bivalent β-carbolines as angiogenesis inhibitors.
AID1757336Antitumor activity against human H22 cells xenografted in ICR mouse assessed as reduction of tumor weight at 20 mg/kg/day, iv for 21 days2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID536411Antiproliferative activity against human SKOV3 cells expressing MDR1-6/6 by sulforhodamine B assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.
AID1887896Antitumor activity against human MHCC97H cells xenografted in BALB/c mouse assessed as tumor volume at 30 mg/kg, ip administered every other day for 30 days2022European journal of medicinal chemistry, Jan-05, Volume: 227Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR.
AID536413Antiproliferative activity against human HeLa cells by sulforhodamine B assay2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.
AID1469265Antitumor activity against human A549 cells xenografted in Balb/c mouse assessed as tumor growth inhibition at 30 mg/kg, ip treated once in 2 days for 10 days relative to control2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1162815Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID1458821Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1263266Cytotoxicity against human SNB75 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1338083Antiproliferative activity against human A2780 cells measured after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of cyclic-indole derivatives as anti-tumor agents via the inhibition of tubulin polymerization.
AID1288168Inhibition of porcine brain tubulin polymerization at 10 uM measured for 1 hr by fluorescence assay2016European journal of medicinal chemistry, May-23, Volume: 114Synthesis and biological evaluation of quinoline analogues of flavones as potential anticancer agents and tubulin polymerization inhibitors.
AID502527Cytotoxicity against human K562 cells after 5 days by MTT assay2010Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18
1,2,3-triazole analogs of combretastatin A-4 as potential microtubule-binding agents.
AID106340Cell growth inhibition against,MES-SA/DX5 human uterine cancer cells using MTS assay2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
AID1176809Cytotoxicity against human HT1080 cells assessed as cell growth inhibition after 72 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Microwave-assisted synthesis and biological evaluation of 3,4-diaryl maleic anhydride/N-substituted maleimide derivatives as combretastatin A-4 analogues.
AID1353635Antiproliferative activity against HEK293 cells after 2 days by MTT assay2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID1486474Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis, biological evaluation and molecular modeling of imidazo[1,2-a]pyridine derivatives as potent antitubulin agents.
AID280071Cytotoxicity against human HeLa cells2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID1737844Intrinsic clearance in human liver microsomes at 10 uM incubated for 60 mins in presence of NADPH by LC/MS/MS analysis2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID93843Compound was tested for cell arrest at S phase at 100 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID662358Induction of apoptosis in human HuTu 80 cells assessed as PARP cleavage at 30 nM after 16 hrs by Western blot analysis2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID1773177Induction of apoptosis in human U-251 cells assessed as increase in late apoptotic cells at 200 nM measured after 24 hrs by PI/FITC analysis (Rvb = 0.311%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1646995Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1535573Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Synthesis, biological evaluation and molecular docking of benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives as novel tubulin polymerization inhibitors.
AID103371Mitotic index in MCF-7 breast cancer cells was determined2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Antineoplastic agents. 487. Synthesis and biological evaluation of the antineoplastic agent 3,4-methylenedioxy-5,4'-dimethoxy-3'-amino-Z-stilbene and derived amino acid amides.
AID1294501Growth inhibition of human MCF7 cells after 3 days by MTT assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1408397Induction of apoptosis in human K562 cells after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1906248Induction of apoptosis in human HeLa cells assessed as necrotic cells at 1.5 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 0.45%)
AID778977Cytotoxicity against human NCI-H460 cells after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and biological evaluation of indole-based, anti-cancer agents inspired by the vascular disrupting agent 2-(3'-hydroxy-4'-methoxyphenyl)-3-(3″,4″,5″-trimethoxybenzoyl)-6-methoxyindole (OXi8006).
AID1399374Antiproliferative activity against human SKOV3 cells after 72 hrs by sulforhodamine B assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and preclinical evaluation of 5-methyl-N
AID1727317Antiproliferative activity against human HT-29 cells assessed as cell viability after 24 hrs by Celltiter-Glo assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation.
AID281348Cytotoxicity against human Hep2 cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID595726Binding affinity at lamb tubulin by spectrofluorimetric analysis2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Synthesis and biological evaluation of 4-arylcoumarin analogues of combretastatins. Part 2.
AID590530Inhibition of tubulin polymerization in human K562 cells by fluorometric analysis2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Design, synthesis, and biological evaluation of novel γ-carboline ketones as anticancer agents.
AID1729296Antiproliferative activity against mouse MC38 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
AID1647029Toxicity in ICR mouse xenografted with mouse H22 cells assessed as effect on body weight at 30 mg/kg, iv administered once daily for 21 consecutive days measured every 2 days for 21 days2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1459295Binding affinity to colchicine-binding site of beta tubulin in human HT-29 cells assessed as inhibition of formation of protein-N,N'-Ethylene-bis(iodoacetamide) adduct at 10 uM after 2 hrs by Western blot method2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1409113Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.
AID293350Cell cycle arrest in HMEC1 cells assessed as accumulation at S phase at 50 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID512244Cell cycle arrest in human A375 cells assessed as accumulation at S phase at 4 uM after 24 hrs using propidium iodide staining by FACS2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis and biological evaluation of 3,5-diaryl-isoxazoline/isoxazole-pyrrolobenzodiazepine conjugates as potential anticancer agents.
AID1233571Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model.
AID382576Cytotoxicity against human SK-BR3 cells assessed as [3H]thymidine incorporation after 72 hrs by microplate scintillation counter2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin.
AID580346Antiproliferative activity against sea urchin embryo assessed as cleavage alteration after 10 to 15 mins fertilization 45 to 60 mins before first mitotic cycle completion2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Application of plant allylpolyalkoxybenzenes in synthesis of antimitotic phenstatin analogues.
AID691615Toxicity in ICR mouse assessed as mortality at 50 mg/kg, ip administered on day 12012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1462296Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis of different heterocycles-linked chalcone conjugates as cytotoxic agents and tubulin polymerization inhibitors.
AID1294465Growth inhibition of human HL-60(TB) cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID502722Growth inhibition of human KM12 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1233619Growth inhibition of human MCF7 cells assessed as inhibition of cell proliferation after 24 hrs by MTT assay2015European journal of medicinal chemistry, Jun-24, Volume: 99Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin polymerization inhibitors.
AID1486471Cytotoxicity against human NCI-H460 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis, biological evaluation and molecular modeling of imidazo[1,2-a]pyridine derivatives as potent antitubulin agents.
AID1327137Inhibition of porcine brain tubulin polymerization measured after 60 mins by fluorescence analysis2016European journal of medicinal chemistry, Oct-21, Volume: 1224,5-Diaryl-3H-1,2-dithiole-3-thiones and related compounds as combretastatin A-4/oltipraz hybrids: Synthesis, molecular modelling and evaluation as antiproliferative agents and inhibitors of tubulin.
AID538693Inhibition of bovine brain tubulin polymerization by turbidimetric analysis2010Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
Synthesis, molecular modeling and biological evaluation of guanidine derivatives as novel antitubulin agents.
AID288669Inhibition of [3H]colchicine binding to tubulin at 5 uM2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies.
AID1771518Induction of apoptosis in human MGC-803 cells assessed as early apoptotic cells at 2 nM measured after 48 hrs by Annexin V-APC/PI double staining based flow cytometry assay (Rvb = 2.42 %)2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID444163Antiproliferative activity against human SKOV3 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID685173Growth inhibition of human SR cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1308560Resistance index, ratio of IC50 for human A549/CDDP cells to IC50 for human A549 cells2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID642053Displacement of [3H]colchicine from tubulin at 5 uM after 10 mins2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID617007Inhibition of bovine brain tubulin assembly in A-10 cells2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID93842Compound was tested for cell arrest at Go/G1 phase at 50 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID286488Inhibition of bovine brain tubulin polymerization2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID1887829Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR.
AID626627Displacement of N,N'-ethylenebis(iodoacetamide) from beta-tubulin colchicine-binding site in human MDA-MB-231 cells at 1000 times IC50 preincubated for 2 hrs before N,N'-ethylenebis(iodoacetamide) addition measured after 1.5 hrs by chemiluminescence assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID195112In vitro cytotoxic activity was tested against human renal cancer (A498) cell line2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.
AID502741Growth inhibition of human SKOV3 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1324109Cytotoxicity against human SF539 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID607533Inhibition of tubulin alpha polymerization in human HeLa cells assessed as increase in soluble tubulin alpha fraction at 3 times IC50 value after 16 hrs by Western blotting in presence of paclitaxel2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues.
AID1263261Cytotoxicity against human SW620 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1183784Cell cycle arrest in human K562 cells assessed as mitotic index at 0.1 nM (Rvb = 3 +/- 1%)2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID486868Inhibition of bovine brain tubulin assembly after 20 mins2010Journal of natural products, Jun-25, Volume: 73, Issue:6
Regio- and stereospecific synthesis of mono-beta-d-glucuronic acid derivatives of combretastatin A-1.
AID1064414Growth inhibition of human HCT15 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID214718Percent inhibition of colchicine binding(ICB) at 1(+/-)uM [3H]colchicine concentration2001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Antitumor Agents. 211. Fluorinated 2-phenyl-4-quinolone derivatives as antimitotic antitumor agents.
AID1317604Cell cycle arrest in human HepG2 cells assessed as accumulation of hypoploid sub-G1 cells at growth inhibitory IC50 measured after 72 hrs by propidium iodide-staining based FACS analysis2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID281345Cytotoxicity against human KB cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID717161Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
AID1824152Disruption of microtubule network in human MCF7 cells at 20 nM measured after 48 hrs by DAPI staining based immunofluorescence microscopic assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Branched alkyl of phenyl 4-(2-oxo-3-alkylimidazolidin-1-yl)benzenesulfonates as unique cytochrome P450 1A1-activated antimitotic prodrugs: Biological evaluation and mechanism of bioactivation.
AID427180Inhibition of bovine brain tubulin polymerization by turbidimetry2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization.
AID1860238Induction of apoptosis in human HepG2 cells assessed as induction of mitochondrial membrane potential collapse at 200 nM measured after 48 hrs by JC-1 probe based flow cytometry2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-functional antitumor conjugates improving the anti-metastasis effect of combretastatin A4 by targeting tubulin polymerization and matrix metalloproteinases.
AID1860229Cell cycle arrest in human HepG2 cells assessed as accumulation of cells in G1 phase at 100 nM measured after 12 hrs by flow cytometry method (Rvb = 53.51%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-functional antitumor conjugates improving the anti-metastasis effect of combretastatin A4 by targeting tubulin polymerization and matrix metalloproteinases.
AID1409114Inhibition of [3H]-colchicine binding to tubulin (unknown origin) at 5 uM relative to control2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.
AID269718Cell cycle arrest in SHSY5Y cells by accumulation at G2 phase after 4 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID89700Evaluated for growth inhibition (anticancer activity) of Human lung-NSC cancer NCI-H460 cell line2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID1308561Cytotoxicity against human MCF7/DX cells assessed as growth inhibition after 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID502729Growth inhibition of human MALME-3M cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1351629Induction of apoptosis in human HaCaT cells assessed as increase in histone-associated DNA fragments in mononucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1524359Cell cycle arrest in human K562 cells assessed as mitotic index at 5 times IC50 by Giemsa staining-based assay (Rvb = 3%)2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents.
AID290173Antiproliferative activity against human Molt3 cells2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents.
AID391282Displacement of [3H]colchicine from tubulin by scintillation proximity assay2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Novel A-ring and B-ring modified combretastatin A-4 (CA-4) analogues endowed with interesting cytotoxic activity.
AID717145Inhibition of bovine brain tubulin polymerization preincubated for 15 mins by turbidimetric analysis2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
AID1317600Cell cycle arrest in human HepG2 cells assessed as accumulation of cells with 4N DNA content at growth inhibitory IC50 measured after 24 hrs by propidium iodide-staining based FACS analysis relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1729295Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
AID723245Cytotoxicity against human K562 cells after 48 hrs by MTT assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Design and synthesis of cyclopropylamide analogues of combretastatin-A4 as novel microtubule-stabilizing agents.
AID1196871Cell cycle arrest in human SH-SY5Y cells assessed as accumulation at G2/M phase at IC50 after 16 hrs by flow cytometry (Rvb = 18.5 %)2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID514404Inhibition of tubulin assembly2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents.
AID761834Displacement of [3H]colchicine from bovine brain tubulin at 1 uM after 10 mins by scintillation counting analysis relative to control2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity.
AID751573Ratio of EC50 for induction of microtubule depolymerization in rat A10 cells to IC50 for human MDA-MB-435 cells2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.
AID397287Cytotoxicity against human NCI60 cells2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Isocombretastatins a versus combretastatins a: the forgotten isoCA-4 isomer as a highly promising cytotoxic and antitubulin agent.
AID1534366Selectivity index, ratio of IC50 for human LO2 cells to IC50 for human HepG2 cells2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
AID1196868Inhibition of tubulin polymerization in human SH-SY5Y cells at 3 times IC50 after 16 hrs by Western blot analysis2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID1690539Antiproliferative activity against human HepG2 cells measured after 48 hrs by SRB assay2020European journal of medicinal chemistry, Apr-01, Volume: 191Synthesis and structure-activity relationship study of water-soluble carbazole sulfonamide derivatives as new anticancer agents.
AID626630Toxicity against fertilized chicken embryo assessed as mortality at 3 ug, iv by CAM assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID306518Cell cycle arrest in human M21 cells assessed as accumulation at S phase at 0.125 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID348401Antiproliferative activity against mouse L1210 cells2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID273085Antiproliferative activity against human DND1 cells after 72 hrs2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and structure-activity relationships of carbazole sulfonamides as a novel class of antimitotic agents against solid tumors.
AID247233Growth inhibition against human thyroid cell line( SW 1736) 2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID1263249Cytotoxicity against human SR cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1196875Cell cycle arrest in human SH-SY5Y cells assessed as accumulation at G0G1 phase at IC50 after 16 hrs by flow cytometry (Rvb = 70.2 %)2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID512245Cell cycle arrest in human A375 cells assessed as accumulation at G2/M phase at 4 uM after 24 hrs using propidium iodide staining by FACS2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis and biological evaluation of 3,5-diaryl-isoxazoline/isoxazole-pyrrolobenzodiazepine conjugates as potential anticancer agents.
AID451276Cytotoxicity against human PC3 cells after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Synthesis and biological evaluation of 3,4-diaryl-5-aminoisoxazole derivatives.
AID691646Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as effect on WBC count at 30 mg/kg, ip qd after 21 days (Rvb = 25.38 +/- 0.22 x 10'3 mm'-3)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID277282Cytotoxicity against P-glycoprotein-overexpressing KB-V1 cell line2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Highly potent triazole-based tubulin polymerization inhibitors.
AID1422792Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
AID1406426Antitumor activity against human HeLa cells xenografted in nude mouse assessed as tumor weight at 10 mg/kg, ip after 14 days (Rvb = 1.54 g)2018European journal of medicinal chemistry, Aug-05, Volume: 156Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation.
AID1771502Induction of cell cycle arrest in human MGC-803 cells assessed as accumulation at G1 phase at 2 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb =39.64 %)2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1731560Antiproliferative activity against human SEM cells assessed as reduction in cell viability after 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents.
AID1711843Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID665828Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 2 uM after 48 hrs by annexin-V FITC/propidium iodide staining based FACS analysis2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID342521Inhibition of tubulin polymerization2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Synthesis and biological evaluation of new disubstituted analogues of 6-methoxy-3-(3',4',5'-trimethoxybenzoyl)-1H-indole (BPR0L075), as potential antivascular agents.
AID1294476Growth inhibition of human SNB75 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1274777Cytotoxicity against human MCF7 cells assessed as induction of cell death at 10 uM after 72 hrs by LDH assay2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Synthesis and Biochemical Evaluation of 3-Phenoxy-1,4-diarylazetidin-2-ones as Tubulin-Targeting Antitumor Agents.
AID1882896Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID691642Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as body weight change at 50 mg/kg, ip qd after 21 days (Rvb = 2.7 g)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID502749Growth inhibition of human DU145 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID643526Cytotoxicity against human HeLa cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Synthesis and evaluation of 1,5-disubstituted tetrazoles as rigid analogues of combretastatin A-4 with potent antiproliferative and antitumor activity.
AID1064416Growth inhibition of human HCT116 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID421861Antitumor activity against human KM20L2 cells by sulforhodamine B assay2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Antineoplastic agents. 578. Synthesis of stilstatins 1 and 2 and their water-soluble prodrugs.
AID1906268Aqueous solubility of compound at pH 7.4 in phosphate buffer incubated overnight by HPLC analysis
AID1572254Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.
AID1406453Antitumor activity against human HeLa cells xenografted in nude mouse assessed as loose and irregular arrangement of tumor cells at 10 mg/kg, ip after 14 days by hematoxylin and eosin staining based microscopic analysis2018European journal of medicinal chemistry, Aug-05, Volume: 156Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation.
AID1689069Anticancer activity against human PC3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1411589Aqueous solubility of the compound after 1 hrs by HPLC-UV method2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID767874Cytotoxicity against human DU145 cells by SRB assay2013Journal of natural products, Sep-27, Volume: 76, Issue:9
Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.
AID769748Displacement of [3H]-colchicine from pig brain tubulin at 1 uM after 10 mins by scintillation counting analysis relative to control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.
AID1906269Aqueous solubility of compound at pH 2.0 in phosphate buffer incubated overnight by HPLC analysis
AID745606Inhibition of tubulin polymerization (unknown origin) at 3 uM after 1 hr by fluorescence plate reader analysis2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Site-specific and far-red-light-activatable prodrug of combretastatin A-4 using photo-unclick chemistry.
AID1408383Cell cycle arrest in human K562 cells assessed as accumulation at G2 phase at 0.005 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 9.51%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID685206Growth inhibition of human OVCAR5 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1550344Inhibition of microtubule formation in human SGC7901 cells assessed as mitotic catastrophe at 2 fold IC50 concentration measured after 24 hrs by DAPI staining based fluorescence microscopy2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and bioevaluation of diarylpyrazoles as antiproliferative agents.
AID1585983Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
AID305461Cell cycle arrest in human HepG2 cells assessed as accumulation at G0/G1 phase at 10 uM after 24 hrs relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and cytotoxic activities of 4,5-diarylisoxazoles.
AID214721Percent inhibition of colchicine(5 uM) binding to tubulin(10 uM) at the compound concentration of 5 uM)2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.
AID1832147Metabolic stability in human liver microsomes assessed as parent compound remaining after 90 mins2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID1406349Inhibition of porcine brain tubulin polymerization measured over 30 mins2018European journal of medicinal chemistry, Aug-05, Volume: 156Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation.
AID1873730Induction of apoptosis in human HeLa cells assessed as late apoptotic cells at 10 nM incubated for 48 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 8.87%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID1635266Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 5 times IC50 after 18 hrs by flow cytometry (Rvb = 17.11 +/- 1.09%)2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID1405370Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID1427230Induction of microtubule disruption in human OVCAR3 cells assessed as nuclear fragmentation at 10 nM after 24 hrs by Alexa Fluor 647/DAPI staining based fluorescence microscopic method2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Combretastatin A4-β-Galactosyl Conjugates for Ovarian Cancer Prodrug Monotherapy.
AID1906224Induction of cell cycle arrest in human HeLa cells assessed as accumulation of cells at G2/M phase at 1.5 nM after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 17.1%)
AID471948Growth inhibition of human KM20L2 cells after 48 hrs by sulforhodamine B assay2009Journal of natural products, Sep, Volume: 72, Issue:9
Antineoplastic agents. 579. Synthesis and cancer cell growth evaluation of E-stilstatin 3: a resveratrol structural modification.
AID1351613Inhibition of tubulin polymerization in human HeLa cells assessed as micronuclei formation at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID265420Cell cycle arrest in NCI-H460 cells by accumulation at G1/0 phase cell at 3 nM post 24 hrs treatment2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID403649Displacement of [3H]colchicine from tubulin2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID1059983Displacement of [3H]-colchicine from tubulin (unknown origin) at 1 uM after 10 mins relative to control2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
AID685175Growth inhibition of human EKVX cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1351631Induction of apoptosis in human MCF7 cells assessed as increase in histone-associated DNA fragments in mononucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID161229In vitro cytotoxic activity against human prostate cancer (DU145) cell line; Not tested2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.
AID1706479Antiproliferative activity against paclitaxel-resistant human A2780 cells assessed as reduction in cell growth after 48 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Development of triazolothiadiazine derivatives as highly potent tubulin polymerization inhibitors: Structure-activity relationship, in vitro and in vivo study.
AID1771456Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 72 hrs by SRB assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID605713Cell cycle arrest in human M21 cells assessed as accumulation at G2/M phase at 5 times IC50 after 24 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 9%)2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID502706Growth inhibition of human CCRF-CEM cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID665824Inhibition of tubulin polymerization in human A549 cells assessed as disrupted microtubule organization at 2 uM after 48 hrs by immunohistochemistry analysis2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID1600465Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1518094Antitumor activity against human MDA-MB-468 cells xenografted in nude mouse assessed as tumour growth inhibition at 60 mg/kg, ip administered every other day for 21 days relative to control2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1647055Induction of apoptosis in human HepG2 cells at 0.1 uM measured after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 4%)2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID261213Cell cycle arrest in NCI/ADR (MDR) cells by accumulation at G2/M phase2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines.
AID1157570Inhibition of Src (unknown origin) assessed as incorporation of [32P] gamma-ATP in to myelin basic protein after 30 mins by autoradiographic analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.
AID1469217Growth inhibition of human A549/CDDP cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1400396Cell cycle arrest in CYP1A1 expressing human MCF7 cells assessed as accumulation at S phase at 0.0010 uM after 24 hrs by flow cytometry (Rvb = 15.1%)2018Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
4-(3-Alkyl-2-oxoimidazolidin-1-yl)-N-phenylbenzenesulfonamides as new antimitotic prodrugs activated by cytochrome P450 1A1 in breast cancer cells.
AID635030Cytotoxicity against human fibroblast cells by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID1460289Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured after 20 mins by Spectrophotometric method2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Bioreductively activatable prodrug conjugates of phenstatin designed to target tumor hypoxia.
AID1875868Inhibition of porcine brain tubulin polymerization at 5 uM measured at 10 mins interval for 100 mins by turbidimetric assay
AID269723Cell cycle arrest in SHSY5Y cells by accumulation at S phase after 8 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID1518068Antiproliferative activity against human T47D cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1174855Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin.
AID1336766Induction of apoptosis in human A549 cells assessed as live cells at 100 nM after 48 hrs by Annexin-V FITC/propidium iodide staining based flow cytometry (Rvb = 94.2%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1906232Induction of apoptosis in human HeLa cells assessed as viable cells at 6 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 75.5%)
AID1324102Cytotoxicity against human HCT116 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID642094Growth inhibition of potorous tridactylus PtK2 cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1288169Cell cycle arrest in human A2780 cells assessed as accumulation at G2/M phase at 3 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 12.71%)2016European journal of medicinal chemistry, May-23, Volume: 114Synthesis and biological evaluation of quinoline analogues of flavones as potential anticancer agents and tubulin polymerization inhibitors.
AID479720Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Synthesis and antitumor activity of 1,5-disubstituted 1,2,4-triazoles as cis-restricted combretastatin analogues.
AID616989Volume of distribution at steady state in Sprague-Dawley rat at 6 umol/kg, iv2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1324101Cytotoxicity against human HCC2998 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID767875Cytotoxicity against human SKOV3 cells by SRB assay2013Journal of natural products, Sep-27, Volume: 76, Issue:9
Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.
AID1462290Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis of different heterocycles-linked chalcone conjugates as cytotoxic agents and tubulin polymerization inhibitors.
AID1057200Cytotoxicity against human HT-29 cells assessed as growth inhibition after 3 days by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity.
AID1068596Growth inhibition of human OVCAR4 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1392078Resistance index, ratio of IC50 for human HeLa cells expressing wild type beta3 tubulin to IC50 for human HeLa cells2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.
AID1824150Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 5 nM measured after 48 hrs by flow cytometric analysis (Rvb = 12.3 + /- 1 %)2022European journal of medicinal chemistry, Feb-05, Volume: 229Branched alkyl of phenyl 4-(2-oxo-3-alkylimidazolidin-1-yl)benzenesulfonates as unique cytochrome P450 1A1-activated antimitotic prodrugs: Biological evaluation and mechanism of bioactivation.
AID674210Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Discovery and optimization of a series of 2-aryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazoles as novel anticancer agents.
AID1873679Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID1882899Resistance index, ratio of IC50 for human MCF7/TxR cells to IC50 for human MCF7 cells2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID310755Antiproliferative activity against human Molt3 cells2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
3-(2'-Bromopropionylamino)-benzamides as novel S-phase arrest agents.
AID695147Antiproliferative activity against human MDA-MB-468 cells expressing NQO1 by MTT assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Novel cyanocombretastatins as potent tubulin polymerisation inhibitors.
AID1865674Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.
AID1693364Relative resistance, ratio of IC50 for antiproliferative activity against human SK-OV-3 MDR-1-6/6 cells expressing Pgp to IC50 antiproliferative activity against human SK-OV-3 cells2021Bioorganic & medicinal chemistry, 01-01, Volume: 29The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
AID1294472Growth inhibition of human HCT116 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1701002Inhibition of cell migration in human HepG2 cells at 10 nM measured after 24 hrs by inverted light microscopy method based wound healing assay relative to control
AID1059050Cell cycle arrest in mouse NIH/3T3 cells assessed as accumulation at G2/M phase at 0.05 uM after 24 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 35.70%)2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis, cytotoxic evaluation and molecular docking study of 2-alkylthio-4-(2,3,4-trimethoxyphenyl)-5-aryl-thiazoles as tubulin polymerization inhibitors.
AID1189933Inhibition of lamb brain tubulin polymerization assessed as reduction in microtubule assembly by spectrophotometry2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Synthesis and biological evaluation of furanoallocolchicinoids.
AID767879Displacement of [3H]colchicine from tubulin (unknown origin) at 1 uM2013Journal of natural products, Sep-27, Volume: 76, Issue:9
Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.
AID1185194Displacement of [3H]colchicine from bovine brain tubulin assessed as rate of assembly at 500 uM after 10 mins by liquid scintillation counting2014European journal of medicinal chemistry, Sep-12, Volume: 84Novel 9'-substituted-noscapines: synthesis with Suzuki cross-coupling, structure elucidation and biological evaluation.
AID1882895Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID665822Inhibition of tubulin polymerization at 3 uM after 1 hr by fluorescence assay2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID1717456Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay
AID1055628Inhibition of calf brain tubulin polymerization after 15 mins by UV-visible spectrophotometry2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis of structurally diverse benzosuberene analogues and their biological evaluation as anti-cancer agents.
AID226442Average growth inhibition against cell lines was calculated2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.
AID1766189Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Design, synthesis and biological evaluation of novel acridine and quinoline derivatives as tubulin polymerization inhibitors with anticancer activities.
AID319826Inhibition of tubulin assembly at 130 uM2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and antitumor activity of benzils related to combretastatin A-4.
AID387311Antiproliferative activity against mouse FM3A cells after 2 days2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.
AID502724Growth inhibition of human SF268 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1565955Metabolic stability in Sprague-Dawley rat liver microsomes assessed as parent compound remaining after 30 mins in presence of NADPH by HPLC-UV-MS analysis
AID1865677Inhibition of pig brain tubulin polymerization by spectrophotometric method2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.
AID1917032Cytotoxicity against human HepG2 cells assessed as cell growth inhibition2022European journal of medicinal chemistry, Nov-05, Volume: 241Recent advances in combretastatin A-4 codrugs for cancer therapy.
AID452433Cell cycle arrest in human K562 cells assessed as accumulation at G2/M phase at 20 nM after 24 hrs by propidium iodide staining-based flow cytometry2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: synthesis and biological evaluation of antivascular activity.
AID746665Cytotoxicity against human AGS cells assessed as growth inhibition after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Design, synthesis, cytotoxic evaluation and tubulin inhibitory activity of 4-aryl-5-(3,4,5-trimethoxyphenyl)-2-alkylthio-1H-imidazole derivatives.
AID761816Inhibition of bovine brain tubulin assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric analysis2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Correlation of hydrogen-bonding propensity and anticancer profile of tetrazole-tethered combretastatin analogues.
AID721879Cytotoxicity against human HCT15 cells assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID1524358Cell cycle arrest in human K562 cells assessed as mitotic index at IC50 by Giemsa staining-based assay (Rvb = 3%)2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents.
AID228453Concentration needed to inhibit tubulin polymerization by 50%2002Journal of medicinal chemistry, Apr-11, Volume: 45, Issue:8
Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation.
AID1068630Growth inhibition of human EKVX cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID202827Cytotoxic concentration required to inhibit 50% cell growth in SKMEL-5 melanoma cell lines1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization.
AID1435073Cell cycle arrest in human HT29-D4 cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID691616Cytotoxicity against human CEM cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID616974Antiproliferative activity against human U87MG after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID685366Growth inhibition of human MCF7 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1411603Toxicity in HEK293 cells assessed as effect on total protein up to 200 uM after 10 mins2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID685209Growth inhibition of human NCI/ADR-RES cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1263245Cytotoxicity against human HL-60(TB) cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1308610Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining at 180 mins in presence of NADPH regenerating system by HPLC method2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1595694Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID1235363Inhibition of bovine brain tubulin polymerization after 30 mins2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes.
AID1600490Effect on RNA synthesis in human CCRF-CEM cells assessed as RNA synthesis level at 5 times IC50 incubated for 24 hrs by propidium iodide staining-based BrdU incorporation assay (Rvb = 47.37%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID383964Cytotoxicity against human MDA-MB-231 cells2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
2-(6-aryl-3(Z)-hexen-1,5-diynyl)anilines as a new class of potent antitubulin agents.
AID1570329Inhibition of porcine tubulin polymerization at 10 uM preincubated at 37 degC for 30 mins followed by chilling to 0 degC and subsequent addition of GTP by microtiter plate based absorbance detection assay relative to control2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.
AID1263258Cytotoxicity against human HCT15 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID622415Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID622614Inhibition of bovine brain tubulin polymerization at 37 degC after 1 hr by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1317595Cytostatic activity against human NHEK cells assessed as cell survival up to 25 uM measured after 72 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID290174Antiproliferative activity against human Bel-7402 cells2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents.
AID1612620Drug resistance index, ratio of IC50 for taxol-resistant human HCT8/T cells to IC50 for human HCT8 cells2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1263260Cytotoxicity against human KM12 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1317629Solubility of compound in water2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID685174Growth inhibition of human A549 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1694124Antiproliferative activity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects.
AID40031Cell growth inhibition against pancreatic BXPC-3 cells, 50% reduction in the net protein increase2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.
AID93841Compound was tested for cell arrest at Go/G1 phase at 25 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID1733023Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition by MTT assay2021Bioorganic & medicinal chemistry letters, 04-15, Volume: 38Synthesis, biological evaluation, and structure-activity relationships of new tubulin polymerization inhibitors based on 5-amino-1,2,4-triazole scaffold.
AID1409120Antiproliferative activity against human SKOV3-MDR1-M6/6 cells after 48 hrs by sulforhodamine B assay2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.
AID657910Antibacterial activity against Micrococcus luteus assessed per disc2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID1717478Cell cycle arrest in human HT-1080 cells assessed as accumulation at S phase at 0.025 uM measured after 12 hrs by propidium iodide staining based flow cytometry (Rvb = 23.09%)
AID1773176Induction of apoptosis in human U-251 cells assessed as increase in early apoptotic cells at 200 nM measured after 24 hrs by PI/FITC analysis (Rvb = 1.12%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1068610Growth inhibition of human SNB75 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID665829Induction of apoptosis in human A549 cells assessed as viable cells at 2 uM after 48 hrs by annexin-V FITC/propidium iodide staining based FACS analysis2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID412969Displacement of [3H]colchicine from tubulin after 2 hrs at 5 uM2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Synthesis and structure-activity relationships of 2-amino-1-aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents.
AID306517Cell cycle arrest in human M21 cells assessed as accumulation at G1 phase at 0.125 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1185459Displacement of [3H]colchicine from long-chain biotin-labeled tubulin (unknown origin) at 5 uM after 2 hrs by competition-binding scintillation proximity assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Concise syntheses of 7-anilino-indoline-N-benzenesulfonamides as antimitotic and vascular disrupting agents.
AID317990Antiproliferative activity against human Molt4/C8 cells2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors.
AID502732Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1408386Cell cycle arrest in human K562 cells assessed as accumulation at G2 phase at 0.01 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 9.51%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID771209Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID146719Cell growth inhibition against NUGC3 human stomach cancer cells using MTS assay2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
AID1469219Resistance factor, ratio of IC50 for human A549/CDDP cells to IC50 for human A549 cells2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1666243Inhibition of pig microtubule polymerization measured every 1 min for 40 mins by spectrophotometric analysis2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID1324090Cytotoxicity against human MOLT4 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1906254Inhibition of colony formation in human HeLa cells at 6 nM and treated for every 48 hrs with fresh medium measured after 14 days by crystal violet staining method
AID1600467Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID546573Cytotoxicity against in CD1 mouse mammary epithelial cells after 72 hrs by alamar blue dye assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Synthesis and evaluation of azetidinone analogues of combretastatin A-4 as tubulin targeting agents.
AID480733Induction of snf1 phosphorylation at T210 in Saccharomyces cerevisiae expressing Snf1-9myc at 450 uM after 3 hrs by Western blot analysis2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID619863Antimitotic activity in human MCF7 cells assessed as mitotic catastrophe at 100 nM after 16 hrs using DAPI staining based immunofluorescence analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID344540Cytotoxicity against human DU145 cells after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4.
AID306514Cell cycle arrest in human M21 cells assessed as accumulation at S phase at 0.050 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1891176Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth by MTT assay
AID1736458Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 2 uM incubated for 2 hrs by scintillation counting method relative to control2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID515463Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
4-(3-Halo/amino-4,5-dimethoxyphenyl)-5-aryloxazoles and -N-methylimidazoles that are cytotoxic against combretastatin A resistant tumor cells and vascular disrupting in a cisplatin resistant germ cell tumor model.
AID1917310Inhibition of pig brain tubulin polymerization at 10 uM by spectrometric method relative to control2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID1058423Cytotoxicity against human BT474 cells assessed as cell viability after 4 days by MTS assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation.
AID1534527Antiproliferative activity against HUVEC after 72 hrs by MTS assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID502744Growth inhibition of human Caki1 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1903082Inhibition of porcine brain tubulin polymerization assessed as inhibition of microtubule polymerization at 5 uM measured at 1 min interval for 90 mins by microplate reader method2022Bioorganic & medicinal chemistry, 03-15, Volume: 58Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors.
AID1612630Inhibition of [3H]-colchicine binding to biotinylated porcine tubulin at 5 uM after 2 hrs by SPA relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1310268Growth inhibition of human EAhy926 cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID317991Antiproliferative activity against human CEM cells2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors.
AID630730Inhibition of human PDE4 expressed in U937 cells using [3H]cAMP as substrate after 30 mins2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
1,1-Diarylalkenes as anticancer agents: dual inhibitors of tubulin polymerization and phosphodiesterase 4.
AID1408371Disruption of microtubule network in human K562 cells at 0.005 to 0.02 uM after 24 hrs by DAPI staining based immunofluorescent microscopic method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1903085Inhibition of tubulin polymerization in human A549 cells assessed as appearance of wrapped microtubule around nucleus at 0.357 uM measured after 24 hrs by immunofluorescence confocal microscopic analysis2022Bioorganic & medicinal chemistry, 03-15, Volume: 58Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors.
AID1466244Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Synthesis and biological evaluation of novel indole-pyrimidine hybrids bearing morpholine and thiomorpholine moieties.
AID348402Antiproliferative activity against mouse FM3A cells2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID1612612Antiproliferative activity against human KB cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1552973Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Synthesis and biological evaluation of 7-methoxy-1-(3,4,5-trimethoxyphenyl)-4,5-dihydro-2H-benzo[e]indazoles as new colchicine site inhibitors.
AID494820Cell cycle arrest in human MCF7 cells assessed as accumulation at G0 phase at 10 uM after 24 hrs by FACS analysis2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
Synthesis and anti-cancer activity of chalcone linked imidazolones.
AID1183658Growth inhibition of human HT-29 cells after 72 hrs by MTT assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID1406433Inhibition of colchicine binding to calf brain tubulin preincubated for 1 hr followed by colchicine addition measured after 1 hr by UPLC-MS/MS analysis2018European journal of medicinal chemistry, Aug-05, Volume: 156Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation.
AID273079Antiproliferative activity against human CEM cells after 72 hrs2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and structure-activity relationships of carbazole sulfonamides as a novel class of antimitotic agents against solid tumors.
AID224778Evaluated for growth inhibition (anticancer activity) of human pancreas-a BXPC-3 cell line.2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID247949Concentration required to inhibit human T-lymphoblast Molt4/C8 cell line proliferation2005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
AID1435102Inhibition of lamb brain tubulin polymerization at compound to tubulin mole ratio of 0.062017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1774983Effect on cell morphology in human MDA-MB-231 cells assessed as microtubule depolymerization at 3 times GI50 measured after 24 hrs by immunostaining based confocal fluorescence microscopic analysis2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Lead Optimization: Synthesis and Biological Evaluation of PBT-1 Derivatives as Novel Antitumor Agents.
AID1411594Cytotoxicity against HEK293FT cells assessed as reduction in cell viability up to 20 uM2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1901289Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay2022European journal of medicinal chemistry, Feb-15, Volume: 230Synthesis and biological evaluation of novel hybrids of phenylsulfonyl furoxan and phenstatin derivatives as potent anti-tumor agents.
AID210312In vitro cytotoxic activity against human TSGH cell line of stomach carcinoma2004Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents.
AID1125804Cytotoxicity against human MKN45 cells after 72 hrs by methylene blue assay2014European journal of medicinal chemistry, Apr-22, Volume: 77Antimitotic and vascular disrupting agents: 2-hydroxy-3,4,5-trimethoxybenzophenones.
AID1334733Antiproliferative activity against human MIAPaCa2 assessed as reduction in cell viability measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility.
AID1162829Binding affinity to tubulin (unknown origin) incubated for 60 mins by colchicine competition assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID1308557Cytotoxicity against human HCT8/VCT cells assessed as growth inhibition after 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1070874Cytotoxicity against human HeLa cells expressing beta3-tubulin containing alanine residue at 227 after 72 hrs by MTS assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
The bat flower: a source of microtubule-destabilizing and -stabilizing compounds with synergistic antiproliferative actions.
AID1731995Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Novel diaryl-2H-azirines: Antitumor hybrids for dual-targeting tubulin and DNA.
AID1162823Induction of cell cycle arrest in human A549 cells assessed as accumulation at S phase at 50 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 4.69%)2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID1351662Inhibition of tubulin polymerization in human HaCaT cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID293340Cell cycle arrest in HMEC1 cells assessed as accumulation at G1 phase at 50 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID1906212Induction of cell cycle arrest in human HeLa cells assessed as 4N cells at 1.5 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 17.1%)
AID502750Growth inhibition of human MCF7 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1572260Inhibition of [3H]-colchicine binding to bovine brain tubulin at 1 to 5 uM after 20 mins relative to control2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.
AID1324127Cytotoxicity against human A498 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID104064Cytotoxicity was determined by inhibition of cell growth of MCF-7 human breast carcinoma cell2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
The synthesis and tubulin binding activity of thiophene-based analogues of combretastatin A-4.
AID442543Inhibition of calf brain tubulin polymerization after 20 mins2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Exploring the effect of 2,3,4-trimethoxy-phenyl moiety as a component of indolephenstatins.
AID1873682Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID1711854Inhibition of porcine brain tubulin polymerization at 3 uM measured after 1 hr in presence of GTP by fluorescence assay relative to control2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID452615Displacement of [3H]colchicine from tubulin2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID1890440Induction of apoptosis in human MDA-MB-231 cells assessed as necrotic cells at 10 uM incubated for 24 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 0.68 %)2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
AID106876Cytotoxic concentration required to inhibit 50% cell growth in MLM melanoma cell lines1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization.
AID502725Growth inhibition of human SF295 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID273081Antiproliferative activity against human Bel7402 cells after 72 hrs2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and structure-activity relationships of carbazole sulfonamides as a novel class of antimitotic agents against solid tumors.
AID1600483Induction of cell cycle arrest in human CCRF-CEM cells assessed as accumulation at G2/M phase at antiproliferative IC50 incubated for 24 hrs by PI staining based flow cytometric analysis (Rvb = 12.12%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1731993Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Novel diaryl-2H-azirines: Antitumor hybrids for dual-targeting tubulin and DNA.
AID306509Cell cycle arrest in human M21 cells assessed as accumulation at G1 phase at 0.015 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1600464Cytotoxicity against human CEM/DNR cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1174241Inhibition of tubulin polymerization (unknown origin) at 5 uM measured every min for 1 hr by fluorescence-based assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Investigation of podophyllotoxin esters as potential anticancer agents: synthesis, biological studies and tubulin inhibition properties.
AID1278683Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 10 mins by scintillation counting analysis2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID437546Anticancer activity against human SMMC7721 cells after 72 hrs2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines).
AID348168Cytotoxicity against human SNU423 cells after 48 hrs by alamar blue assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Design, synthesis and biological evaluation of novel stilbene-based antitumor agents.
AID1657524Cytotoxicity against human NCI-H460 cells after 68 hrs by MTT assay2020Journal of natural products, 05-22, Volume: 83, Issue:5
Synthesis and Cytotoxicity Studies of Stilbene Long-Chain Fatty Acid Conjugates.
AID247585Inhibitory concentration against Human SH-SY5Y neuroblastoma cells2005Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
Synthesis and biological activity of mustard derivatives of combretastatins.
AID1565961Half-life in Sprague-Dawley rat liver microsomes in presence of NADPH by HPLC-UV-MS analysis
AID1832132Induction of apoptosis in human HeLa cells assessed as late apoptotic cells at 5 nM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 1 %)2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID1518081Induction of apoptosis in human MDA-MB-468 cells assessed as necrotic cells at 100 nM after 24 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 0.97 to 1.29%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID93846Compound was tested for cell arrest at sub-G1 phase at 100 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID427178Antiproliferative activity against human CEM cells after 2 days by coulter counter method2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization.
AID1732753Antiproliferative activity against human RL cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-05, Volume: 215Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies.
AID1348624Cytotoxicity against human PBL cells assessed as reduction in cell proliferation after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID301313Induction of tubulin depolymerization after 16 hrs2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Replacement of the lactone moiety on podophyllotoxin and steganacin analogues with a 1,5-disubstituted 1,2,3-triazole via ruthenium-catalyzed click chemistry.
AID1709301Cytotoxicity against human HeLa cells over expressing WT-beta3 assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1709303Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1689057Metabolic stability in human liver microsomes assessed as UGT-mediated N-glucuronidation by measuring intrinsic clearance at 3 uM measured up to 45 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells.
AID214184Percentage inhibition of colchicine binding to tubulin by compound was evaluated1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
AID685201Growth inhibition of human SK-MEL-5 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1263288Cytotoxicity against human MDA-MB-468 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1308541Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1408387Cell cycle arrest in human K562 cells assessed as accumulation at G1 phase at 0.02 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 41.08%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1422794Antiproliferative activity against human H22 cells after 72 hrs by MTT assay
AID1534523Antiproliferative activity against human A549 cells after 72 hrs by MTS assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID1693353Induction of microtubule depolymerisation in rat A-10 cell line measured after 18 hrs by indirect immunofluorescence method2021Bioorganic & medicinal chemistry, 01-01, Volume: 29The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
AID243597Inhibition of [3H]colchicine binding to 1 uM beta-tubulin at 2 uM2005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
AID1068592Growth inhibition of human 786-0 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1586365Cell cycle arrest in human A549 cells assessed as accumulation at subG0 phase at 0.2 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 2 +/- 0.8%)2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4.
AID299206Antiproliferative activity against human DU145 cells2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity relationships.
AID691617Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1717463Inhibition of tubulin polymerization in human HT-1080 cells assessed as reduction of interphase microtubule network wrapped around the cell nucleus at 0.032 uM measured after 48 hrs by DAPI/immunofluorescence staining based fluorescence microscopic analys
AID281505Growth inhibition of human MCF7 cells assessed as G2/M DNA content after 48 hrs2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Arylthioindoles, potent inhibitors of tubulin polymerization.
AID502742Growth inhibition of human 786-0 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID658263Inhibition of sheep brain tubulin polymerization using DAPI by fluorescence assay2012European journal of medicinal chemistry, Jun, Volume: 52Conformationnally restricted naphthalene derivatives type isocombretastatin A-4 and isoerianin analogues: synthesis, cytotoxicity and antitubulin activity.
AID613262Antiproliferative activity against human H460 cells after 72 hrs by methylene blue assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and biological evaluation of 1-(4'-Indolyl and 6'-Quinolinyl) indoles as a new class of potent anticancer agents.
AID1285330Induction of apoptosis in human HT-29 cells assessed as reduction in mitochondrial membrane potential at 10 nM after 48 hrs by JC-1 staining based flow cytometry (Rvb = 94.3%)2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID1324089Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1183668Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 5 uM2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID1254255Inhibition of tubulin (unknown origin) polymerization after 1 hr by ELISA plate reader analysis2015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Triazole linked mono carbonyl curcumin-isatin bifunctional hybrids as novel anti tubulin agents: Design, synthesis, biological evaluation and molecular modeling studies.
AID1689133Cytotoxicity against human HDfa cells assessed as inhibition of cell growth after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.
AID376521Cytotoxicity against human FaDu cells2000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID290176Antiproliferative activity against human DU145 cells2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents.
AID636399Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Design, synthesis, biological evaluation and molecular modeling of 1,3,4-oxadiazoline analogs of combretastatin-A4 as novel antitubulin agents.
AID1294477Growth inhibition of human U251 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1351627Induction of apoptosis in human A431 cells after 24 hrs by FITC Annexin V/propidium iodide staining-based FACScan flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID663558Antiproliferative activity against human CA46 cells2012ACS medicinal chemistry letters, Jan-12, Volume: 3, Issue:1
Steroidomimetic Tetrahydroisoquinolines for the Design of New Microtubule Disruptors.
AID214723Percent inhibition of colchicine(5 uM) binding to tubulin(10 uM) at the compound concentration of 50 uM)2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.
AID248447Concentration required for the 50% inhibition of human stomach cancer (NUGC3) cell line growth2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.
AID1612621Antiproliferative activity against human taxol-resistant A549/TR cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1057124Inhibition of porcine brain tubulin polymerization by turbidity assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID1717457Antiproliferative activity against human HT-1080 cells measured after 72 hrs by MTT assay
AID1338084Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of cyclic-indole derivatives as anti-tumor agents via the inhibition of tubulin polymerization.
AID622610Inhibition of bovine brain tubulin polymerization preincubation at 37 degC, cooled followed by addition of GTP and acquisition at 37 degC by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID769828Inhibition of beta3 tubulin overexpressed in human HeLa cells after 48 hrs by SRB assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.
AID306508Induction of apoptosis in human M21 cells at 0.015 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1310184Growth inhibition of combretastatin A-4 resistant human HT-29 cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1458816Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID644555Antivascular activity against HUVEC cells assessed as cell growth inhibition measured every 30 mins for 21 hrs by xCELLigence assay2012Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5
Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A-1.
AID642054Antiproliferative activity against human HeLa cells assessed as growth inhibition after 48 hrs by MTT assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1851617Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells at G2 phase at 10 uM (Rvb = 16.5 %)2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives.
AID1263265Cytotoxicity against human SNB19 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1534528Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID1174857Inhibition of tubulin (unknown origin) polymerization after 1 hr by multiplate reader method2015European journal of medicinal chemistry, Jan-07, Volume: 89Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin.
AID1628252Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 50 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 35%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID1420996Antiproliferative activity against human HT-29 cells after 72 hrs by XTT assay
AID1593627Selectivity index, ratio of IC50 for human MCF10A cells to IC50 for human MDA-MB-468 cells expressing CYP1A1 and CYP1B12019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells.
AID452619Antiproliferative activity against mouse L1210 cells after 5 days by MTT assay2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID1068639Antimitotic activity in sea urchin fertilized egg assessed as cleavage arrest treated at 8 to 20 mins post-fertilization measured at 2.5 to 5.5 hrs post-fertilization2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID657882Growth inhibition of human DU145 cells after 48 hrs by sulforhodamine B assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID771215Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID1185191Inhibition of bovine brain tubulin assessed as extent of assembly preincubated for 15 mins by turbidimetry2014European journal of medicinal chemistry, Sep-12, Volume: 84Novel 9'-substituted-noscapines: synthesis with Suzuki cross-coupling, structure elucidation and biological evaluation.
AID685177Growth inhibition of human HOP92 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1348625Cytotoxicity against human PBL cells assessed as reduction in cell viability after 72 hrs by MTS assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID1600476Therapeutic index, ratio of IC50 for human MCR5 cells to IC50 for human CCRF-CEM cells2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1706480Antiproliferative activity against cisplatin resistant human A549 cells assessed as reduction in cell growth after 48 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Development of triazolothiadiazine derivatives as highly potent tubulin polymerization inhibitors: Structure-activity relationship, in vitro and in vivo study.
AID1637530Induction of inner mitochondrial membrane potential depolarization in isolated mitochondria from human HeLa cells at 40 to 60 nM after 48 hrs by JC-1 staining based fluorescence plate reader assay2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID637149Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3
Synthesis, biological evaluation, and molecular docking studies of cinnamic acyl 1,3,4-thiadiazole amide derivatives as novel antitubulin agents.
AID1737839Metabolic stability in human liver microsomes assessed as parent compound remaining at 10 uM measured after 20 mins in presence of NADPH by LC/MS/MS analysis2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID1729880Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by XTT assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Methylsulfanylpyridine based diheteroaryl isocombretastatin analogs as potent anti-proliferative agents.
AID214160The compound was tested for the concentration to inhibit 50% of tubulin polymerization.1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
AID1399381Inhibition of [3H]colchicine binding to bovine brain tubulin at 1 uM measured after 10 mins relative to control2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and preclinical evaluation of 5-methyl-N
AID605712Cell cycle arrest in human M21 cells assessed as accumulation at S phase at 5 times IC50 after 24 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 30%)2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID1431177Growth inhibition of human HeLa cells measured after 96 hrs by sulforhodamine B assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
AID685172Growth inhibition of human RPMI8226 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1351632Induction of apoptosis in human MDA-MB-231 cells assessed as increase in histone-associated DNA fragments in mononucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1673998Inhibition of porcine tubulin polymerization by UV/visible spectrophotometry2020Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives.
AID1165180Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Design and synthesis of pironetin analogue/combretastatin A-4 hybrids containing a 1,2,3-triazole ring and evaluation of their cytotoxic activity.
AID607287Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID685372Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 4 uM after 24 hrs by FACS analysis (Rvb = 58.33%)2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1174856Cytotoxicity against human HeLa cells after 72 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin.
AID1760489Antiproliferative activity against human Calu-1 cells incubated for 24 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020).
AID1862610Antiproliferative activity against imatinib-resistant human K562 cells over expressing MDR1 after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID780971Displacement of [3H]-colchicine from biotin-labeled tubulin (unknown origin) at 5 uM after 2 hrs by scintillation proximity assay relative to control2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Furanylazaindoles: potent anticancer agents in vitro and in vivo.
AID213846Antitubulin activity against tubulin polymerization1999Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
Synthesis and biological evaluation of dihydrobenzofuran lignans and related compounds as potential antitumor agents that inhibit tubulin polymerization.
AID674213Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Discovery and optimization of a series of 2-aryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazoles as novel anticancer agents.
AID247232Growth inhibition against human prostate cell line (DU-145)2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID622612Inhibition of pig brain tubulin polymerization at 37 degC by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1517355Antiproliferative activity against human A549 cells incubated for 48 hrs by MTS assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Design and synthesis of (2-(phenylamino)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone analogues as potent anti-tubulin polymerization agents.
AID1064412Growth inhibition of human KM12 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1689095Induction of apoptosis in human HeLa cells assessed as necrotic cells at 0.5 uM measured after 24 hrs by Annexin-V-FITC and PI staining based flow cytometry (Rvb = 0.956%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1771459Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by SRB assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1773152Cell cycle arrest in human U-251 cells assessed as G2/M phase at 200 nM measured after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 14.43%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID317732Cytotoxicity against human HIV1RF infected CEM-SS cells by MTT assay2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID1773142Cell cycle arrest in human A549 cells assessed as G0/G1 phase at 500 nM incubated for 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 79.14%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID685365Growth inhibition of human DU145 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1851616Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells at G1 phase at 10 uM (Rvb = 61.33 %)2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives.
AID745607Inhibition of tubulin polymerization (unknown origin) at 3 uM after 20 mins by fluorescence plate reader analysis2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Site-specific and far-red-light-activatable prodrug of combretastatin A-4 using photo-unclick chemistry.
AID1187061Antiproliferative activity against human A549 cells after 24 to 48 hrs by CKK8 assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Discovery and molecular modeling of novel 1-indolyl acetate--5-nitroimidazole targeting tubulin polymerization as antiproliferative agents.
AID403052Displacement of [3H]colchicine from bovine tubulin at 2 uM2005Journal of natural products, Aug, Volume: 68, Issue:8
Antineoplastic agents. 515. Synthesis of human cancer cell growth inhibitors derived from 3,4-methylenedioxy-5,4'-dimethoxy-3'-amino-Z-stilbene.
AID306483Growth inhibition of human MDA-MB-231 cells2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1200598Toxicity in human HT-29 cells xenografted BALB/c mouse assessed as change in body weight at 50 mg/kg, ip administered once daily for 18 days (Rvb = 2.5 g)2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Quantum chemistry calculation-aided structural optimization of combretastatin A-4-like tubulin polymerization inhibitors: improved stability and biological activity.
AID1730567Antiproliferative activity against human M21 cells assessed as reduction in cell viability measured after 48 hrs by sulforhodamine B assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID627394Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID1408394Induction of apoptosis in human K562 cells at 0.005 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.46%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1508156Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 2 uM after 24 hrs by flow cytometric analysis (Rvb = 79.1%)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID723247Cytotoxicity against human SW480 cells after 48 hrs by MTT assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Design and synthesis of cyclopropylamide analogues of combretastatin-A4 as novel microtubule-stabilizing agents.
AID1064430Growth inhibition of human K562 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID502739Growth inhibition of human OVCAR8 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1125810Displacement of [3H]colchicine from tubulin (unknown origin) at 1 uM after 2 hrs by scintillation counting analysis2014European journal of medicinal chemistry, Apr-22, Volume: 77Antimitotic and vascular disrupting agents: 2-hydroxy-3,4,5-trimethoxybenzophenones.
AID1901291Antiproliferative activity against human HCT-116 cells after 48 hrs by MTT assay2022European journal of medicinal chemistry, Feb-15, Volume: 230Synthesis and biological evaluation of novel hybrids of phenylsulfonyl furoxan and phenstatin derivatives as potent anti-tumor agents.
AID1336767Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 100 nM after 48 hrs by Annexin-V FITC/propidium iodide staining based flow cytometry (Rvb = 5.2%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1882897Cytotoxicity against human MCF7/TxR cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID492260Antiproliferative activity against human CEM cells after 2 days by coulter counting2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Substituted 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]thiophene derivatives as potent tubulin polymerization inhibitors.
AID261211Inhibition of tubulin polymerization2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines.
AID1694899Cytotoxicity against mouse B16 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2020RSC medicinal chemistry, Mar-01, Volume: 11, Issue:3
Application of triazoles as bioisosteres and linkers in the development of microtubule targeting agents.
AID1906271Cytotoxicity against HK-2 cells assessed as reduction in cell growth measured after 24 hrs by microplate reader analysis
AID442547Cytotoxicity against human HT-29 cells after 72 hrs by XTT assay2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Exploring the effect of 2,3,4-trimethoxy-phenyl moiety as a component of indolephenstatins.
AID1854156Cytotoxicity against human A549 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Cascade synthetic strategies opening access to medicinal-relevant aliphatic 3- and 4-membered N-heterocyclic scaffolds.
AID1421770Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Conformation impacts on the bioactivities of SMART analogues.
AID451277Inhibition of bovine tubulin polymerization by fluorescent plate reader analysis2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Synthesis and biological evaluation of 3,4-diaryl-5-aminoisoxazole derivatives.
AID1400400Disruption of microtubule dynamics in CYP1A1 expressing human MCF7 cells at 0.0010 uM after 24 hrs by immunofluorescence method2018Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
4-(3-Alkyl-2-oxoimidazolidin-1-yl)-N-phenylbenzenesulfonamides as new antimitotic prodrugs activated by cytochrome P450 1A1 in breast cancer cells.
AID1424792Growth inhibition of human OVCAR8 cells after 96 hrs by trypan blue exclusion assay2018European journal of medicinal chemistry, May-25, Volume: 152New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors.
AID1324112Cytotoxicity against human M14 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1327867Cell cycle arrest in human A549 cells assessed as accumulation in G2/M phase at 0.018 uM by propidium iodide-staining based FACS analysis
AID1157572Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 10 mins2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.
AID691657Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as effect on platelet count at 50 mg/kg, ip qd after 21 days (Rvb = 1509 +/- 34 x 10'3 mm'-3)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID502713Growth inhibition of human HOP62 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID765487Competitive inhibition of [3H]colchicine binding to tubulin (unknown origin) at 1 uM after 10 mins by radioligand displacement assay2013European journal of medicinal chemistry, Sep, Volume: 67N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines: a novel class of antitumor agents targeting the colchicine site on tubulin.
AID1562379Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin.
AID1392072Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM measured after 10 mins by scintillation counting method relative to control2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.
AID1411597Inhibition of human OAT3 expressed in HEK293 cells assessed as 6-CF uptake after 5 mins by fluorescence assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1689082Inhibition of cell migration in human HeLa cells at 0.5 uM measured after 24 hrs by wound healing assay (Rvb = 61%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1324108Cytotoxicity against human SF295 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1873731Induction of apoptosis in human HeLa cells assessed as necrotic cells at 10 nM incubated for 48 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 1.85 %)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID1408364Antiproliferative activity against human K562 cells at 1 uM after 72 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1600489Effect on RNA synthesis in human CCRF-CEM cells assessed as RNA synthesis level at IC50 incubated for 24 hrs by propidium iodide staining-based BrdU incorporation assay (Rvb = 47.37%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1595691Antiproliferative activity against human HCT8 cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID276459Cytotoxicity against NCI60 cell line2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
Novel imidazole-based combretastatin A-4 analogues: evaluation of their in vitro antitumor activity and molecular modeling study of their binding to the colchicine site of tubulin.
AID1779199Inhibition of [3H]Colchicine binding to tubulin (unknown origin) at 1 uM measured after 10 mins by DEAE-Cellulose filter method relative to control2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia.
AID723248Cytotoxicity against human HeLa cells after 48 hrs by MTT assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Design and synthesis of cyclopropylamide analogues of combretastatin-A4 as novel microtubule-stabilizing agents.
AID1851429Induction of apoptosis in human K562 cells assessed as late apoptotic cells at 10 uM by AnnexinV-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 5.1%)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Synthesis and antitumor activity of a series of novel N-aryl-5-(2,2,2-trifluoroethoxy)-1,5-dihydro-2H-pyrrol-2-ones derivatives.
AID1647003Induction of apoptosis in human HepG2 cells assessed as late apoptotic cells at 0.1 uM measured after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.155 %)2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1906206Induction of cell cycle arrest in human HeLa cells assessed as S-phase at 1.5 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 23.4%)
AID249469Therapeutic index (IC90/percentage of CFUGEMM inhibition) value after 14 days for bone marrow cells treated with compound at IC902005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Heterocyclic and phenyl double-bond-locked combretastatin analogues possessing potent apoptosis-inducing activity in HL60 and in MDR cell lines.
AID1732759Induction of cell cycle arrest in human RL cells assessed as increase in accumulation in subG0/G1 phase at 1 nM incubated for 48 hrs by PI staining based flow cytometry analysis (Rvb = 8 %)2021European journal of medicinal chemistry, Apr-05, Volume: 215Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies.
AID1234873Cytotoxicity against human HL60 cells assessed as inhibition of cell proliferation after 72 hrs by XTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Exploring the size adaptability of the B ring binding zone of the colchicine site of tubulin with para-nitrogen substituted isocombretastatins.
AID607282Antiproliferative activity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID778974Displacement of [3H]colchicine from tubulin (unknown origin) at 1 uM after 10 mins by scintillation counting analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and biological evaluation of indole-based, anti-cancer agents inspired by the vascular disrupting agent 2-(3'-hydroxy-4'-methoxyphenyl)-3-(3″,4″,5″-trimethoxybenzoyl)-6-methoxyindole (OXi8006).
AID1647046Toxicity in immunocompetent BALB/c nude mouse xenografted with human A549 cells assessed as effect on kidney damage or inflammation at 30 mg/kg, iv administered once daily for 29 consecutive days measured after 29 days by hematoxylin-eosin staining based 2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1458819Antiproliferative activity against human RKO cells after 48 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1724512Antiproliferative activity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay2020Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19
A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors.
AID314006Antiproliferative activity against human SR cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID1057128Inhibition of porcine brain tubulin polymerization at 30 uM by turbidity assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID1324132Cytotoxicity against human 786-0 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1310192Cell cycle arrest in combretastatin A-4 resistant human HT-29 cells assessed as mitotic cells at 5 uM after 24 hrs by propidium iodide/immunostaining method (Rvb = 3.1 to 3.2%)2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1191397Cytotoxicity against human K562 cells after 72 hrs by CellTitre-Blue assay2015European journal of medicinal chemistry, Jan-27, Volume: 90Rapid synthesis of 4-arylchromenes from ortho-substituted alkynols: A versatile access to restricted isocombretastatin A-4 analogues as antitumor agents.
AID1411592Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability up to 20 uM after 24 hrs by MTT assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1535612Antitumor activity against rat hepatoma H22 cells implanted in mouse assessed as reduction in tumor volume at 3 mg/kg, ip measured after 8 to 28 days2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Synthesis, biological evaluation and molecular docking of benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives as novel tubulin polymerization inhibitors.
AID349340Cytotoxicity against human HT-29 cells after 72 hrs by XTT assay2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Naphthylphenstatins as tubulin ligands: synthesis and biological evaluation.
AID1773165Induction of apoptosis in human A549 cells assessed as increase in late apoptotic cells at 500 nM measured after 24 hrs by PI/FITC analysis (Rvb = 0.955%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID42826Inhibition of bovine brain microtubule polymerization2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
AID1348617Antiproliferative activity against human HCT116 cells after 72 hrs by resazurin-based fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID349339Cytotoxicity against human A549 cells after 72 hrs by XTT assay2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Naphthylphenstatins as tubulin ligands: synthesis and biological evaluation.
AID502723Growth inhibition of human SW620 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID552580Induction of cell cycle arrest in human KB cells assessed as accumulation at subG1 phase at 20 nM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 1.2%)2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis of antiproliferative flavones from calycopterin, major flavonoid of Calycopteris floribunda Lamk.
AID1508155Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 2 uM after 24 hrs by flow cytometric analysis (Rvb = 2.35%)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1647000Cell cycle arrest in human HepG2 cells assessed as accumulation at S phase at 0.1 uM measured after 24 hrs by RNase A/propidium iodide staining based flow cytometry (Rvb = 23.04 %)2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1774979Antiproliferative activity against human KB-VIN cells assessed as cell growth inhibition measured after 72 hrs by SRB assay2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Lead Optimization: Synthesis and Biological Evaluation of PBT-1 Derivatives as Novel Antitumor Agents.
AID746666Cytotoxicity against mouse NIH/3T3 cells assessed as growth inhibition after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Design, synthesis, cytotoxic evaluation and tubulin inhibitory activity of 4-aryl-5-(3,4,5-trimethoxyphenyl)-2-alkylthio-1H-imidazole derivatives.
AID626626Cell cycle arrest in human M21 cells assessed as accumulation at G2/M phase at 5 times IC50 after 24 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 9%)2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID502737Growth inhibition of human OVCAR-3 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID397290Cytotoxicity against human K562 cells after 72 hrs2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Isocombretastatins a versus combretastatins a: the forgotten isoCA-4 isomer as a highly promising cytotoxic and antitubulin agent.
AID1865670Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.
AID403647Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID1736454Antiproliferative activity against drug resistant human K562 cells incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1324088Cytotoxicity against human HL-60(TB) cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID727482Inhibition of tubulin (unknown origin) assessed as inhibition of GTP-induced polymerization incubated for 45 mins prior to GTP-addition measured after 2 hrs by DAPI-staining based fluorimetric analysis2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
Synthesis and biological evaluation of enantiomerically pure cyclopropyl analogues of combretastatin A4.
AID502734Growth inhibition of human SK-MEL-5 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1730574Cell cycle arrest in human M21 cells assessed as accumulation at G0/G1 phase at 11 nM measured after 24 hrs by DAPI staining based flow cytometry (Rvb = 65.5%)2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID241105Concentration required for 50% inhibition of tubulin polymerization2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Quantitative structure-activity relationship (5D-QSAR) study of combretastatin-like analogues as inhibitors of tubulin assembly.
AID287911Growth inhibition of MCF7 cells after 48 hrs2007Bioorganic & medicinal chemistry, May-01, Volume: 15, Issue:9
The concise synthesis of chalcone, indanone and indenone analogues of combretastatin A4.
AID1608958Antiproliferative activity against human HL60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.
AID607286Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID265415Antiproliferative activity against human A2780 cells2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID471949Growth inhibition of human DU145 cells after 48 hrs by sulforhodamine B assay2009Journal of natural products, Sep, Volume: 72, Issue:9
Antineoplastic agents. 579. Synthesis and cancer cell growth evaluation of E-stilstatin 3: a resveratrol structural modification.
AID1666251Induction of cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 0.6 uM incubated for 48 hrs by PI staining based flow cytometric analysis (Rvb = 68.26%)2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID1387439Cytotoxicity against human MCF7 cells after 72 hrs by MTS/PMS assay2018Journal of natural products, 09-28, Volume: 81, Issue:9
Synthesis and in Vitro Bioactivity of Polyunsaturated Fatty Acid Conjugates of Combretastatin A-4.
AID514405Displacement [3H]colchicine from tubulin at 5 uM2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents.
AID1612611Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID757690Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Synthesis and antitumor activity of novel 3,4-diaryl squaric acid analogs.
AID142305Evaluated for growth inhibition (anticancer activity) of Murine P388 lymphocytic leukemia cell line2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID248425Concentration required for the 50% inhibition of human breast cancer (MCF-7) cell line growth2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.
AID403054Displacement of [3H]vinblastine from bovine tubulin at 10 uM2005Journal of natural products, Aug, Volume: 68, Issue:8
Antineoplastic agents. 515. Synthesis of human cancer cell growth inhibitors derived from 3,4-methylenedioxy-5,4'-dimethoxy-3'-amino-Z-stilbene.
AID1709300Cytotoxicity against human HeLa cells assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID84127Cytotoxic concentration required to inhibit 50% cell growth in HT-29 colon adenocarcinoma cell lines1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization.
AID1400379Antiproliferative activity against human HaCaT cells after 72 hrs by SRB assay2018Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
4-(3-Alkyl-2-oxoimidazolidin-1-yl)-N-phenylbenzenesulfonamides as new antimitotic prodrugs activated by cytochrome P450 1A1 in breast cancer cells.
AID1586076Displacement of [3H]-colchicine from bovine brain tubulin at 5 uM by scintillation proximity assay relative to control2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1324123Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID247567Concentration required to inhibit tubulin polymerization at 10 uM2005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
AID479721Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetry2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Synthesis and antitumor activity of 1,5-disubstituted 1,2,4-triazoles as cis-restricted combretastatin analogues.
AID1338590Cytotoxicity against human HCT116 cells assessed as growth inhibition after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of novel alkylsulfanyl-1,2,4-triazoles as cis-restricted combretastatin A-4 analogues.
AID388080Inhibition of lamb brain microtubule assembly assessed as mole ratio of total drug per mole of tubulin by DAPI fluorimetry2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Synthesis and biological evaluation of polymethoxylated 4-heteroarylcoumarins as tubulin assembly inhibitor.
AID1411601Inhibition of human OCT2 expressed in HEK293 cells assessed as Asp+ uptake after 10 mins by fluorescence assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID767877Displacement of [3H]colchicine from tubulin (unknown origin) at 50 uM2013Journal of natural products, Sep-27, Volume: 76, Issue:9
Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.
AID737004Displacement of [3H]colchicine from tubulin (unknown origin) at 1 uM after 10 mins2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Identification of diaryl 5-amino-1,2,4-oxadiazoles as tubulin inhibitors: the special case of 3-(2-fluorophenyl)-5-(4-methoxyphenyl)amino-1,2,4-oxadiazole.
AID1694126Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects.
AID1517169Inhibition of porcine brain tubulin polymerization assessed as decrease in fluorescence intensity measured every 60 sec for 90 mins in presence of GTP by DAPI staining based fluorescence assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Potent combretastatin A-4 analogs containing 1,2,4-triazole: Synthesis, antiproliferative, anti-tubulin activity, and docking study.
AID1403596Inhibition of alpha-tubulin polymerization in human HeLa cells assessed as increase in ratio of supernatant faction to pellet fraction at 500 nM after 6 hrs by Western blot analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
AID1541867Antiproliferative activity against human KBVIN cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
AID269721Cell cycle arrest in SHSY5Y cells by accumulation at G2 phase after 24 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID1774976Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Lead Optimization: Synthesis and Biological Evaluation of PBT-1 Derivatives as Novel Antitumor Agents.
AID1666241Antiproliferative activity against human U251 cells incubated for 48 hrs by MTT assay2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID461782Antiproliferative activity against human KB cells after 72 hrs by methylene blue dye assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors.
AID1125805Cytotoxicity against human HT-29 cells after 72 hrs by methylene blue assay2014European journal of medicinal chemistry, Apr-22, Volume: 77Antimitotic and vascular disrupting agents: 2-hydroxy-3,4,5-trimethoxybenzophenones.
AID1628409Inhibition of porcine brain tubulin polymerization incubated for 60 mins by fluorescence-based assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Design, Synthesis, and Biological Evaluation of 1-Methyl-1,4-dihydroindeno[1,2-c]pyrazole Analogues as Potential Anticancer Agents Targeting Tubulin Colchicine Binding Site.
AID769747Displacement of [3H]-colchicine from pig brain tubulin at 5 uM after 10 mins by scintillation counting analysis relative to control2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.
AID717163Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
AID1348628Increase in PGF2alpha-induced contractile response in isolated Wistar rat aorta rings at 10 uM after 10 mins (Rvb = 115.4 +/- 5.1%)2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID1294620Cytotoxicity against human HT-29 cells assessed as reduction in cell growth after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, biological evaluation and molecular docking studies of 2-amino-3,4,5-trimethoxyaroylindole derivatives as novel anticancer agents.
AID1917038Cytotoxicity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Recent advances in combretastatin A-4 codrugs for cancer therapy.
AID1195292Antiproliferative activity against human HeLa cells overexpressing wild type beta3 tubulin after 48 hrs by sulforhodamine B assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID1351616Inhibition of tubulin polymerization in human A431 cells assessed as micronuclei formation at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1593628Antiproliferative activity against ER negative human MDA-MB-468 cells expressing CYP1A1 and CYP1B1 assessed as reduction in cell viability measured after 96 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells.
AID1165181Cytotoxicity against HEK293 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Design and synthesis of pironetin analogue/combretastatin A-4 hybrids containing a 1,2,3-triazole ring and evaluation of their cytotoxic activity.
AID1310267Growth inhibition of human MCF7/Topo cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1706474Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth after 48 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Development of triazolothiadiazine derivatives as highly potent tubulin polymerization inhibitors: Structure-activity relationship, in vitro and in vivo study.
AID612421Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT based ELISA assay2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Synthesis, biological evaluation, and molecular modeling of cinnamic acyl sulfonamide derivatives as novel antitubulin agents.
AID1400397Cell cycle arrest in CYP1A1 expressing human MCF7 cells assessed as accumulation at G2/M phase at 0.0010 uM after 24 hrs by flow cytometry (Rvb = 13%)2018Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
4-(3-Alkyl-2-oxoimidazolidin-1-yl)-N-phenylbenzenesulfonamides as new antimitotic prodrugs activated by cytochrome P450 1A1 in breast cancer cells.
AID1862616Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID691623Inhibition of porcine brain tubulin assembly measured every 1 min for 60 mins by turbidimetric analysis2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1906261Antiproliferative activity against human HeLa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
AID1274782Binding affinity to beta-Tubulin in human MCF7 cells assessed as inhibition of protein-EBI adduct formation at Cys239 and Cys354 at 10 uM pre-incubated for 2 hrs followed by EBI addition after 1.5 hrs by Western blot analysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Synthesis and Biochemical Evaluation of 3-Phenoxy-1,4-diarylazetidin-2-ones as Tubulin-Targeting Antitumor Agents.
AID349337Inhibition of calf brain tubulin polymerization relative to control2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Naphthylphenstatins as tubulin ligands: synthesis and biological evaluation.
AID1882911Induction of microtubule disruption in human HT-29 cells at 50 nM measured after 6 hrs by immunofluorescence assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1903084Inhibition of tubulin polymerization in human A549 cells assessed as appearance of short microtubule at 0.357 uM measured after 24 hrs by immunofluorescence confocal microscopic analysis2022Bioorganic & medicinal chemistry, 03-15, Volume: 58Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors.
AID1435067Solubility of the compound in PBS at pH 7.4 after 2 hrs2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1376366Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM after 10 mins by scintillation counting method relative to control
AID1887834Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR.
AID52669Growth inhibition of colon 26 adenocarcinoma cells by 50 %.1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel combretastatin analogues effective against murine solid tumors: design and structure-activity relationships.
AID1711857Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells at 50 nM measured after 48 hrs by annexinV-FITC/propidium iodide staining based flow cytometry (Rvb = 4.4 %)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID1736447Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1057118Chemical stability of the compound in PBS at pH 7.4 assessed as compound remaining after 24 hrs by HPLC analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID1628255Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 50 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 16%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID306512Induction of apoptosis in human M21 cells at 0.050 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1367975Antiproliferative activity against human MDA-MB-231 cells by MTT assay
AID1399382Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM measured after 10 mins relative to control2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and preclinical evaluation of 5-methyl-N
AID379684Inhibition of Saccharomyces cerevisiae RS322 expressing Rad52.erg6 by agar diffusion assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID442974Growth inhibition of human NCI60 cells after 3 days by crystal violet staining2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Vascular disrupting activity of tubulin-binding 1,5-diaryl-1H-imidazoles.
AID549150Inhibition of tubulin polymerization at 40 uM after 20 mins by turbidimetry2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-aryl/arylaminobenzo[b]thiophene derivatives as a novel class of antiproliferative agents.
AID461022Antiproliferative activity against human MCF7 cells after 24 hrs by SRB assay2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
A boronic acid chalcone analog of combretastatin A-4 as a potent anti-proliferation agent.
AID455030Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID769832Antiproliferative activity against human SKOV3 cells after 48 hrs by SRB assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.
AID1917313Cytotoxicity against human NCM460 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID659047Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G0/G1 phase at 3 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 43.9 %)2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
AID1263247Cytotoxicity against human MOLT4 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1068587Growth inhibition of human TK10 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1524340Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM after 20 mins relative to control2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents.
AID536405Inhibition of bovine brain tubulin assembly by spectrophotometric analysis2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.
AID1351656Inhibition of tubulin polymerization in human HaCaT cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1757289Inhibition of pig brain tubulin polymerisation incubated for 30 mins and measured every 2 mins for 60 mins by spectrophotometric method2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID594374Displacement [3H]colchicine from tubulin at 5 uM after 10 mins2011Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
Synthesis of novel antimitotic agents based on 2-amino-3-aroyl-5-(hetero)arylethynyl thiophene derivatives.
AID1731557Inhibition of tubulin (unknown origin) polymerization incubated for 90 mins by fluorescence-based assay2021European journal of medicinal chemistry, Mar-15, Volume: 214A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents.
AID1459302Induction of reactive oxygen species generation in human MCF7 cells assessed as decrease in cell viability at 100 nM in presence of N-acetyl cysteine after 48 hrs by alamarBlue assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1595693Antiproliferative activity against human H22 cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID607531Inhibition of tubulin alpha in human SH-SY5Y cells assessed as inhibition of tubulin alpha polymerization at 3 times IC50 value after 24 hrs by immunofluorescence2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues.
AID1310243Cytotoxicity against human EAhy926 cells assessed as cell viability at 100 nM after 16 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID202141Compound was evaluated against Human cell line melanoma SK-MEL-51999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID716409Antiproliferative activity against human HaCaT cells assessed as cell viability by MTT assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4.
AID1595695Inhibition of tubulin polymerization (unknown origin) in presence of GTP measured after 60 mins by spectrophotometric method2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID1741566Cytotoxicity against HEK293 cells measured after 48 hrs by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Synthesis, and biological evaluation of 3,6-diaryl-[1,2,4]triazolo[4,3-a]pyridine analogues as new potent tubulin polymerization inhibitors.
AID286489Displacement of [3H]colchicine from bovine brain tubulin at 1 uM2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID730196Antiangiogenic activity in human A549 cells xenografted in BALB/c nu/nu mouse assessed as disruption of tumor vasculature at 100 mg/kg, ip after 16 hrs by Hoechst 33342 staining-based Zeiss microscopic analysis relative to control2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Synthesis and structure-activity relationships of N-methyl-5,6,7-trimethoxylindoles as novel antimitotic and vascular disrupting agents.
AID1237706Inhibition of tubulin (unknown origin) assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric analysis2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID1695606Inhibition of tubulin polymerization in human BT-474 cells assessed as microtubule disruption at 2 uM by immunohistochemistry assay
AID1600494Inhibition of tubulin polymerization in human HCT116 cells assessed as disruption of mitotic spindle at antiproliferative IC50 incubated for 24 hrs by DAPI staining based spinning disk confocal microscopic method2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1731564Inhibition of bovine brain tubulin polymerization incubated for 15 mins followed by GTP addition and measured after 20 mins by spectrophotometric method2021European journal of medicinal chemistry, Mar-15, Volume: 214A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents.
AID685360Growth inhibition of human RXF393 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1689074Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 0.5 uM measured after 24 hrs by Annexin-V-FITC and PI staining based flow cytometry (Rvb = 2.58%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1690540Antiproliferative activity against human Bel-7402 cells measured after 48 hrs by SRB assay2020European journal of medicinal chemistry, Apr-01, Volume: 191Synthesis and structure-activity relationship study of water-soluble carbazole sulfonamide derivatives as new anticancer agents.
AID1195295Antiproliferative activity against human SKOV3-MDR1-M6/6 cells overexpressing wild type beta3 tubulin after 48 hrs by sulforhodamine B assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID52664Cytotoxic activity was determined against Colon 26 adenocarcinoma cells1998Bioorganic & medicinal chemistry letters, Dec-01, Volume: 8, Issue:23
Novel B-ring modified combretastatin analogues: syntheses and antineoplastic activity.
AID1351590Cytotoxicity against human HeLa cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1535578Cytotoxicity against HEK293T cells after 24 hrs by MTT assay2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Synthesis, biological evaluation and molecular docking of benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives as novel tubulin polymerization inhibitors.
AID1851430Induction of apoptosis in human K562 cells assessed as dead cells at 10 uM by AnnexinV-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 5.94%)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Synthesis and antitumor activity of a series of novel N-aryl-5-(2,2,2-trifluoroethoxy)-1,5-dihydro-2H-pyrrol-2-ones derivatives.
AID1070870Resistance ratio of IC50 for human SKOV3 cells expressing MDR1 to IC50 for human SKOV3 cells2013Journal of natural products, Oct-25, Volume: 76, Issue:10
The bat flower: a source of microtubule-destabilizing and -stabilizing compounds with synergistic antiproliferative actions.
AID1336768Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 100 nM after 48 hrs by Annexin-V FITC/propidium iodide staining based flow cytometry (Rvb = 0.6%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID727483Antivascular activity against human EAhy926 cells assessed as rounding up morphology after 2 hrs by microscopic analysis2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
Synthesis and biological evaluation of enantiomerically pure cyclopropyl analogues of combretastatin A4.
AID1237725Cytotoxicity against human MESSA cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID1854154Cytotoxicity against human HCT-116 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Cascade synthetic strategies opening access to medicinal-relevant aliphatic 3- and 4-membered N-heterocyclic scaffolds.
AID1351652Inhibition of tubulin polymerization in human A431 cells assessed as micronuclei formation at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1779197Inhibition of [3H]Colchicine binding to tubulin (unknown origin) at 5 uM measured after 10 mins by DEAE-Cellulose filter method relative to control2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia.
AID1165182Selectivity index, ratio of IC50 for HEK293 cells to IC50 for human HT-29 cells2014European journal of medicinal chemistry, Nov-24, Volume: 87Design and synthesis of pironetin analogue/combretastatin A-4 hybrids containing a 1,2,3-triazole ring and evaluation of their cytotoxic activity.
AID1338081Antiproliferative activity against human Bel7402 cells measured after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of cyclic-indole derivatives as anti-tumor agents via the inhibition of tubulin polymerization.
AID1628258Inhibition of goat brain tubulin assembly incubated for 10 mins by spectrophotometry2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID1304313Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell proliferation after 3 days by 3H-thymidine incorporation assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synthesis and biological activity of pyrrole analogues of combretastatin A-4.
AID1891190Inhibition of tubulin polymerization (unknown origin) at 10 uM measured every minute for 20 mins by fluorescence based assay relative to control
AID480729Induction of G1 phase arrest in Saccharomyces cerevisiae expressing TAP-tagged Cln2 assessed as down-regulation of Cln2 level at 450 uM after 3 hrs by Western blot analysis2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID1237724Cytotoxicity against Pgp overexpressing human NCI-ADR-RES cells assessed as growth inhibition after 48 hrs by SRB assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID1886181Inhibition of HDAC in human HeLa cells using BOC-K(Ac)-AMC as substrate at 10 uM measured after 30 mins by fluorescence based microtiter plate reader assay relative to control2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1263277Cytotoxicity against human OVCAR4 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1741569Antiproliferative activity against human T47D cells measured after 48 hrs by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Synthesis, and biological evaluation of 3,6-diaryl-[1,2,4]triazolo[4,3-a]pyridine analogues as new potent tubulin polymerization inhibitors.
AID611186Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 2 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 60.5%)2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Synthesis and biological evaluation of 4β-acrylamidopodophyllotoxin congeners as DNA damaging agents.
AID1819035Induction of microtubule depolymerization in human MDA-MB-231 cells assessed as spindle formation incubated for 24 hrs by immunofluorescence staining based confocal microscopic analysis2022Journal of natural products, 01-28, Volume: 85, Issue:1
Chemical Space Expansion of Flavonoids: Induction of Mitotic Inhibition by Replacing Ring B with a 10π-Electron System, Benzo[
AID421983Cytotoxicity against mouse P388 cells2009Journal of natural products, May-22, Volume: 72, Issue:5
Antineoplastic agents. 565. Synthesis of combretastatin D-2 phosphate and dihydro-combretastatin D-2.
AID449227Growth inhibition of Potorous tridactylus PtK2 cells2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
AID643531Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Synthesis and evaluation of 1,5-disubstituted tetrazoles as rigid analogues of combretastatin A-4 with potent antiproliferative and antitumor activity.
AID685371Growth inhibition of human MDA-MB-468 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID248446Concentration required for the 50% inhibition of human stomach cancer (MKN45) cell line growth2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.
AID721875Cytotoxicity against human MESSA cells assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID723249Cytotoxicity against human A549 cells after 48 hrs by MTT assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Design and synthesis of cyclopropylamide analogues of combretastatin-A4 as novel microtubule-stabilizing agents.
AID1324118Cytotoxicity against human MALME-3M cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1517172Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Potent combretastatin A-4 analogs containing 1,2,4-triazole: Synthesis, antiproliferative, anti-tubulin activity, and docking study.
AID1402687Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by SRB assay
AID1757887Inhibition of tubulin assembly (unknown origin)2021Bioorganic & medicinal chemistry letters, 06-01, Volume: 41Novel pyrazolo[4,3-d]pyrimidine microtubule targeting agents (MTAs): Synthesis, structure-activity relationship, in vitro and in vivo evaluation as antitumor agents.
AID1294484Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1637519Cell cycle arrest in human HeLa cells assessed as accumulation at G0 phase at 60 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 5.64%)2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID695146Antiproliferative activity against human K562 cells by MTT assay2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Novel cyanocombretastatins as potent tubulin polymerisation inhibitors.
AID665816Cell cycle arrest in human A549 cells assessed as cell accumulation at G0/G1 phase at 2 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 70.15%)2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID1426065Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM relative to control2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, structure-activity relationships and biological evaluation of 7-phenyl-pyrroloquinolinone 3-amide derivatives as potent antimitotic agents.
AID1431176Cytotoxicity against human A431 cells2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
AID317734Inhibition of tubulin polymerization after 20 mins2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID1185207Cell cycle arrest in human CA46 cells assessed as reduction in mitotic index by Giemsa staining method relative to control2014European journal of medicinal chemistry, Sep-12, Volume: 84Novel 9'-substituted-noscapines: synthesis with Suzuki cross-coupling, structure elucidation and biological evaluation.
AID1608956Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.
AID1059055Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis, cytotoxic evaluation and molecular docking study of 2-alkylthio-4-(2,3,4-trimethoxyphenyl)-5-aryl-thiazoles as tubulin polymerization inhibitors.
AID548392Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 72 hrs by MTT assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Lead identification of conformationally restricted β-lactam type combretastatin analogues: synthesis, antiproliferative activity and tubulin targeting effects.
AID1628398Growth inhibition of human HepG2 cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Design, Synthesis, and Biological Evaluation of 1-Methyl-1,4-dihydroindeno[1,2-c]pyrazole Analogues as Potential Anticancer Agents Targeting Tubulin Colchicine Binding Site.
AID1906195Induction of cell cycle arrest in human HeLa cells assessed as < 2N cells at 3 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 9.32%)
AID146553Compound was evaluated against Human cell line lung-NSC NCI-H4601999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID1666240Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID1863086Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway.
AID1324103Cytotoxicity against human HCT15 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1694122Antiproliferative activity against human HCT-116 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects.
AID617004Cell cycle arrest in human MDA-MB-435 cells assessed as accumulation of cells at G2/M phase at 3 times IC50 after 18 hrs by flow cytometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID1698444Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Ultrasound assisted synthesis of tetrazole based pyrazolines and isoxazolines as potent anticancer agents via inhibition of tubulin polymerization.
AID1518082Induction of apoptosis in human MDA-MB-468 cells assessed as viable cells at 100 nM after 48 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 96.8%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1317617Induction of apoptosis in human HepG2 cells assessed as early apoptotic cells at 0.11 uM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID265406Antiproliferative activity against bovine BMEC2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID271660Inhibition of [3H]colchicine binding to tubulin at 5 uM2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents.
AID1294467Growth inhibition of human SR cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1196877Cell cycle arrest in human SH-SY5Y cells assessed as accumulation at S phase at 3 times IC50 after 16 hrs by flow cytometry (Rvb = 10.6 %)2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID1875874Cell cycle arrest in human 5182A cells assessed as increase in accumulation at G2/M phase at 25 nM measured after 6 to 24 hrs by propidium iodide staining based FACS analysis
AID1231329Anticancer activity against human Jurkat E6-1 cells assessed as reduction in cell proliferation after 48 hrs by WST-1 assay2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4.
AID611188Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 2 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 26.42%)2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Synthesis and biological evaluation of 4β-acrylamidopodophyllotoxin congeners as DNA damaging agents.
AID1518069Antiproliferative activity against human HCT15 cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1765567Inhibition of bovine brain tubulin assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by turbidimetry-based spectrophotometric method2021European journal of medicinal chemistry, Oct-15, Volume: 222Effects of substituent pattern on the intracellular target of antiproliferative benzo[b]thiophenyl chromone derivatives.
AID1064385Growth inhibition of human ACHN cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID307424Cytotoxicity against human HeLa cells2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Synthesis and biological activity of naphthalene analogues of phenstatins: naphthylphenstatins.
AID451273Cytotoxicity against human ECA109 cells after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Synthesis and biological evaluation of 3,4-diaryl-5-aminoisoxazole derivatives.
AID1666242Inhibition of pig microtubule polymerization at 10 uM measured every 1 min for 40 mins by spectrophotometric analysis relative to control2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID1240945Inhibition of tubulin (unknown origin) assembly pre-incubated for 15 mins before GTP addition measured after 20 mins by turbidimetry2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines as tubulin polymerization inhibitors.
AID1183727Induction of apoptosis in human HeLa cells assessed as failure of MT elongation at 20 nM by immunofluorescence analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID461786Antiproliferative activity against P-gp170/MDR expressing human KBVIN cells after 72 hrs by methylene blue dye assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors.
AID1324105Cytotoxicity against human KM12 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1689130Induction of microtubule cytoskeleton disruption in human EA.hy926 cells at 50 nM assessed as nuclear breakdown and blebbing measured after 24 hrs by DAPI staining based fluorescence microscopic analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.
AID1070872Cytotoxicity against human SKOV3 cells after 72 hrs by MTS assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
The bat flower: a source of microtubule-destabilizing and -stabilizing compounds with synergistic antiproliferative actions.
AID1287983Displacement of [3H]-colchicine from porcine tubulin at 20 uM preincubated for 1 hr followed by radioligand addition measured after 30 mins by DE81 filter-based scintillation spectrometric assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Discovery of novel 2-phenyl-imidazo[1,2-a]pyridine analogues targeting tubulin polymerization as antiproliferative agents.
AID1595688Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID548394Cytotoxicity against human MCF7 cells expressing estrogen receptor assessed as LDH release at 10 uM2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Lead identification of conformationally restricted β-lactam type combretastatin analogues: synthesis, antiproliferative activity and tubulin targeting effects.
AID1728938Induction of apoptosis in human MDA-MB-231 cells assessed as necrotic cells at 1 uM measured after 24 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.74%)2021European journal of medicinal chemistry, Mar-05, Volume: 213Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.
AID1741599Induction of microtubule disruption in human HeLa cells at 12 nM measured after 6 hrs by DAPI staining based immunofluorescence microscopy2020European journal of medicinal chemistry, Oct-15, Volume: 204Synthesis, and biological evaluation of 3,6-diaryl-[1,2,4]triazolo[4,3-a]pyridine analogues as new potent tubulin polymerization inhibitors.
AID450674Cytotoxicity against human A549 cells after 72 hrs by XTT assay2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Isocombretastatins A: 1,1-diarylethenes as potent inhibitors of tubulin polymerization and cytotoxic compounds.
AID1647047Toxicity in immunocompetent BALB/c nude mouse xenografted with human A549 cells assessed as effect on spleen damage or inflammation at 30 mg/kg, iv administered once daily for 29 consecutive days measured after 29 days by hematoxylin-eosin staining based 2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1196880Metabolic stability in human liver microsomes assessed as peak area after 60 mins by LC-UV analysis in presence of NADPH2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID1411595Cytotoxicity against HEK293FT cells expressing GLUT1 assessed as reduction in cell viability up to 20 uM2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1068628Growth inhibition of human HOP92 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1310198Cell cycle arrest in combretastatin A-4 resistant human HT-29 cells assessed as accumulation at S phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 13.7 +/- 0.3%)2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1324104Cytotoxicity against human HT-29 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1068629Growth inhibition of human A549/ATCC cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1183657Growth inhibition of human HeLa cells after 72 hrs by MTT assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID256882Displacement of [3H]colchicine from tubulin2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors.
AID685190Growth inhibition of human SF295 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID214331Percentage inhibition of [3H]-colchicine binding at 5 uM1993Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic
AID1608957Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.
AID1324136Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1535575Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured after 20 mins by turbidimetric method2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Synthesis, biological evaluation and molecular docking of benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives as novel tubulin polymerization inhibitors.
AID1698447Inhibition of tubulin polymerization in human A549 cells assessed as decrease in polymerized fraction of tubulin content after 48 hrs by western blot analysis2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Ultrasound assisted synthesis of tetrazole based pyrazolines and isoxazolines as potent anticancer agents via inhibition of tubulin polymerization.
AID685192Growth inhibition of human SNB19 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1338591Inhibition of porcine brain tubulin polymerization at 10 uM in presence of GTP by spectrophotometric method relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of novel alkylsulfanyl-1,2,4-triazoles as cis-restricted combretastatin A-4 analogues.
AID1534521Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID1731559Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability after 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents.
AID1860221Antiproliferative activity against human L02 cells measured after 48 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-functional antitumor conjugates improving the anti-metastasis effect of combretastatin A4 by targeting tubulin polymerization and matrix metalloproteinases.
AID1651882Cytotoxicity against human A549 cells incubated for 52 hrs in oxic condition by sulforhodamine B assay2020Journal of natural products, 04-24, Volume: 83, Issue:4
Bioreductively Activatable Prodrug Conjugates of Combretastatin A-1 and Combretastatin A-4 as Anticancer Agents Targeted toward Tumor-Associated Hypoxia.
AID644542Cell cycle arrest in human SKOV3 cells assessed as accumulation at G1 phase at 5 nM by flow cytometry (Rvb = 54%)2012Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5
Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A-1.
AID1126007Cell cycle arrest in human HeLa cells assessed as accumulation at S phase at 1 uM after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 22.10%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1771467Inhibition of HDAC (unknown origin)2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID305458Cytotoxicity against human HeLa cells2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and cytotoxic activities of 4,5-diarylisoxazoles.
AID662342Antiproliferative activity in human HeLa cells assessed as cell viability at 10 uM after 48 hrs by MTT assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID1189966Reduction in blood-brain barrier permeability in C57BL/6 mouse endothelial cells2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Synthesis and biological evaluation of furanoallocolchicinoids.
AID1541870Inhibition of tubulin polymerization in human MDA-MB-231 cells at 3 times of antiproliferative IC50 incubated for 24 hrs by DAPI staining based confocal fluorescence microscopy
AID1694128Inhibition of pig brain tubulin polymerization by spectrophotometric method2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects.
AID281349Cytotoxicity against human PA1 cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID348166Cytotoxicity against human MDA-MB-231 cells after 48 hrs by alamar blue assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Design, synthesis and biological evaluation of novel stilbene-based antitumor agents.
AID538692Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
Synthesis, molecular modeling and biological evaluation of guanidine derivatives as novel antitubulin agents.
AID305462Cell cycle arrest in human HepG2 cells assessed as accumulation at S phase at 10 uM after 24 hrs relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and cytotoxic activities of 4,5-diarylisoxazoles.
AID502721Growth inhibition of human HT-29 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1732755Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-05, Volume: 215Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies.
AID502746Growth inhibition of human TK10 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1059049Cell cycle arrest in mouse NIH/3T3 cells assessed as accumulation at S phase at 0.05 uM after 24 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 24.39%)2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis, cytotoxic evaluation and molecular docking study of 2-alkylthio-4-(2,3,4-trimethoxyphenyl)-5-aryl-thiazoles as tubulin polymerization inhibitors.
AID1550336Antiproliferative activity against human KB cells measured after 72 hrs by MTT assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and bioevaluation of diarylpyrazoles as antiproliferative agents.
AID1191392Cytotoxicity against human HCT116 cells after 72 hrs by CellTitre-Blue assay2015European journal of medicinal chemistry, Jan-27, Volume: 90Rapid synthesis of 4-arylchromenes from ortho-substituted alkynols: A versatile access to restricted isocombretastatin A-4 analogues as antitumor agents.
AID1508150Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by MTT assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1906202Induction of cell cycle arrest in human HeLa cells assessed as 2N cells at 6 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 41.7%)
AID277280Cytotoxicity against HeLa cell line2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Highly potent triazole-based tubulin polymerization inhibitors.
AID437549Anticancer activity against human HCT116 cells after 72 hrs2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines).
AID1157571Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetry analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.
AID1811592Antiproliferative activity against human HT-1080 cells assessed as inhibition of cell proliferation measured after 48 hrs by SRB assay2021Bioorganic & medicinal chemistry, 12-15, Volume: 52Synthetic development of sugar amino acid oligomers towards novel podophyllotoxin analogues.
AID771207Cytotoxicity against human MX1 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID1728929Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G2 phase at 1 uM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 5.77%)2021European journal of medicinal chemistry, Mar-05, Volume: 213Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.
AID1463418Inhibition of porcine brain tubulin polymerization at 3 uM incubated for 80 mins by fluorescence based spectrophotometry2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Constructing novel dihydrofuran and dihydroisoxazole analogues of isocombretastatin-4 as tubulin polymerization inhibitors through [3+2] reactions.
AID1694125Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects.
AID737110Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID1064399Growth inhibition of human SK-MEL-2 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1518085Induction of apoptosis in human MDA-MB-468 cells assessed as necrotic cells at 100 nM after 48 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 0.97 to 1.29%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID248448Concentration required for the 50% inhibition of human uterine cancer (MESSA) cell line growth2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.
AID1411600Inhibition of human OCT1 expressed in HEK293 cells assessed as Asp+ uptake after 10 mins by fluorescence assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1059993Cytotoxicity against mouse L1210 cells assessed as growth inhibition after 48 hrs by coulter counting analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
AID1064424Growth inhibition of human EKVX cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID548640Inhibition of bovine tubulin polymerization at 10 uM measured every 30 seconds for 60 mins by spectrophotometry relative to control2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Lead identification of conformationally restricted β-lactam type combretastatin analogues: synthesis, antiproliferative activity and tubulin targeting effects.
AID1565958Metabolic stability in Sprague-Dawley rat liver microsomes assessed as parent compound remaining after 120 mins in presence of NADPH by HPLC-UV-MS analysis
AID1402065Antiproliferative activity against human CEM cells after 3 days by Coulter counter method2018European journal of medicinal chemistry, Jan-01, Volume: 1432-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.
AID1863109Inhibition of porcine brain microtubule polymerization measured after 1 hrs by fluorescence based assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway.
AID1628410Displacement of [3H]colchicine from biotinylated porcine tubulin at 1 uM incubated for 2 hrs by competition scintillation proximity2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Design, Synthesis, and Biological Evaluation of 1-Methyl-1,4-dihydroindeno[1,2-c]pyrazole Analogues as Potential Anticancer Agents Targeting Tubulin Colchicine Binding Site.
AID1729300Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
AID1757886Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 0.5 uM relative to control2021Bioorganic & medicinal chemistry letters, 06-01, Volume: 41Novel pyrazolo[4,3-d]pyrimidine microtubule targeting agents (MTAs): Synthesis, structure-activity relationship, in vitro and in vivo evaluation as antitumor agents.
AID1405401Inhibition of bovine MAP-rich tubulin polymerization at 10 uM measured every 1 min for 30 mins relative to control2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID1541869Cell cycle arrest in human MDA-MB-231 cells assessed as increase in accumulation of G2/M phase at 3 times of antiproliferative IC50 incubated for 24 hrs by propidium iodide based flow cytometry
AID1176808Cytotoxicity against human SGC7901 cells assessed as cell growth inhibition after 72 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Microwave-assisted synthesis and biological evaluation of 3,4-diaryl maleic anhydride/N-substituted maleimide derivatives as combretastatin A-4 analogues.
AID1194524Displacement of [3H]colchicine from tubulin (unknown origin) at 5 uM2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Novel hybrid nocodazole analogues as tubulin polymerization inhibitors and their antiproliferative activity.
AID627392Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID306482Growth inhibition of human MCF7 cells2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1466260Inhibition of pig brain tubulin polymerization by spectrophotometric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 134Synthesis and biological evaluation of novel indole-pyrimidine hybrids bearing morpholine and thiomorpholine moieties.
AID1126015Antiangiogenic activity in chicken embryo chorioallantoic membrane model assessed as inhibition of bFGF/VEGF-induced new vessel growth2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1324124Cytotoxicity against human NCI-ADR-RES cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1757273Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1263271Cytotoxicity against human SK-MEL-2 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1458853Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining after 90 mins in presence of NADPH by UV-based HPLC-MS/MS analysis2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1348621Antiproliferative activity against human MCF7 cells after 72 hrs by resazurin-based fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID293345Cell cycle arrest in HMEC1 cells assessed as accumulation at G2/M phase at 50 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID474636Cell cycle arrest in human HeLa cells assessed as accumulation of cells in S phase at 0.2 uM after 24 hrs using propidium iodide by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1327135Antiproliferative activity against human KB cells measured after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 1224,5-Diaryl-3H-1,2-dithiole-3-thiones and related compounds as combretastatin A-4/oltipraz hybrids: Synthesis, molecular modelling and evaluation as antiproliferative agents and inhibitors of tubulin.
AID314023Antiproliferative activity against human TD-47D cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID444154Antiproliferative activity against rat A10 cells assessed as microtubule depolymerization after 18 to 24 hrs by indirect immunofluorescence technique2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID52656In vitro cytotoxic activity tested against human colon cancer (SW620) cell line2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.
AID1338080Antiproliferative activity against human PC3 cells measured after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of cyclic-indole derivatives as anti-tumor agents via the inhibition of tubulin polymerization.
AID1906225Induction of cell cycle arrest in human HeLa cells assessed as accumulation of cells at G2/M phase at 3 nM after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 17.1%)
AID214167Inhibition of radiolabeled Colchicine binding to tubulin at 37 degrees C (1.0 mM MgCl2)1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions.
AID1906270Octanol-water partition coefficient, logP of the compound incubated overnight by HPLC analysis
AID281352Inhibition of tubulin polymerization in bovine brain2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1353642Inhibition of calf brain tubulin polymerization after 60 mins by turbidimetric method2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID1693354Antiproliferative activity against human MDA-MB-435 cell line assessed as inhibition of cell proliferation measured after 48 hrs by SRB assay2021Bioorganic & medicinal chemistry, 01-01, Volume: 29The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
AID1811594Antiproliferative activity against human HaCaT cells assessed as inhibition of cell proliferation measured after 48 hrs by SRB assay2021Bioorganic & medicinal chemistry, 12-15, Volume: 52Synthetic development of sugar amino acid oligomers towards novel podophyllotoxin analogues.
AID455039Cytotoxicity against human OVCAR-3 cells after 48 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID1411608Substrate activity at human OAT3 expressed in HEK293 cells assessed as compound uptake by HPLC-UV method2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1158427Inhibition of [3H]colchicine binding to pig brain tubulin at 1 uM2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
AID1860218Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-functional antitumor conjugates improving the anti-metastasis effect of combretastatin A4 by targeting tubulin polymerization and matrix metalloproteinases.
AID619867Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 100 nM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 8.77+/-0.9%)2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID1162837Induction of apoptosis in human A549 cells assessed as caspase-3 activation at 50 nM incubated for 48 hrs by ELISA method2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID622531Inhibition of bovine brain tubulin polymerization incubated for 15 mins at 30 degC, cooled followed by 20 mins acquisition at 30 degC by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID94321Inhibitory concentration against vincristine-resistant cell line (KB-Vin 10) using tetrazolium dye reduction assay (MTT)2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID1733022Antiproliferative activity against human HeLa cells assessed as cell growth inhibition by MTT assay2021Bioorganic & medicinal chemistry letters, 04-15, Volume: 38Synthesis, biological evaluation, and structure-activity relationships of new tubulin polymerization inhibitors based on 5-amino-1,2,4-triazole scaffold.
AID492261Antiproliferative activity against human HeLa cells after 2 days by coulter counting2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Substituted 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]thiophene derivatives as potent tubulin polymerization inhibitors.
AID1324113Cytotoxicity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID779082Selectivity index, ratio of IC50 for HUVEC to IC50 for human MCF7 cells2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
The synthesis and anticancer activity of analogs of the indole phytoalexins brassinin, 1-methoxyspirobrassinol methyl ether and cyclobrassinin.
AID717162Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
AID1518611Inhibition of porcine brain tubulin polymerization at 1.25 uM by fluorescence assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.
AID281356AUC in iv dosed Swiss Albino mouse plasma2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID241079Inhibition of tubulin polymerization upon incubation for 20 min at 30 degree C2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID348403Antiproliferative activity against human Molt4/C8 cells2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID1263250Cytotoxicity against human A549 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1600482Induction of cell cycle arrest in human CCRF-CEM cells assessed as accumulation at S phase at 5 times antiproliferative IC50 incubated for 24 hrs by PI staining based flow cytometric analysis (Rvb = 46%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID662362Induction of AMPK-mediated p53 pser15 accumulation in human HuTu 18 cells at 30 nM after 24 hrs by Western blot analysis2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID737114Cytotoxicity against human HL60 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID494826Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 30 uM after 24 hrs by FACS analysis2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
Synthesis and anti-cancer activity of chalcone linked imidazolones.
AID502718Growth inhibition of human HCC2998 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1251950Inhibition of bovine brain tubulin polymerization assessed as protein assembly after 20 mins by turbidimetric analysis2015Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
Novel 3-Substituted 7-Phenylpyrrolo[3,2-f]quinolin-9(6H)-ones as Single Entities with Multitarget Antiproliferative Activity.
AID314013Antiproliferative activity against human LOX IMVI cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID626625Cell cycle arrest in human M21 cells assessed as accumulation at S phase at 5 times IC50 after 24 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 30%)2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID442540Inhibition of calf brain tubulin polymerization at 20 uM after 20 mins2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Exploring the effect of 2,3,4-trimethoxy-phenyl moiety as a component of indolephenstatins.
AID1486473Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis, biological evaluation and molecular modeling of imidazo[1,2-a]pyridine derivatives as potent antitubulin agents.
AID1733033Inhibition of tubulin (unknown origin) polymerization measured every 1 min over 20 mins by fluorescence assay2021Bioorganic & medicinal chemistry letters, 04-15, Volume: 38Synthesis, biological evaluation, and structure-activity relationships of new tubulin polymerization inhibitors based on 5-amino-1,2,4-triazole scaffold.
AID437551Cell cycle arrest in human HepG2 cells assessed as increase in G2/M phase cells after 20 hrs by flow cytometry using propidium iodide staining2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines).
AID761818Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Correlation of hydrogen-bonding propensity and anticancer profile of tetrazole-tethered combretastatin analogues.
AID1906174Antiproliferation activity against human HeLa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
AID619865Cell cycle arrest in human MCF7 cells assessed as accumulation at sub-G1 phase at 100 nM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 1.65+/-0.38%)2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID642061Growth inhibition of human OVCAR8 cells overexpressing P-glycoprotein after 96 hrs2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1731566Displacement of [3H]colchicine from bovine brain tubulin at 0.5 uM by DEAE-cellulose filter method relative to control2021European journal of medicinal chemistry, Mar-15, Volume: 214A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents.
AID1832146Metabolic stability in human liver microsomes assessed as parent compound remaining after 60 mins2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID1336779Induction of ROS generation in human A549 cells at 100 nM after 48 hrs by DCFDA staining based flow cytometry (Rvb = 4.4%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID510856Cytotoxicity against human HCT116 cells after 72 hrs2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Regioselective hydrostannation of diarylalkynes directed by a labile ortho bromine atom: an easy access to stereodefined triarylolefins, hybrids of combretastatin A-4 and isocombretastatin A-4.
AID1183718Cytotoxicity against human MESSA/DX5 cells assessed as growth inhibition after 72 hrs by CellTitre-Glo assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID1882983Induction of apoptosis in human MDA-MB-231 cells assessed as apoptotic cells at 10 uM incubated for 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometric method (Rvb = 5.68%)2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and evaluation of a novel series of mono-indolylbenzoquinones derivatives for the potential treatment of breast cancer.
AID587608Inhibition of tubulin assembly after 20 mins by turbidimetric assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Antitumor agents. 284. New desmosdumotin B analogues with bicyclic B-ring as cytotoxic and antitubulin agents.
AID1730573Cell cycle arrest in human M21 cells assessed as accumulation at SubG1 phase at 11 nM measured after 24 hrs by DAPI staining based flow cytometry (Rvb = 5%)2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID552581Induction of cell cycle arrest in human KB cells assessed as accumulation at G0/G1phase at 20 nM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 66.6%)2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis of antiproliferative flavones from calycopterin, major flavonoid of Calycopteris floribunda Lamk.
AID1628237Antiproliferative activity against human HeLa cells incubated for 24 hrs by sulforhodamine B assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID1276122Cytotoxicity against human SF188 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1240946Displacement of [3H]-colchicine from tubulin (unknown origin) at 5 uM after 10 mins2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines as tubulin polymerization inhibitors.
AID1263262Cytotoxicity against human SF268 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID685380Inhibition of ERK1/2 protein expression in human MCF7 cells at 4 uM after 24 hrs by Western blot analysis2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1666253Induction of cell cycle arrest in human A549 cells assessed as accumulation at S phase at 0.6 uM incubated for 48 hrs by PI staining based flow cytometric analysis (Rvb = 14.71%)2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID1367982Inhibition of pig brain tubulin polymerization measured every 1 min for 20 mins by spectrophotometric analysis
AID90853Cell growth inhibition against Hone-1 human NPC cancer cells using MTS assay2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
AID751506Displacement of [3H]-colchicine from bovine brain tubulin at 5 uM after 10 mins relative to control2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.
AID1064387Growth inhibition of human 786-0 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1126643Inhibition of sheep brain tubulin assembly by DAPI-staining based fluorescence assay2014European journal of medicinal chemistry, May-06, Volume: 78Discovery of azaisoerianin derivatives as potential antitumors agents.
AID1409119Antiproliferative activity against human SKOV3 cells after 48 hrs by sulforhodamine B assay2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.
AID1730568Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by sulforhodamine B assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID607535Metabolic stability in human liver microsomes assessed as phase 1 transformation after 60 mins by LC-ESI-MS and LC-UV analysis in presence of NADP(H)-regenerating system2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues.
AID1057192Inhibition of c-myc mRNA expression in human HT-29 cells after 48 hrs by RT-PCR analysis relative to control2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity.
AID1709298Induction of microtubule depolymerization in rat A10 cells incubated for over night by immunofluorescence method2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID643532Inhibition of bovine tubulin polymerisation after 20 mins by turbidimetric analysis2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Synthesis and evaluation of 1,5-disubstituted tetrazoles as rigid analogues of combretastatin A-4 with potent antiproliferative and antitumor activity.
AID273364Antiproliferative activity against human TSGH stomach carcinoma cell line by methylene blue dye assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
AID1585985Cytotoxicity against human BT549 cells after 72 hrs by MTT assay
AID1235364Displacement of 1 uM of [3H]colchicine from biotin-labeled tubulin (unknown origin) after 2 hrs by scintillation proximity assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes.
AID1486478Inhibition of tubulin polymerization in human HT-29 cells assessed as abnormal microtubule network formation at 20 nM after 24 hrs by DAPI staining based immunofluorescence microscopic analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis, biological evaluation and molecular modeling of imidazo[1,2-a]pyridine derivatives as potent antitubulin agents.
AID449228Selectivity index, ratio of IC50 for Potorous tridactylus PtK2 cells to IC50 for human MCF7 cells2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
AID1738833Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM relative to control2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors.
AID761833Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 10 mins by scintillation counting analysis relative to control2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity.
AID1324094Cytotoxicity against human EKVX cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1873709Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 10 nM incubated for 24 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 0.12%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID669461Growth inhibition of human A549 cells after 48 hrs by SRB assay2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID1651875Inhibition of bovine brain tubulin polymerisation preincubated for 15 mins followed by GTP addition and measured for 20 mins by turbidimetry based spectrophotometric method2020Journal of natural products, 04-24, Volume: 83, Issue:4
Bioreductively Activatable Prodrug Conjugates of Combretastatin A-1 and Combretastatin A-4 as Anticancer Agents Targeted toward Tumor-Associated Hypoxia.
AID450675Cytotoxicity against human HeLa cells after 72 hrs by XTT assay2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Isocombretastatins A: 1,1-diarylethenes as potent inhibitors of tubulin polymerization and cytotoxic compounds.
AID1406451Antitumor activity against human HeLa cells xenografted in nude mouse assessed as necrosis of tumor cells at 10 mg/kg, ip after 14 days by hematoxylin and eosin staining based microscopic analysis2018European journal of medicinal chemistry, Aug-05, Volume: 156Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation.
AID1570343Cytotoxicity against human HuH7 cells assessed as induction of mitosis after 24 hrs2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.
AID1235366Antivascular activity in HUVEC assessed as inhibition of VEGF-induced capillary tube formation at 20 nM after 4 hrs by microscopic analysis relative to control2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes.
AID657575Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Design, synthesis and biological evaluation of novel chalcone derivatives as antitubulin agents.
AID1403605Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M-phase at 50 nM after 24 hrs by propidium iodide staining based flow cytometry2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
AID1865673Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.
AID1431179Growth inhibition of human OVCAR8 cells measured after 96 hrs by sulforhodamine B assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
AID214021Inhibition of tubulin polymerization with preincubation for 15 minutes at 37 degree Centigrade prior to addition of the GTP required for polymerization1993Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic
AID474624Cytotoxicity against human HeLa cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID479718Antiproliferative activity against human Jurkat cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Synthesis and antitumor activity of 1,5-disubstituted 1,2,4-triazoles as cis-restricted combretastatin analogues.
AID619859Antiproliferative activity against ER-independent human MDA-MB-231 cells assessed as cell death at 10 uM after 72 hrs by MTT assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID1068621Growth inhibition of human COLO205 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1352478Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation.
AID348169Cytotoxicity against human UCI101 cells after 48 hrs by alamar blue assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Design, synthesis and biological evaluation of novel stilbene-based antitumor agents.
AID1733021Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by MTT assay2021Bioorganic & medicinal chemistry letters, 04-15, Volume: 38Synthesis, biological evaluation, and structure-activity relationships of new tubulin polymerization inhibitors based on 5-amino-1,2,4-triazole scaffold.
AID730198Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 0.01 uM after 24 hrs by propidium iodide staining-based FACS flow cytometric analysis (Rvb = 8.52%)2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Synthesis and structure-activity relationships of N-methyl-5,6,7-trimethoxylindoles as novel antimitotic and vascular disrupting agents.
AID1348295Inhibition of [3H]colchicine binding to bovine brain tubulin at 1 to 5 uM by DEAE-cellulose filter method relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Targeting tubulin polymerization by novel 7-aryl-pyrroloquinolinones: Synthesis, biological activity and SARs.
AID214524Percentage control on Tubulin- Dependent GTP hydrolysis was evaluated at 10 micro M concentration1999Bioorganic & medicinal chemistry letters, Apr-19, Volume: 9, Issue:8
A new anti-tubulin agent containing the benzo[b]thiophene ring system.
AID1600463Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID606033Cytotoxicity against mouse L1210 cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
A novel class of trans-methylpyrazoline analogs of combretastatins: synthesis and in-vitro biological testing.
AID662347Antiproliferative activity in human T84 cells assessed as cell viability after 72 hrs by MTT assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID605709Antiproliferative activity against human M21 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID1472467Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured after 20 mins by spectrophotometric analysis2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Quinazolinone-Based Anticancer Agents: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Tubulin Co-crystal Structure.
AID605779Toxicity against fertilized chicken embryo assessed as mortality at 1 ug per egg, iv by CAM assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID1689079Induction of apoptosis in human HeLa cells assessed as down regulation of Bcl-2 protein expression at 0.5 uM measured after 24 hrs by western blot analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1472476Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Quinazolinone-Based Anticancer Agents: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Tubulin Co-crystal Structure.
AID1059991Cytotoxicity against human CEM/0 cells assessed as growth inhibition after 48 hrs by coulter counting analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
AID1435090Induction of cytoplasmic microtubule network disassembly in human A549 cells assessed as cell surface occupied by fluorescent microtubule network at 0.01 uM after 4 hrs by confocal fluorescence microscopic method (Rvb = 31 +/- 4%)2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID107052In vitro cytotoxic activity was tested against human melanoma cancer (M14) cell line2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.
AID1778192Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition after 48 hrs by MTT assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines.
AID1068627Growth inhibition of human HOP62 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1917302Antiproliferative activity against human RKO cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID730200Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 0.01 uM after 24 hrs by propidium iodide staining-based FACS flow cytometric analysis (Rvb = 32.56%)2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Synthesis and structure-activity relationships of N-methyl-5,6,7-trimethoxylindoles as novel antimitotic and vascular disrupting agents.
AID1194525Cytotoxicity against human A549 cells2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Novel hybrid nocodazole analogues as tubulin polymerization inhibitors and their antiproliferative activity.
AID1263251Cytotoxicity against human HOP62 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID767273Inhibition of [3H] radiolabelled colchicine binding to tubulin beta (unknown origin) at 5 uM by DEAE-cellulose filter method2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exploring natural product chemistry and biology with multicomponent reactions. 5. Discovery of a novel tubulin-targeting scaffold derived from the rigidin family of marine alkaloids.
AID685373Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 4 uM after 24 hrs by FACS analysis (Rvb = 6.79%)2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1534542Drug metabolism in human liver microsomes assessed as cytochrome P450-mediated 4-(1-(3-hydroxy-4-methoxyphenyl)vinyl)-2,6-dimethoxyphenol metabolite formation at 100 uM after 6 hrs in presence of NADPH generating system by HPLC-UV-MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID1233620Inhibition of bovine brain tubulin polymerization extent after 20 mins by turbidimetrically2015European journal of medicinal chemistry, Jun-24, Volume: 99Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin polymerization inhibitors.
AID1508149Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1728928Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at S phase at 1 uM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 19.84%)2021European journal of medicinal chemistry, Mar-05, Volume: 213Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.
AID642055Antiproliferative activity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1506490Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2017MedChemComm, Jan-01, Volume: 8, Issue:1
Design, synthesis, anticancer activity and docking studies of theophylline containing 1,2,3-triazoles with variant amide derivatives.
AID1514431Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 48 hrs by MTT assay
AID1324128Cytotoxicity against human Caki1 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID669464Growth inhibition of combretastatin-resistant human HT-29 cells after 48 hrs by SRB assay2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID630729Cytotoxicity against human HCT116 cells assessed as reduction of [3H]thymidine incorporation after 72 hrs by scintillation counting2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
1,1-Diarylalkenes as anticancer agents: dual inhibitors of tubulin polymerization and phosphodiesterase 4.
AID771217Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID95871Inhibitory concentration against human oral cancer cell line (KB) using tetrazolium dye reduction assay (MTT)2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID103262Cytotoxic concentration required to inhibit 50% cell growth in MCF-7 breast carcinoma cell lines1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization.
AID1405371Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK8 assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID595052Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis, biological evaluation, and molecular docking studies of resveratrol derivatives possessing chalcone moiety as potential antitubulin agents.
AID146552Cell growth inhibition of lung-NSC NCI-H460 cells, expressed as 50% reduction in the net protein increase2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.
AID1882904Inhibition of porcine brain tubulin polymerization at 5 uM measured at 1 min interval for 60 mins by fluorescence assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1459301Induction of reactive oxygen species generation in human MCF7 cells assessed as decrease in cell viability at 0.1 to 10 uM in presence of N-acetyl cysteine after 48 hrs by alamarBlue assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1462293Antiproliferative activity against human U87 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis of different heterocycles-linked chalcone conjugates as cytotoxic agents and tubulin polymerization inhibitors.
AID273359Inhibition of tubulin polymerization2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
AID443468Cytotoxicity against human MCF7 cells by MTT assay2009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
Synthesis and antitumor-evaluation of cyclopropyl-containing combretastatin analogs.
AID685186Growth inhibition of human HCT15 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1408369Inhibition of porcine brain tubulin polymerization after 30 mins by spectrophotometric method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID616977Antiproliferative activity against human MDA-MB-231 after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1351620Inhibition of tubulin polymerization in human SKOV3 cells assessed as micronuclei formation at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID643529Cytotoxicity against human Jurkat cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Synthesis and evaluation of 1,5-disubstituted tetrazoles as rigid analogues of combretastatin A-4 with potent antiproliferative and antitumor activity.
AID1774977Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Lead Optimization: Synthesis and Biological Evaluation of PBT-1 Derivatives as Novel Antitumor Agents.
AID1411599Inhibition of human OATP2B1 expressed in HEK293 cells assessed as DBF uptake after 5 mins by fluorescence assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1570328Antiviral activity against wild type Dengue virus serotype 2 infected in human HuH7 cells assessed as reduction in viral titer measured after 24 hrs by Cell-Titer Glo luminescent assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.
AID569520Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 5 uM after 24 hrs using propidium iodide staining by flow cytometry relative to control2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents.
AID273362Antiproliferative activity against human H460 cell line by methylene blue dye assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
AID1263264Cytotoxicity against human SF539 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID616988Half life in Sprague-Dawley rat at 6 umol/kg, iv2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1392071Inhibition of bovine brain tubulin polymerization assessed as reduction in tubulin assembly pretreated for 15 mins followed by GTP addition by spectrophotometric method2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.
AID757691Cytotoxicity against human SMMC7721 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Synthesis and antitumor activity of novel 3,4-diaryl squaric acid analogs.
AID1689141Cell cycle arrest in human EA.hy926 cells assessed as accumulation at sub-G1 phase after 24 hrs by propidium iodide staining based flow cytometric analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.
AID1906214Induction of cell cycle arrest in human HeLa cells assessed as 4N cells at 6 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 17.1%)
AID550209Antimitotic activity against Paracentrotus lividus embryo assessed as cleavage alteration after 2.5 to 6 hrs post fertilization by sea urchin embryo assay2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Synthesis of antimitotic polyalkoxyphenyl derivatives of combretastatin using plant allylpolyalkoxybenzenes.
AID1709302Resistant index, ratio of IC50 for cytotoxicity against human HeLa cells expressing WT-beta3 to IC50 for cytotoxicity against human HeLa cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1628251Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 10 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 35%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID1421771Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Conformation impacts on the bioactivities of SMART analogues.
AID1738827Antiproliferative activity against human SEM cells assessed as inhibition of cell growth2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors.
AID502716Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID57722Compound was evaluated against Human cell line prostate DU-1451999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID93448Evaluated for growth inhibition (anticancer activity) of Human prostate cancer DU-145 cell line2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID200796Cell growth inhibition of central nervous system (CNS) SF-268 cells, expressed as 50% reduction in the net protein increase2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.
AID1317614Induction of apoptosis in human EAhy926 cells assessed as increase in apoptotic cells at growth inhibitory IC50 measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1353646Cell cycle arrest in human A549 cells assessed as accumulation at sub-G0 phase at 50 nM after 20 hrs by propidium iodide staining based flow cytometry (Rvb = 6.6 +/- 0.1%)2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID1351630Induction of apoptosis in human HeLa cells assessed as increase in histone-associated DNA fragments in mononucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1463423Cell cycle arrest in human PC3 cells assessed as accumulation at S phase at 0.05 uM incubated for 24 hrs by propidium iodide staining based FACS assay (Rvb = 23.5%)2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Constructing novel dihydrofuran and dihydroisoxazole analogues of isocombretastatin-4 as tubulin polymerization inhibitors through [3+2] reactions.
AID502717Growth inhibition of human COLO205 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID642529Growth inhibition of human HT-29 cells after 72 hrs by methylene blue assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. Part 2. The impact of bridging groups at position C-2.
AID1064411Growth inhibition of human SW620 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID288668Growth inhibition of human MCF7 cells after 48 hrs2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies.
AID1126009Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 58.60%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1431170Inhibition of bovine brain tubulin assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
AID1068625Growth inhibition of human NCI-H23 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1352484Inhibition of beta-tubulin polymerization in human MCF7 cells after 72 hrs by ELISA2018European journal of medicinal chemistry, Feb-25, Volume: 146Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation.
AID461021Displacement of [3H]colchicine from tubulin at 5 uM by turbidimetry2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
A boronic acid chalcone analog of combretastatin A-4 as a potent anti-proliferation agent.
AID142329Inhibitory activity against murine colon 26 adenocarcinoma cell2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Antineoplastic agents. 487. Synthesis and biological evaluation of the antineoplastic agent 3,4-methylenedioxy-5,4'-dimethoxy-3'-amino-Z-stilbene and derived amino acid amides.
AID1647056Induction of apoptotic cell death in human HepG2 cells assessed as decrease in viable cells by measuring reduction in green fluorescence at 0.1 uM measured after 24 hrs by acridine orange/ethidium bromide staining based fluorescence microscopy2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID273280Inhibition of tubulin polymerization2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.
AID1860219Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-functional antitumor conjugates improving the anti-metastasis effect of combretastatin A4 by targeting tubulin polymerization and matrix metalloproteinases.
AID213997Evaluated for the inhibition of tubulin polymerization without pre-incubation1993Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
Antitumor agents. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic
AID1422355Inhibition of bovine brain t in presence of 0.4 mM GTP2018European journal of medicinal chemistry, Nov-05, Volume: 159Modified carbazoles destabilize microtubules and kill glioblastoma multiform cells.
AID474641Induction of apoptosis in human HeLa cells assessed as cells containing hypodiploid DNA at 0.02 uM after 24 hrs by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID502710Growth inhibition of human RPMI8266 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID449225Growth inhibition of HSMC2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
AID1401724Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and biological evaluation of N-substituted 3-oxo-1,2,3,4-tetrahydro-quinoxaline-6-carboxylic acid derivatives as tubulin polymerization inhibitors.
AID1466245Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Synthesis and biological evaluation of novel indole-pyrimidine hybrids bearing morpholine and thiomorpholine moieties.
AID1308609Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining at 150 mins in presence of NADPH regenerating system by HPLC method2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1860525Antiproliferative activity against human CAL-27 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC.
AID1263268Cytotoxicity against human LOXIMVI cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1435086Induction of mitosis in human A549 cells at 0.5 uM after 24 hrs by Draq5 staining-based confocal fluorescence microscopic method (Rvb = 2.7 +/- 0.8%)2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1724517Inhibition of pig brain tubulin polymerization by fluorescence based assay2020Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19
A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors.
AID1713786Induction of nuclear fragmentation in human KB-VIN cells at 0.2 uM incubated for 24 hrs by immunofluorescence staining based confocal microscopy2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Triethylated chromones with substituted naphthalenes as tubulin inhibitors.
AID1917305Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID1263256Cytotoxicity against human HCC2998 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID444159Antiproliferative activity against human HeLa cells expressing wild type beta3 tubulin after 48 hrs by SRB assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID79469Cell growth inhibition against HA22T human liver cancer cells using MTS assay2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
AID1064434Antimitotic activity against sea urchin embryo free-swimming blastula model assessed as embryo spinning compound treated at 8 to 10 hrs post-fertilization measured after 0.25 to 20 hrs2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1299681Inhibition of porcine brain tubulin polymerization measured every 2 mins for 1 hr by fluorescence analysis in presence of GTP2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Far-Red Light-Activatable Prodrug of Paclitaxel for the Combined Effects of Photodynamic Therapy and Site-Specific Paclitaxel Chemotherapy.
AID502528Inhibition of pig tubulin polymerization2010Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18
1,2,3-triazole analogs of combretastatin A-4 as potential microtubule-binding agents.
AID1179508Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetric method2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Synthesis, biological evaluation and molecular modeling of 1,3,4-thiadiazol-2-amide derivatives as novel antitubulin agents.
AID1472475Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Quinazolinone-Based Anticancer Agents: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Tubulin Co-crystal Structure.
AID1730586Inhibition of porcine brain tubulin polymerization at 15 uM measured after 60 mins by fluorescence assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID1064436Antimitotic activity against sea urchin embryo model assessed as cleavage alteration of fertilized egg compound treated at 8 to 20 mins post-fertilization and 45 to 55 mins prior to first mitotic cycle completion measured 2.5 to 5.5 hrs post-fertilization2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1906264Antiproliferative activity against human SiHa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
AID1435098Inhibition of cytoplasmic microtubule network assembly in human A549 cells at 0.05 uM preincubated for 4 hrs followed by compound washout measured after 120 mins by confocal fluorescence microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID363250Growth inhibition of human SK-OV-3 after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Design, synthesis and biological evaluation of dihydronaphthalene and benzosuberene analogs of the combretastatins as inhibitors of tubulin polymerization in cancer chemotherapy.
AID314022Antiproliferative activity against human HS578T cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID1059992Cytotoxicity against human Molt4/C8 cells assessed as growth inhibition after 48 hrs by coulter counting analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
AID1738834Inhibition of [3H]colchicine binding to bovine brain tubulin at 0.5 uM relative to control2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors.
AID281503Inhibition of tubulin polymerization2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Arylthioindoles, potent inhibitors of tubulin polymerization.
AID1737845Half life in human liver microsomes at 10 uM in presence of NADPH by LC/MS/MS analysis2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID391281Inhibition of tubulin polymerization2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Novel A-ring and B-ring modified combretastatin A-4 (CA-4) analogues endowed with interesting cytotoxic activity.
AID1458823Antiproliferative activity against human MGC803 cells after 48 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1517173Inhibition of tubulin beta polymerization in human HepG2 cells at IC50 using TMB substrate preincubated for 2 hrs followed by substrate addition measured after 15 to 20 mins in presence of GTP by ELISA relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Potent combretastatin A-4 analogs containing 1,2,4-triazole: Synthesis, antiproliferative, anti-tubulin activity, and docking study.
AID341686Displacement of [3H]colchicine from tubulin at 5 uM2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Asymmetric synthesis of 2,3-dihydro-2-arylquinazolin-4-ones: methodology and application to a potent fluorescent tubulin inhibitor with anticancer activity.
AID1727314Antiproliferative activity against human MiaPaca2 cells assessed as cell viability after 24 hrs by Celltiter-Glo assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation.
AID1860220Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-functional antitumor conjugates improving the anti-metastasis effect of combretastatin A4 by targeting tubulin polymerization and matrix metalloproteinases.
AID1906266Resistant factor, ratio of IC50 for antiproliferative activity against human SiHa/DDP cells to IC50 for human SiHa cells
AID502730Growth inhibition of human M14 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID658261Cytotoxicity against human MDA-MB-231 cells after 72 hrs using resazurin dye by microtiter plate fluorimeter analysis2012European journal of medicinal chemistry, Jun, Volume: 52Conformationnally restricted naphthalene derivatives type isocombretastatin A-4 and isoerianin analogues: synthesis, cytotoxicity and antitubulin activity.
AID1917311Inhibition of pig brain tubulin polymerization by spectrometric method2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID1403598Disruption of microtubule structure in human SKOV3 cells assessed as decrease in density at 50 nM after 24 hrs by DAPI staining based immunofluorescence assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
AID1811591Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation measured after 48 hrs by SRB assay2021Bioorganic & medicinal chemistry, 12-15, Volume: 52Synthetic development of sugar amino acid oligomers towards novel podophyllotoxin analogues.
AID280076Antiproliferative activity against drug sensitive NCI-H69 cell line by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID1233574Antiproliferative activity against human HT1080 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model.
AID1162821Induction of cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 50 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 87.75%)2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID1693361Relative resistance, ratio of IC50 for inhibition of beta3 Tubulin (unknown origin) expressed in human HeLa cell line assessed as inhibition of cell proliferation to IC50 antiproliferative activity against human HeLa cells2021Bioorganic & medicinal chemistry, 01-01, Volume: 29The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
AID1469220Resistance factor, ratio of IC50 for human HepG2/DOX cells to IC50 for human HepG2 cells2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1317622Induction of apoptosis in human EAhy926 cells assessed as necrotic cells at 0.11 uM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID617011Antiproliferative activity against MDR-1-6/6 overexpressing human SKOV3 cells2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID228626Inhibition of tubulin polymerization2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID1075759Inhibition of tubulin (unknown origin) polymerization incubated for 15 mins prior to GTP addition measured after 20 mins by turbidimetry2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of 4-(N-cycloamino)phenylquinazolines as a novel class of tubulin-polymerization inhibitors targeting the colchicine site.
AID1308545Cytotoxicity against human A2780 cells assessed as cell viability after 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID265426Cell cycle arrest in NCI-H460 cells by accumulation at G1/0 phase cell at 3 nM post 24 hrs treatment and 48 hrs recovery2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID1198455Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents.
AID1276120Cytotoxicity against human HT-29 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID94872Cell growth inhibition of colon KM20L2 cells, expressed as 50% reduction in the net protein increase2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.
AID644546Cell cycle arrest in human SKOV3 cells assessed as accumulation at S phase at 5 nM by flow cytometry (Rvb = 31%)2012Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5
Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A-1.
AID635032Inhibition of porcine brain tubulin polymerization after 60 mins2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID1187065Inhibition of bovine brain tubulin preincubated for 20 mins by turbidimetry2014European journal of medicinal chemistry, Oct-06, Volume: 85Discovery and molecular modeling of novel 1-indolyl acetate--5-nitroimidazole targeting tubulin polymerization as antiproliferative agents.
AID670878Inhibition of bovine brain microtubule polymerization by spectrophotometric analysis2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
AID281357Volume of distribution in iv dosed Swiss Albino mouse plasma2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID214692Inhibitory concentration required against tubulin polymerization in the antimicrotubule activity test2001Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9
Antitumor agents. Part 204: synthesis and biological evaluation of substituted 2-aryl quinazolinones.
AID757689Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Synthesis and antitumor activity of novel 3,4-diaryl squaric acid analogs.
AID1263255Cytotoxicity against human COLO205 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1518087Induction of apoptosis in human MDA-MB-468 cells assessed as early apoptotic cells at 100 nM after 72 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 0.35 to 1.25%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1064432Growth inhibition of human HL-60(TB) cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1408388Cell cycle arrest in human K562 cells assessed as accumulation at S phase at 0.02 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 49.41%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID437547Anticancer activity against human MCF7 cells after 72 hrs2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines).
AID502736Growth inhibition of human IGROV1 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1689065Cytotoxicity against HUVEC cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1901292Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2022European journal of medicinal chemistry, Feb-15, Volume: 230Synthesis and biological evaluation of novel hybrids of phenylsulfonyl furoxan and phenstatin derivatives as potent anti-tumor agents.
AID670880Binding affinity to bovine brain tubulin by spectrophotometric analysis2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
AID1917306Antiproliferative activity against human U-87 MG cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID1055627Cytotoxicity against human SKOV3 cells after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis of structurally diverse benzosuberene analogues and their biological evaluation as anti-cancer agents.
AID1405368Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CCK8 assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID1736444Antiproliferative activity against human HT29 cells incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1403592Antiproliferative activity against human SKOV3 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
AID314011Antiproliferative activity against human SF295 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID1873708Induction of apoptosis in human HeLa cells assessed as viable cells at 10 nM incubated for 24 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 85.7%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID415690Cytotoxicity against human HCT116 cells after 72 hrs by MTS assay2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
Synthesis and biological evaluation of cis-locked vinylogous combretastatin-A4 analogues: derivatives with a cyclopropyl-vinyl or a cyclopropyl-amide bridge.
AID1517359Inhibition of pig brain tubulin polymerization by spectrophotometric method2019European journal of medicinal chemistry, Dec-01, Volume: 183Design and synthesis of (2-(phenylamino)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone analogues as potent anti-tubulin polymerization agents.
AID1068613Growth inhibition of human SF295 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1421773Selectivity index, ratio of IC50 for mouse L929 cells to IC50 for human SGC7901 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158Conformation impacts on the bioactivities of SMART analogues.
AID1635334Antiproliferative activity against multidrug resistant human HeLa cells expressing wild type beta3 tubulin after 48 hrs by SRB assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID1693362Antiproliferative activity against human SK-OV-3 cells assessed as decrease in cell growth measured after 48 hrs by SRB method2021Bioorganic & medicinal chemistry, 01-01, Volume: 29The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
AID1906226Induction of cell cycle arrest in human HeLa cells assessed as accumulation of cells at G2/M phase at 6 nM after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 17.1%)
AID494822Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 10 uM after 24 hrs by FACS analysis2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
Synthesis and anti-cancer activity of chalcone linked imidazolones.
AID635031Inhibition of angiogenesis in endothelial cells assessed as inhibition of tube formation after 18 hrs by inverted microscopic analysis2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID1890476Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells in G2 phase at 10 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 8.95 %)2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
AID290177Antiproliferative activity against human PC3 cells2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents.
AID1524357Cytotoxicity against human K562 cells after 48 hrs by SRB assay2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents.
AID455035Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID663556Displacement of colchicine from tubulin at 5 uM2012ACS medicinal chemistry letters, Jan-12, Volume: 3, Issue:1
Steroidomimetic Tetrahydroisoquinolines for the Design of New Microtubule Disruptors.
AID437544Anticancer activity against human Bel7402 cells after 72 hrs2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines).
AID1263279Cytotoxicity against human SKOV3 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID450676Cytotoxicity against human HT-29 cells after 72 hrs by XTT assay2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Isocombretastatins A: 1,1-diarylethenes as potent inhibitors of tubulin polymerization and cytotoxic compounds.
AID502751Growth inhibition of human Hs 578T cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID548393Antiproliferative activity against estrogen receptor deficient human MDA-MB-231 cells after 72 hrs by MTT assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Lead identification of conformationally restricted β-lactam type combretastatin analogues: synthesis, antiproliferative activity and tubulin targeting effects.
AID1064380Growth inhibition of human UO31 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID691618Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID494824Cell cycle arrest in human MCF7 cells assessed as accumulation at G0 phase at 30 uM after 24 hrs by FACS analysis2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
Synthesis and anti-cancer activity of chalcone linked imidazolones.
AID1324119Cytotoxicity against human SK-MEL-5 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1506735Antiproliferative activity in human IMR32 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay2017MedChemComm, Feb-01, Volume: 8, Issue:2
Synthesis and biological evaluation of (-)-kunstleramide and its derivatives.
AID1709307Displacement of [3H]-colchicine from bovine brain tubulin at 5 uM after 10 mins by DEAE-cellulose filter method relative to control2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1317621Induction of apoptosis in human HepG2 cells assessed as necrotic cells at 0.11 uM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID280073Antiproliferative activity against drug resistant Messa/DX5 cell line expressing MDR1 by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID1728935Induction of apoptosis in human MDA-MB-231 cells assessed as viable cells at 1 uM measured after 24 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 90.9%)2021European journal of medicinal chemistry, Mar-05, Volume: 213Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.
AID1469206Growth inhibition of human HepG2 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1458822Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1628256Inhibition of cell migration of human MDA-MB-231 cells at 50 nM by wound closure assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID330410Cytotoxicity against human NCIH460 cells after 48 hrs by SRB assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID269714Cell cycle arrest in SHSY5Y cells by accumulation at G1 phase after 4 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID479723Displacement of [3H]colchicine from bovine tubulin at 1 uM2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Synthesis and antitumor activity of 1,5-disubstituted 1,2,4-triazoles as cis-restricted combretastatin analogues.
AID1533672Inhibition of porcine brain tubulin polymerization after 2 hrs2019European journal of medicinal chemistry, Feb-01, Volume: 163New naphthopyran analogues of LY290181 as potential tumor vascular-disrupting agents.
AID1064379Growth inhibition of human MCF7 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1381552Cytotoxicity against human Capan1 cells after 48 hrs by XTT assay2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
New somatostatin-drug conjugates for effective targeting pancreatic cancer.
AID1411593Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability up to 20 uM after 24 hrs by MTT assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID307425Cytotoxicity against human A549 cells2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Synthesis and biological activity of naphthalene analogues of phenstatins: naphthylphenstatins.
AID1600469Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1689103Toxicity in BALB/c nude mouse transfected with human HeLa cells assessed as kidney damage at 30 mg/kg/day, iv for 21 days by H&E staining based immunohistochemistry2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID685183Growth inhibition of human COLO205 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID691652Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as effect on lymphocyte count at 50 mg/kg, ip qd after 21 days (Rvb = 15.88 +/- 0.41 x 10'3 mm'-3)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1310180Inhibition of porcine brain alpha/beta tubulin polymerization at 5 uM measured every 20 sec by microplate reader analysis2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1408402Antitumor activity against mouse H22 cells implanted in ICR mouse assessed as tumor growth inhibition at 30 mg/kg, iv administered once daily for 21 consecutive days relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID331686Inhibition of rat brain tubulin polymerization2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Tubulysin analogs incorporating desmethyl and dimethyl tubuphenylalanine derivatives.
AID1196866Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 1 uM after 48 hrs by MTT assay2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID1586363Antiproliferative activity against HMEC1 cells by MTT assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4.
AID1057194Antiangiogenic activity in human HT-29 cells assessed as inhibition of VEGF mRNA expression at < IC50 after 48 hrs by RT-PCR analysis relative to control2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity.
AID1882892Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID474627Cytotoxicity against human RT112 cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1717477Cell cycle arrest in human HT-1080 cells assessed as accumulation at G2/M phase at 0.025 uM measured after 12 hrs by propidium iodide staining based flow cytometry (Rvb = 32.81%)
AID685194Growth inhibition of human U251cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1162814Cytotoxicity against human HeLa cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID657881Growth inhibition of human KM20L2 cells after 48 hrs by sulforhodamine B assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID1057197Selectivity ratio of IC50 for HEK293 cells to IC50 for human HT-29 cells2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity.
AID103917Concentration which produces 50% inhibition of growth of human breast tumor MCF-7 cell line2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Combretoxazolones: synthesis, cytotoxicity and antitumor activity.
AID403055Displacement of [3H]vinblastine from bovine tubulin at 80 uM2005Journal of natural products, Aug, Volume: 68, Issue:8
Antineoplastic agents. 515. Synthesis of human cancer cell growth inhibitors derived from 3,4-methylenedioxy-5,4'-dimethoxy-3'-amino-Z-stilbene.
AID1422790Antiproliferative activity against human KB cells after 72 hrs by MTT assay
AID1736455Selectivity index, ratio of IC50 for drug resistant human K562 cells to IC50 for human K562 cells2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID455988Cytotoxicity against mouse FM3A0 cells after 2 days2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of tubulin polymerization.
AID619861Effect on microtubule network in human MCF7 cells assessed as microtubule depolymerization at 100 nM after 16 hrs by confocal microscopic analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID1565959Metabolic stability in Sprague-Dawley rat liver microsomes assessed as parent compound remaining after 150 mins in presence of NADPH by HPLC-UV-MS analysis
AID780972Displacement of [3H]-colchicine from biotin-labeled tubulin (unknown origin) at 1 uM after 2 hrs by scintillation proximity assay relative to control2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Furanylazaindoles: potent anticancer agents in vitro and in vivo.
AID1773139Inhibition of pig brain tubulin polymerization at 10 uM by spectrometric method relative to control2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1336763Inhibition of colchicine binding to tubulin (unknown origin) at 5 to 20 uM after 60 mins by fluorescence assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1585997Cell cycle arrest in human BT549 cells assessed as accumulation of cells at G2/M phase at 8 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 8.88%)
AID1533704Antiangiogenic activity in Leghorn chicken embryo chorioallantoic membrane assessed as reduction in blood vessel area at 2.5 nmol after 6 hrs by light microscopic analysis relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163New naphthopyran analogues of LY290181 as potential tumor vascular-disrupting agents.
AID697461Toxicity in fertilized chicken embryo assessed as mortality rate at 1 ug per egg, iv administered on day 11 measured on day 17 by CAM assay2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Synthesis, biological evaluation, and structure-activity relationships of novel substituted N-phenyl ureidobenzenesulfonate derivatives blocking cell cycle progression in S-phase and inducing DNA double-strand breaks.
AID1411596Inhibition of human OAT1 expressed in HEK293 cells assessed as 6-CF uptake after 5 mins by fluorescence assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1771500Induction of cell cycle arrest in human MGC-803 cells assessed as accumulation at G2/M phase at 2 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 28.59 %)2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1324100Cytotoxicity against human COLO205 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1689075Induction of apoptosis in human HeLa cells assessed as cell membrane integrity loss, chromatin condensation and apoptotic body formation by measuring reduction in green fluorescence intensity at 0.5 uM measured after 24 hrs by AO/EB dual staining based fl2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID397292Cytotoxicity against human MDA-MB-231 cells after 72 hrs2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Isocombretastatins a versus combretastatins a: the forgotten isoCA-4 isomer as a highly promising cytotoxic and antitubulin agent.
AID455713Inhibition of bovine tubulin polymerization after 30 mins by turbidimetrically2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Application of the McMurry coupling reaction in the synthesis of tri- and tetra-arylethylene analogues as potential cancer chemotherapeutic agents.
AID662344Antiproliferative activity in human SW48 cells assessed as cell viability after 72 hrs by MTT assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID595713Cytotoxicity against human HBL100 cells after 72 hrs by MTT assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Synthesis and biological evaluation of 4-arylcoumarin analogues of combretastatins. Part 2.
AID1183716Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID1431180Growth inhibition of human NCI/ADR-RES cells over expressing Pgp measured after 96 hrs by sulforhodamine B assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
AID1459289Disruption of microtubule network in human MCF7 cells at 100 nM after 16 hrs by immunofluorescence analysis2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1727316Antiproliferative activity against human MCF7 cells assessed as cell viability after 24 hrs by Celltiter-Glo assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation.
AID461788Displacement of [3H]colchicine from tubulin by at 1 uM scintillation proximity assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors.
AID1906243Induction of apoptosis in human HeLa cells assessed as late apoptotic cells at 3 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 5.22%)
AID1068619Growth inhibition of human HCT116 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1411802Inhibition of pig brain tubulin polymerization by spectrophotometric analysis2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID622409Cytotoxicity against human HT29 cells after 48 hrs by sulforhodamine B assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID474631Inhibition of tubulin polymerization2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID622530Inhibition of bovine brain tubulin polymerization pre-incubated for 15 mins at 26 degC, cooled followed by 20 mins acquisition at 26 degC by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1126017Plasma concentration in C57BL/6 mouse at 5 mg/kg, po after 3 hrs2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1608964Displacement of [3H]-colchicine from bovine brain tubulin at 0.5 uM incubated for 1 hr by relative to control2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.
AID685368Growth inhibition of human Hs578T cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1498595Displacement of [3H]colchicine from tubulin (unknown origin) at 1 uM after 10 mins relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
The inhibitory effect of kokusaginine on the growth of human breast cancer cells and MDR-resistant cells is mediated by the inhibition of tubulin assembly.
AID1317603Cell cycle arrest in human HepG2 cells assessed as decrease in accumulation of G2/M phase at growth inhibitory IC50 measured after 72 hrs by propidium iodide-staining based FACS analysis2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1352576Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Synthesis and biological evaluation of 4,6-diphenyl-2-(1H-pyrrol-1-yl)nicotinonitrile analogues of crolibulin and combretastatin A-4.
AID281359Mean residence time in iv dosed Swiss Albino mouse plasma2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID730209Antimitotic activity in human A549 cells assessed as disruption of microtubule organization at 0.01 uM after 16 hrs by DAPI staining-based Zeiss microscopic analysis relative to control2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Synthesis and structure-activity relationships of N-methyl-5,6,7-trimethoxylindoles as novel antimitotic and vascular disrupting agents.
AID737112Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID1310188Growth inhibition of human HCT116 cells expressing wild type p53 after 72 hrs by MTT assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1757276Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID269725Cell cycle arrest in SHSY5Y cells by accumulation at S phase after 24 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID90436Evaluated for growth inhibition (anticancer activity) of Human colon KM20L2 cancer cell line2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID1183725Induction of apoptosis in human HeLa cells assessed as unstructured tubulin foci at 100 nM by immunofluorescence analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID749586Inhibition of sheep brain tubulin assembly by DAPI staining-based fluorescence assay2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Synthesis and biological evaluation of fluoro analogues of antimitotic phenstatin.
AID1367972Antiproliferative activity against human HeLa cells by MTT assay
AID657608Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Synthesis, biological evaluation, and molecular docking studies of 2,6-dinitro-4-(trifluoromethyl)phenoxysalicylaldoxime derivatives as novel antitubulin agents.
AID502738Growth inhibition of human OVCAR4 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1317593Cytostatic activity against human HaCaT cells assessed as cell survival up to 25 uM measured after 72 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID382330Inhibition of pig brain tubulin polymerization2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin.
AID1351655Inhibition of tubulin polymerization in human HeLa cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1538717Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM relative to control2019European journal of medicinal chemistry, Sep-15, Volume: 178Evaluating the effects of fluorine on biological properties and metabolic stability of some antitubulin 3-substituted 7-phenyl-pyrroloquinolinones.
AID1402698Inhibition of microtubules in human HeLa cells assessed as induction of cell cycle arrest in metaphase at 5 uM after 24 hrs by DAPI staining-based confocal microscopic analysis
AID1701013Selectivity index, ratio of GI50 for cytotoxicity against human L02 cells to GI50 for antiproliferation activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
AID1411798Antiproliferative activity against human HepG2 cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID1263259Cytotoxicity against human HT-29 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1860231Cell cycle arrest in human HepG2 cells assessed as accumulation of cells in S phase at 100 nM measured after 12 hrs by flow cytometry method (Rvb = 34.29%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-functional antitumor conjugates improving the anti-metastasis effect of combretastatin A4 by targeting tubulin polymerization and matrix metalloproteinases.
AID1738828Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors.
AID1068636Growth inhibition of human CCRF-CEM cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1059054Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis, cytotoxic evaluation and molecular docking study of 2-alkylthio-4-(2,3,4-trimethoxyphenyl)-5-aryl-thiazoles as tubulin polymerization inhibitors.
AID1689073Induction of apoptosis in human HeLa cells assessed as viable cells at 0.5 uM measured after 24 hrs by Annexin-V-FITC and PI staining based flow cytometry (Rvb = 96.3%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1811593Antiproliferative activity against human M21 cells assessed as inhibition of cell proliferation measured after 48 hrs by SRB assay2021Bioorganic & medicinal chemistry, 12-15, Volume: 52Synthetic development of sugar amino acid oligomers towards novel podophyllotoxin analogues.
AID1406424Antitumor activity against human HeLa cells xenografted in nude mouse assessed as tumor volume at 10 mg/kg, ip after 14 days (Rvb = 2292.17 mm3)2018European journal of medicinal chemistry, Aug-05, Volume: 156Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation.
AID1760385Antiproliferative activity against human HepG2 cells incubated for 24 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020).
AID642092Growth inhibition of human HSMC cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID685382Growth inhibition of human SW620 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1352575Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Synthesis and biological evaluation of 4,6-diphenyl-2-(1H-pyrrol-1-yl)nicotinonitrile analogues of crolibulin and combretastatin A-4.
AID1431171Displacement of [3H]colchicine from bovine brain tubulin at 5 uM measured after 10 mins by liquid scintillation counting method relative to control2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
AID670879Cytotoxicity against human A549 cells after 48 hrs by WST-8 assay2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
AID1059984Displacement of [3H]-colchicine from tubulin (unknown origin) at 5 uM after 10 mins relative to control2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
AID1064395Growth inhibition of human IGROV1 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID605776Disruption of cytoskeleton microtubule structure of human M21 cells at 5 times IC50 after 16 hrs by indirect immunofluorescence assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID1811164Inhibition of tubulin polymerization (unknown origin)2021Bioorganic & medicinal chemistry letters, 11-01, Volume: 51Synthesis of the analogs of plocabulin and their preliminary structure-activity relationship study.
AID1647058Induction of mitochondrial membrane potential disruption in human HepG2 cells assessed as reduction in red fluorescence at 0.1 uM measured after 24 hrs by JC1 staining based fluorescence microscopy2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1195296Resistance ratio of IC50 for human SKOV3-MDR1-M6/6 cells to IC50 for human SKOV3 cells2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID1324096Cytotoxicity against human HOP92 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1541865Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
AID331685Antiproliferative activity against human 1A9 cells2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Tubulysin analogs incorporating desmethyl and dimethyl tubuphenylalanine derivatives.
AID1285317Cytotoxicity against human A549 cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID1351600Cell cycle arrest in human SKOV3 cells assessed as accumulation of cells at G2/M phase at 0.1 to 1 uM after 24 hrs by propidium iodide staining-based FACS analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1231336Induction of apoptosis in human NCM460 cells assessed as phosphatidylserine externalization 0.1 and 20 uM after 48 hrs by AnnexinV/propidium iodide staining based Tali-image based cytometry2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4.
AID340149Growth inhibition of P-gp 170/MDR overexpressing human KB-vin10 cells after 72 hrs by methylene blue dye assay2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.
AID1402063Antiproliferative activity against mouse L1210 cells after 2 days by Coulter counter method2018European journal of medicinal chemistry, Jan-01, Volume: 1432-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.
AID616891Antiproliferative activity against human MCF7 cells assessed after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1518067Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID403056Growth inhibition of human MCF7 after 48 hrs by sulforhodamine B method2005Journal of natural products, Aug, Volume: 68, Issue:8
Antineoplastic agents. 515. Synthesis of human cancer cell growth inhibitors derived from 3,4-methylenedioxy-5,4'-dimethoxy-3'-amino-Z-stilbene.
AID605711Cell cycle arrest in human M21 cells assessed as accumulation at G0/G1 phase at 5 times IC50 after 24 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 61%)2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID1324137Cytotoxicity against human Hs 578T cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID473861Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 10 mins2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Synthesis, antitubulin, and antiproliferative SAR of analogues of 2-methoxyestradiol-3,17-O,O-bis-sulfamate.
AID1263257Cytotoxicity against human HCT116 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1689067Anticancer activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1565960Metabolic stability in Sprague-Dawley rat liver microsomes assessed as parent compound remaining after 180 mins in presence of NADPH by HPLC-UV-MS analysis
AID1064382Growth inhibition of human TK10 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1183655Growth inhibition of human CCRF-CEM cells after 72 hrs by MTT assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID1862611Antiproliferative activity against human MIA PaCa-2 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1294469Growth inhibition of human HOP62 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1399380Inhibition of bovine brain tubulin assembly pretreated for 15 mins followed by GTP addition by spectrophotometric method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and preclinical evaluation of 5-methyl-N
AID613266Displacement of [3H]colchicine from biotin-labeled bovine brain tubulin at 5 uM after 2 hrs by liquid scintillation counter2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and biological evaluation of 1-(4'-Indolyl and 6'-Quinolinyl) indoles as a new class of potent anticancer agents.
AID691656Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as effect on platelet count at 30 mg/kg, ip qd after 21 days (Rvb = 1509 +/- 34 x 10'3 mm'-3)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1422353Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM after 1 hr liquid scintillation counting assay relative to control2018European journal of medicinal chemistry, Nov-05, Volume: 159Modified carbazoles destabilize microtubules and kill glioblastoma multiform cells.
AID1353659Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 50 nM after 20 hrs by propidium iodide staining based flow cytometry (Rvb = 66 +/- 1%)2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID1263274Cytotoxicity against human UACC62 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID403648Inhibition of tubulin polymerization2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID1236600Inhibition of pig microtubule polymerization after 30 mins by turbidimetric assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of diarylthiazole derivatives as antimitotic and antivascular agents with potent antitumor activity.
AID314012Antiproliferative activity against human SNB75 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID1514444Inhibition of tubulin (unknown origin) polymerization
AID1508153Induction of intrinsic apoptosis in human MCF7 cells assessed as effect on mitochondrial membrane depolarization by measuring mean fluorescence intensity at 2 uM after 18 hrs by DiOC6 staining-based FACS analysis (Rvb = 463 No_unit)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1351634Induction of apoptosis in human A431 cells assessed as increase in histone-associated DNA fragments in oligonucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID280075Antiproliferative activity against drug resistant ACHN cell line expressing MDR1 by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID1162819Induction of cell cycle arrest in human A549 cells assessed as accumulation at subG1 phase at 50 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 1.41%)2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID1064419Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1637525Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 60 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 17.56%)2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID685367Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID344538Inhibition of calf brain tubulin polymerization2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4.
AID1308608Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining at 120 mins in presence of NADPH regenerating system by HPLC method2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID474632Cell cycle arrest in human HeLa cells assessed as accumulation of cells in G0/1 phase at 0.02 uM after 24 hrs using propidium iodide by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1285332Induction of apoptosis in human HT-29 cells assessed as necrotic cells at 10 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb=0.82%)2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID1366859Antiproliferative activity against human A549 cells after 48 hrs by SRB cell proliferation assay2017Bioorganic & medicinal chemistry letters, 12-15, Volume: 27, Issue:24
Potential anti-proliferative agents from 1,4-benzoxazinone-quinazolin-4(3H)-one templates.
AID1709304Cytotoxicity against human SK-OV-3 cells over expressing MDR1-6/6 assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1310238Antivascular activity in human EAhy926 cells assessed as induction of retraction of cells to nodes at 100 nM after 16 hrs by light microscopic analysis2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID310083Inhibition of tubulin polymerization2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Conformationally restricted macrocyclic analogues of combretastatins.
AID265410Antiproliferative activity against human H460 cells2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID293335Antiproliferative activity against human HMEC1 cells2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID1586366Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 0.2 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 60 +/- 1%)2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4.
AID1191396Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTitre-Blue assay2015European journal of medicinal chemistry, Jan-27, Volume: 90Rapid synthesis of 4-arylchromenes from ortho-substituted alkynols: A versatile access to restricted isocombretastatin A-4 analogues as antitumor agents.
AID437545Anticancer activity against human HepG2 cells after 72 hrs2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines).
AID1726856Antiproliferative activity against human HCT-116 cells assessed as cell viability after 72 hrs by MTT assay2020European journal of medicinal chemistry, Feb-01, Volume: 187The discovery of novel indazole derivatives as tubulin colchicine site binding agents that displayed potent antitumor activity both in vitro and in vivo.
AID144204Antimicrobial activity against Neisseria gonorrhoeae1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID622207Inhibition of tubulin polymerization by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1402066Antiproliferative activity against human HeLa cells after 4 days by Coulter counter method2018European journal of medicinal chemistry, Jan-01, Volume: 1432-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.
AID444153Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID1068624Growth inhibition of human NCI-H322M cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID265413Antiproliferative activity against human MCF7 cells2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID1518328Disruption of microtubule network in human HCT116 cells assessed as microtubule disorganization at 50 nM for 18 hrs by FITC/DAPI staining-based confocal microscopic analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.
AID286487Antiproliferative effect against human CEM cells after 3 days2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID1466259Inhibition of pig brain tubulin polymerization at 10 uM by spectrophotometric analysis2017European journal of medicinal chemistry, Jul-07, Volume: 134Synthesis and biological evaluation of novel indole-pyrimidine hybrids bearing morpholine and thiomorpholine moieties.
AID221796Compound was evaluated for cytotoxicity against human A-549 non-small cell lung cancer cell line.1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Synthesis and evaluation of analogues of (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene as potential cytotoxic and antimitotic agents.
AID1064388Growth inhibition of human A498 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID611185Cell cycle arrest in human MCF7 cells assessed as accumulation at GO phase at 2 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 6.09%)2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Synthesis and biological evaluation of 4β-acrylamidopodophyllotoxin congeners as DNA damaging agents.
AID1667118Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological evaluation of novel pyrazolo[3,4-b]pyridines as cis-restricted combretastatin A-4 analogues.
AID1906186Inhibition of pig brain tubulin polymerization at 6 uM by spectrophotometer analysis
AID670886Antimitotic activity in human HeLa cells assessed as multipolar spindle formation at 3 nM after 6 hrs by DAPI staining-based immunofluorescence analysis2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
AID1276118Cytotoxicity against human T98G cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID281351Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1195289Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID1731562Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents.
AID1666250Inhibition of tubulin polymerization in human A549 cells assessed as fragmentation of microtubule network at 0.6 uM incubated for 18 hrs by Hoechst33342 staining based confocal microscopic analysis2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID685178Growth inhibition of human NCI-H226 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1206085Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay2015European journal of medicinal chemistry, Apr-13, Volume: 94Design, synthesis and biological evaluation of novel pyrazoline-containing derivatives as potential tubulin assembling inhibitors.
AID622424Cytotoxicity against human A498 cells after 48 hrs by sulforhodamine B assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1773143Cell cycle arrest in human A549 cells assessed as G2/M phase at 500 nM measured after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 6.08%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1164800Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Synthesis and biological evaluation of novel 3,4-diaryl-1,2,5-selenadiazol analogues of combretastatin A-4.
AID53777Cell growth inhibition against DLD-1 human colon cancer cells using MTS assay2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
AID1431172Displacement of [3H]colchicine from bovine brain tubulin at 1 uM measured after 10 mins by liquid scintillation counting method relative to control2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
AID607293Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetric analysis2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID1336761Inhibition of alpha-tubulin polymerization in human A549 cells assessed as disruption of microtubule organization at 50 nM after 48 hrs by FITC/DAPI staining based immunofluorescence microscopic assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID271659Inhibition of [3H]colchicine binding to tubulin at 1 uM2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents.
AID746662Cell cycle arrest in mouse NIH/3T3 cells assessed as accumulation at S phase at 0.05 uM after 24 hrs by propidium iodide staining-based FACS flow cytometric analysis (Rvb = 24.39%)2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Design, synthesis, cytotoxic evaluation and tubulin inhibitory activity of 4-aryl-5-(3,4,5-trimethoxyphenyl)-2-alkylthio-1H-imidazole derivatives.
AID657576Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Design, synthesis and biological evaluation of novel chalcone derivatives as antitubulin agents.
AID1709308Displacement of [3H]-colchicine from bovine brain tubulin at 1 uM after 10 mins by DEAE-cellulose filter method relative to control2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID455040Cytotoxicity against human A498 cells after 48 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID273084Antiproliferative activity against human PC3 cells after 72 hrs2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and structure-activity relationships of carbazole sulfonamides as a novel class of antimitotic agents against solid tumors.
AID737113Cytotoxicity against human Jurkat cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID567093Inhibition of tubulin polymerization by DAPI fluorescent assay2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues.
AID637197Inhibition of bovine brain tubulin polymerization preincubated for 10 mins measured after 20 mins2012Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3
Synthesis, biological evaluation, and molecular docking studies of cinnamic acyl 1,3,4-thiadiazole amide derivatives as novel antitubulin agents.
AID1294500Growth inhibition of human MDA-MB-435 cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID480728Induction of G1 phase arrest in Saccharomyces cerevisiae expressing TAP-tagged Cln1 assessed as down-regulation of Cln1 level at 450 uM after 3 hrs by Western blot analysis2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID1667117Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological evaluation of novel pyrazolo[3,4-b]pyridines as cis-restricted combretastatin A-4 analogues.
AID1647007Induction of mitochondrial membrane depolarization in human HepG2 cells at 0.1 uM measured after 24 hrs by JC1 staining based flow cytometry (Rvb = 5.96 %)2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID404191Displacement of [3H]colchicine from bovine brain tubulin at 1 uM2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Design, synthesis, and biological evaluation of thiophene analogues of chalcones.
AID1308562Resistance index, ratio of IC50 for human MCF7/DX cells to IC50 for human MCF7 cells2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1294479Growth inhibition of human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID273363Antiproliferative activity against human HT29 cell line by methylene blue dye assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
AID1917043Phototoxicity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 24 hrs followed by LED illumination by MTT assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Recent advances in combretastatin A-4 codrugs for cancer therapy.
AID1263284Cytotoxicity against human UO31 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1336759Inhibition of porcine brain tubulin polymerization at 3 uM in presence of GTP by fluorescence assay relative to control2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1647015Antimigratory activity against human HepG2 cells assessed as inhibition of cell migration at 0.1 uM measured after 12 hrs by scratch wound healing assay2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1070873Resistance ratio of IC50 for human HeLa cells expressing beta3-tubulin containing alanine residue at 227 to IC50 for human HeLa cells2013Journal of natural products, Oct-25, Volume: 76, Issue:10
The bat flower: a source of microtubule-destabilizing and -stabilizing compounds with synergistic antiproliferative actions.
AID1310195Cell cycle arrest in combretastatin A-4 resistant human HT-29 cells assessed as accumulation at G1 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 68.1 +/- 0.3%)2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID382329Cytotoxicity against human K562 cells after 5 days by MTT assay2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin.
AID1234869Aqueous solubility of the compound in phosphate buffer at pH 7 after 48 hrs by spectrophotometric analysis2015European journal of medicinal chemistry, Jul-15, Volume: 100Exploring the size adaptability of the B ring binding zone of the colchicine site of tubulin with para-nitrogen substituted isocombretastatins.
AID644540Cytotoxicity against human SKOV3 cells after 48 hrs by MTS assay2012Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5
Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A-1.
AID642056Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 48 hrs by MTT assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1162825Induction of cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 50 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 6.15%)2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID778975Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetric analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and biological evaluation of indole-based, anti-cancer agents inspired by the vascular disrupting agent 2-(3'-hydroxy-4'-methoxyphenyl)-3-(3″,4″,5″-trimethoxybenzoyl)-6-methoxyindole (OXi8006).
AID1700953Inhibition of porcine brain tubulin polymerization measured every 60 sec for 60 mins in presence of GTP by fluorescence assay
AID1518076Inhibition of tubulin polymerization in mouse B16F10 cells assessed as disruption of microtubule network at 200 nM incubated for 6 hrs by DAPI staining based confocal microscopy2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID657610Inhibition of bovine tubulin polymerization after 20 mins by spectrophotometry2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Synthesis, biological evaluation, and molecular docking studies of 2,6-dinitro-4-(trifluoromethyl)phenoxysalicylaldoxime derivatives as novel antitubulin agents.
AID1600472Cytotoxicity against human BJ cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID691732Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as change in spleen weight at 50 mg/kg, ip qd after 21 days relative to vehicle-treated control2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1647032Toxicity in ICR mouse xenografted with mouse H22 cells assessed as effect on spleen damage or inflammation at 30 mg/kg, iv administered once daily for 21 consecutive days measured after 21 days by hematoxylin-eosin staining based fluorescence microscopy2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID455037Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID1189964Toxicity in C57BL/6 mouse assessed as interphase microtubule de-stabilizing activity by measuring influx of rhodamine in to heart at 1 mg/kg, iv co-administered with rhodamine B by fluorimetry2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Synthesis and biological evaluation of furanoallocolchicinoids.
AID228620Percent inhibition of 5 uM of [3H]colchicine binding to 1 uM of tubulin by 5 uM of compound after a 10 min incubation at 37 degrees C2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
One-pot synthesis of benzo[b]furan and indole inhibitors of tubulin polymerization.
AID1689077Induction of apoptosis in human HeLa cells assessed as mitochondrial membrane potential dissipation at 0.5 uM incubated for 24 hrs by JC-1 staining based flow cytometry (Rvb = 6.6%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1778189Antiproliferative activity against human HT29 cells assessed as cell growth inhibition after 48 hrs by MTT assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines.
AID1205511Antiproliferative activity against human Jurkat cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.
AID1736450Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1351591Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID79922Cytotoxic activity against H116 cell line2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
A new family of quinoline and quinoxaline analogues of combretastatins.
AID1068632Growth inhibition of human SR cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1773178Induction of apoptosis in human U-251 cells assessed as increase in necrotic cells at 200 nM measured after 24 hrs by PI/FITC analysis (Rvb = 0.301%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1317577Growth inhibition of human EAhy926 cells measured after 72 hrs by MTT assay2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1308605Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining at 30 mins in presence of NADPH regenerating system by HPLC method2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1518330Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.
AID391279Cytotoxicity against human HT29 cells by sulforhodamine B test2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Novel A-ring and B-ring modified combretastatin A-4 (CA-4) analogues endowed with interesting cytotoxic activity.
AID502712Growth inhibition of human EKVX cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID293349Cell cycle arrest in HMEC1 cells assessed as accumulation at S phase at 25 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID1068638Microtubule destabilizing activity in sea urchin free-swimming blastula assessed as embryo spinning treated at 9 to 10 hrs post-fertilization measured after 0.15 to 15 hrs2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID642528Growth inhibition of human KB cells after 72 hrs by methylene blue assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. Part 2. The impact of bridging groups at position C-2.
AID1427227Induction of microtubule disruption in human OVCAR3 cells assessed as cytoskeleton contraction at 10 nM after 24 hrs by Alexa Fluor 647/DAPI staining based fluorescence microscopic method2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Combretastatin A4-β-Galactosyl Conjugates for Ovarian Cancer Prodrug Monotherapy.
AID1196879Metabolic stability in human liver microsomes assessed as peak area after 60 mins by LC-UV analysis2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID1068599Growth inhibition of human OVCAR3 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID569526Reduction of cyclin A expression in human MCF7 cells at 5 uM after 24 hrs by Western blotting2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents.
AID1741598Inhibition of pig brain tubulin polymerization measured at 1 min interval for 20 mins by spectrophotometric method2020European journal of medicinal chemistry, Oct-15, Volume: 204Synthesis, and biological evaluation of 3,6-diaryl-[1,2,4]triazolo[4,3-a]pyridine analogues as new potent tubulin polymerization inhibitors.
AID1458856Half life in Sprague-Dawley rat by UV-based HPLC-MS/MS analysis2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID265450Cell cycle arrest in NCI-H460 cells by accumulation at G2/M phase cell at 160 nM post 24 hrs treatment and 48 hrs recovery2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID1411799Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID665820Cell cycle arrest in human A549 cells assessed as cell accumulation at G2/M phase at 2 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 23.75%)2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID1647004Induction of apoptosis in human HepG2 cells assessed as necrotic cells at 0.1 uM measured after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.02 %)2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1726858Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay2020European journal of medicinal chemistry, Feb-01, Volume: 187The discovery of novel indazole derivatives as tubulin colchicine site binding agents that displayed potent antitumor activity both in vitro and in vivo.
AID735018Growth inhibition of human HCT116 cells after 72 hrs by Victor microtiter plate fluorimeter analysis2013European journal of medicinal chemistry, Apr, Volume: 62Design, synthesis and anticancer properties of 5-arylbenzoxepins as conformationally restricted isocombretastatin A-4 analogs.
AID152759Concentration required for 50% inhibition of P388 murine leukemia cell growth in MTT assay2001Bioorganic & medicinal chemistry letters, Jan-08, Volume: 11, Issue:1
Antimitotic and cell growth inhibitory properties of combretastatin A-4-like ethers.
AID1195293Resistance ratio of IC50 for human HeLa cells overexpressing wild type beta3 tubulin to IC50 for human HeLa cells2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID1737795Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID1757284Antiproliferative activity against VCR resistant human K562/VCR cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID286486Antiproliferative effect against human Molt4/C8 cells after 3 days2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID502747Growth inhibition of human UO31 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1733032Inhibition of tubulin (unknown origin) polymerization at 10 uM measured every 1 min over 20 mins by fluorescence assay relative to control2021Bioorganic & medicinal chemistry letters, 04-15, Volume: 38Synthesis, biological evaluation, and structure-activity relationships of new tubulin polymerization inhibitors based on 5-amino-1,2,4-triazole scaffold.
AID1466243Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Synthesis and biological evaluation of novel indole-pyrimidine hybrids bearing morpholine and thiomorpholine moieties.
AID657876Growth inhibition of mouse P388 cells after 48 hrs by Z1 Beckman/Coulter particle counter analysis2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID515461Cytotoxicity against human 518A2 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
4-(3-Halo/amino-4,5-dimethoxyphenyl)-5-aryloxazoles and -N-methylimidazoles that are cytotoxic against combretastatin A resistant tumor cells and vascular disrupting in a cisplatin resistant germ cell tumor model.
AID1351639Induction of apoptosis in human SKOV3 cells assessed as increase in histone-associated DNA fragments in oligonucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1742934Antiproliferative activity against human HCT8 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors.
AID1351625Induction of apoptosis in human HeLa cells after 24 hrs by FITC Annexin V/propidium iodide staining-based FACScan flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID277283Inhibition of tubulin polymerization2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Highly potent triazole-based tubulin polymerization inhibitors.
AID629596Antiproliferative activity against human MOLT4 cells after 2 days by coulter counter analysis2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID1348294Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured after 20 mins by spectrophotometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Targeting tubulin polymerization by novel 7-aryl-pyrroloquinolinones: Synthesis, biological activity and SARs.
AID9208Cytotoxic concentration required to inhibit 50% cell growth in A-549 lung carcinoma cell lines1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization.
AID1068618Growth inhibition of human HCT15 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID622527Drug metabolism in human microsomes assessed as metabolite formation2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1637516Antiproliferative activity against human A549 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID1572255Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.
AID1906219Induction of cell cycle arrest in human HeLa cells assessed as >4N cells at 3 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis relative to control
AID281364Apoptosis in strongly adherent human ECV304 cells at 10 nM assessed as DNA fragmentation2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID317731Antiviral activity against HIV2ROD infected in human MT4 cells2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID1730565Antiproliferative activity against human HT-1080 cells assessed as reduction in cell viability measured after 48 hrs by sulforhodamine B assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID1517174Inhibition of [3H] colchicine binding to bovine brain tubulin incubated for 30 mins by scintillation proximity assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Potent combretastatin A-4 analogs containing 1,2,4-triazole: Synthesis, antiproliferative, anti-tubulin activity, and docking study.
AID619857Antiproliferative activity against ER-independent human MDA-MB-231 cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID1294466Growth inhibition of human K562 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID605708Antiproliferative activity against human HT-29 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID480726Cell cycle arrest in Saccharomyces cerevisiae BY4741 assessed as accumulation of cells at G1 phase at 450 uM after 3 hrs by FACS analysis2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID1517353Antiproliferative activity against human HL60 cells incubated for 48 hrs by MTS assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Design and synthesis of (2-(phenylamino)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone analogues as potent anti-tubulin polymerization agents.
AID461787Inhibition of tubulin polymerization by turbidimetric assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors.
AID758698Cytotoxicity against human CA46 cells2013European journal of medicinal chemistry, Jul, Volume: 652-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action.
AID1351593Cytotoxicity against human A549 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1408381Cell cycle arrest in human K562 cells assessed as accumulation at G1 phase at 0.005 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 41.08%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID348404Antiproliferative activity against human CEM cells2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID1906213Induction of cell cycle arrest in human HeLa cells assessed as 4N cells at 3 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 17.1%)
AID293347Cell cycle arrest in HMEC1 cells assessed as accumulation at S phase at 6.25 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID735009Inhibition of tubulin polymerization (unknown origin)2013European journal of medicinal chemistry, Apr, Volume: 62Design, synthesis and anticancer properties of 5-arylbenzoxepins as conformationally restricted isocombretastatin A-4 analogs.
AID1205518Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 20 mins by scintillation counting analysis2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.
AID630731Inhibition of LPS-induced TNFalpha production in human PBMC preincubated 1 hr prior to LPS stimulation measured after 18 to 20 hrs by ELISA2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
1,1-Diarylalkenes as anticancer agents: dual inhibitors of tubulin polymerization and phosphodiesterase 4.
AID1586362Antiproliferative activity against human HL60 cells by MTT assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4.
AID1206088Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetric analysis2015European journal of medicinal chemistry, Apr-13, Volume: 94Design, synthesis and biological evaluation of novel pyrazoline-containing derivatives as potential tubulin assembling inhibitors.
AID1158426Inhibition of pig brain tubulin polymerization by spectrophotometric analysis2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
AID1263280Cytotoxicity against human 786-0 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1233597Induction of cell cycle arrest in human M21 cells assessed as cells accumulation at S phase at 10 nM after 24 hrs by flow cytometry (Rvb = 22.2%)2015European journal of medicinal chemistry, Jul-15, Volume: 100Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model.
AID685361Growth inhibition of human SN12C cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID479717Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Synthesis and antitumor activity of 1,5-disubstituted 1,2,4-triazoles as cis-restricted combretastatin analogues.
AID1409121Resistance index, ratio of IC50 for human SKOV3-MDR1-M6/6 cells to IC50 for human SKOV3 cells2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.
AID1886235Inhibition of [3H]Colchicine binding to tubulin (unknown origin) at 5 uM measured after 2 hrs by scintillation counting method relative to control2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1550346Cell cycle arrest in human SGC7901 cells assessed as increase in cell population at G2/M phase at 2 fold IC50 concentration measured after 12 hrs by propidium iodide staining based FACScan flow cytometry2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and bioevaluation of diarylpyrazoles as antiproliferative agents.
AID1338078Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of cyclic-indole derivatives as anti-tumor agents via the inhibition of tubulin polymerization.
AID1628249Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 50 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 49%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID675715Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 10 mins2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones and analogues: synthesis, cytotoxic activity, and study of the mechanism of action.
AID685199Growth inhibition of human SK-MEL-2 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID611187Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 2 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 6.99%)2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Synthesis and biological evaluation of 4β-acrylamidopodophyllotoxin congeners as DNA damaging agents.
AID771195Cell cycle arrest in human HT-29 cells assessed as accumulation at G2/M phase at 25 nM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 7.37%)2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID1586364Antiproliferative activity against HEK293 cells by MTT assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4.
AID1906201Induction of cell cycle arrest in human HeLa cells assessed as 2N cells at 3 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 41.7%)
AID659049Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 3 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 16.2 %)2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
AID1408382Cell cycle arrest in human K562 cells assessed as accumulation at S phase at 0.005 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 49.41%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1402069Inhibition of bovine brain tubulin polymerization in presence of GTP by spectrophotometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 1432-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.
AID657609Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Synthesis, biological evaluation, and molecular docking studies of 2,6-dinitro-4-(trifluoromethyl)phenoxysalicylaldoxime derivatives as novel antitubulin agents.
AID663555Inhibition of tubulin polymerization2012ACS medicinal chemistry letters, Jan-12, Volume: 3, Issue:1
Steroidomimetic Tetrahydroisoquinolines for the Design of New Microtubule Disruptors.
AID314017Antiproliferative activity against human CAKI-1 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID1064384Growth inhibition of human SN12C cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1068609Growth inhibition of human U251 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID449230Selectivity index, ratio of IC50 for rat A10 cells to IC50 for human MCF7 cells2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
AID685164Cytotoxicity against human THP1 cells after 48 hrs assessed as inhibition of cell growth at 10 uM after 48 hrs by SRB assay relative to control2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID273358Inhibition of [3H]colchicine binding to tubulin at 5 uM2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
AID1317601Cell cycle arrest in human HepG2 cells assessed as >4N DNA content at growth inhibitory IC50 measured after 24 hrs by propidium iodide-staining based FACS analysis relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1535571Antiproliferative activity against human A549 cells after 24 hrs by MTT assay2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Synthesis, biological evaluation and molecular docking of benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives as novel tubulin polymerization inhibitors.
AID666751Inhibition of tubulin polymerization preincubated for 45 mins before GTP addition measured after 2 hrs by DAPI-based fluorescenct assay2012European journal of medicinal chemistry, Aug, Volume: 54In vitro and in vivo biological evaluation of new 4,5-disubstituted 1,2,3-triazoles as cis-constrained analogs of combretastatin A4.
AID1757287Aqueous solubility of the compound in aqueous HCl at pH 2 by HPLC-UV analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID607538Metabolic stability in human liver microsomes assessed as phase 2 transformation after 60 mins by LC-ESI-MS and LC-UV analysis2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues.
AID674223Displacement of [3H]colchicine from bovine brain tubulin at 5 uM2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Discovery and optimization of a series of 2-aryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazoles as novel anticancer agents.
AID384968Cell cycle arrest in human NCI-H460 cells assessed as S phase accumulation after 24 hrs by flow cytometry2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
Synthesis and biological activity of fluorinated combretastatin analogues.
AID52490Cell growth inhibition against colo 205 human colon cancer cells using tetrazolium dye reduction (MTS) assay2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
AID1059051Cell cycle arrest in mouse NIH/3T3 cells assessed as accumulation at G0/G1 phase at 0.05 uM after 24 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 39.91%)2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis, cytotoxic evaluation and molecular docking study of 2-alkylthio-4-(2,3,4-trimethoxyphenyl)-5-aryl-thiazoles as tubulin polymerization inhibitors.
AID1267534Antiproliferative activity against human MES-SA cells after 72 hrs by resazurin assay2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Synthesis and biological evaluation of thiophene and benzo[b]thiophene analogs of combretastatin A-4 and isocombretastatin A-4: A comparison between the linkage positions of the 3,4,5-trimethoxystyrene unit.
AID629598Antiproliferative activity against human HeLa cells after 2 days by coulter counter analysis2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID761815Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 10 mins relative to control2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Correlation of hydrogen-bonding propensity and anticancer profile of tetrazole-tethered combretastatin analogues.
AID397291Cytotoxicity against human H1299 cells after 72 hrs2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Isocombretastatins a versus combretastatins a: the forgotten isoCA-4 isomer as a highly promising cytotoxic and antitubulin agent.
AID461024Displacement of [3H]colchicine from tubulin at 50 uM by turbidimetry2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
A boronic acid chalcone analog of combretastatin A-4 as a potent anti-proliferation agent.
AID452624Cell cycle arrest in human K562 cells assessed as accumulation at G2/M phase at 10 uL after overnight incubation by propidium iodide staining-based flow cytometry2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID1431173Inhibition of VEGFR-2 in human U251 cells assessed as reduction in VEGF induced phosphorylation preincubated for 60 mins followed by VEGF addition measured after 10 mins by ELISA method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
AID1366860Antiproliferative activity against human HeLa cells after 48 hrs by SRB cell proliferation assay2017Bioorganic & medicinal chemistry letters, 12-15, Volume: 27, Issue:24
Potential anti-proliferative agents from 1,4-benzoxazinone-quinazolin-4(3H)-one templates.
AID299202Antiproliferative activity against human CEM cells2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity relationships.
AID1666252Induction of cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 0.6 uM incubated for 48 hrs by PI staining based flow cytometric analysis (Rvb = 17.03%)2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID658260Cytotoxicity against human H1299 cells after 72 hrs using resazurin dye by microtiter plate fluorimeter analysis2012European journal of medicinal chemistry, Jun, Volume: 52Conformationnally restricted naphthalene derivatives type isocombretastatin A-4 and isoerianin analogues: synthesis, cytotoxicity and antitubulin activity.
AID1586361Antiproliferative activity against human A549 cells by MTT assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4.
AID247220Growth inhibition against human pharynx FADU cell line2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID746663Cell cycle arrest in mouse NIH/3T3 cells assessed as accumulation at G2/M phase at 0.05 uM after 24 hrs by propidium iodide staining-based FACS flow cytometric analysis (Rvb = 35.70%)2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Design, synthesis, cytotoxic evaluation and tubulin inhibitory activity of 4-aryl-5-(3,4,5-trimethoxyphenyl)-2-alkylthio-1H-imidazole derivatives.
AID1367973Antiproliferative activity against human A2780 cells by MTT assay
AID594373Inhibition of tubulin polymerization assessed as protein assembly after 20 mins by turbidimetric analysis2011Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
Synthesis of novel antimitotic agents based on 2-amino-3-aroyl-5-(hetero)arylethynyl thiophene derivatives.
AID1288165Antiproliferative activity against cisplatin resistant human A2780 cells assessed as cell viability after 48 hrs by MTT assay2016European journal of medicinal chemistry, May-23, Volume: 114Synthesis and biological evaluation of quinoline analogues of flavones as potential anticancer agents and tubulin polymerization inhibitors.
AID1887832Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR.
AID1064402Growth inhibition of human M14 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID293341Cell cycle arrest in HMEC1 cells assessed as accumulation at G1 phase at 100 nM after 24 hrs by flow cytometry assay relative to contro2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID1294473Growth inhibition of human HCT15 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID306480Growth inhibition of human HT29 cells2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID595724Inhibition of lamb tubulin assembly at 3 uM after 18 hrs by fluorimetry2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Synthesis and biological evaluation of 4-arylcoumarin analogues of combretastatins. Part 2.
AID348406Displacement of [3H]colchicine from bovine brain tubulin at 1 uM2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID515465Cytotoxicity against human multidrug-resistant MCF7/Topo cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
4-(3-Halo/amino-4,5-dimethoxyphenyl)-5-aryloxazoles and -N-methylimidazoles that are cytotoxic against combretastatin A resistant tumor cells and vascular disrupting in a cisplatin resistant germ cell tumor model.
AID691631Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as mortality at 30 mg/kg, ip qd after 21 days2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID427179Antiproliferative activity against human HeLa cells after 2 days by coulter counter method2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization.
AID299204Antiproliferative activity against human Bel7402 cells2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity relationships.
AID95844In vitro cytotoxic activity against human KB cell line of epidermoid carcinoma2004Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents.
AID281366Apoptosis in strongly adherent human ECV304 cells at 1000 nM assessed as DNA fragmentation2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1179656Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design, synthesis and biological evaluation of (E)-3-(3,4-dihydroxyphenyl)acrylylpiperazine derivatives as a new class of tubulin polymerization inhibitors.
AID102519In vitro cytotoxic activity tested against human lung cancer (H-522) cell line2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.
AID670883Antimitotic activity in human HeLa cells assessed as microtubule network damage at interphase at 1 nM after 6 hrs by DAPI staining-based immunofluorescence analysis2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
AID1064409Growth inhibition of human SF295 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1413261Inhibition of porcine brain tubulin polymerization measured for 15 mins by spectrophotometric method2018MedChemComm, May-01, Volume: 9, Issue:5
Synthesis and biological evaluation of new 3-amino-2-azetidinone derivatives as anti-colorectal cancer agents.
AID769831Inhibition of p-gp overexpressed in human SKOV3/M6-6 isogenic cells after 48 hrs by sulforhodamine B assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.
AID1667119Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological evaluation of novel pyrazolo[3,4-b]pyridines as cis-restricted combretastatin A-4 analogues.
AID1336749Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID340147Growth inhibition of human H460 cells after 72 hrs by methylene blue dye assay2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.
AID247673Cytotoxicity against SH-SY5Y human neuroblastoma cell line was determined2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Synthesis and cytotoxic evaluation of combretafurazans.
AID665697Cytotoxicity against human ACHN cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID247803Concentration required to inhibit murine leukemia L1210 cell line proliferation2005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
AID455992Inhibition of bovine tubulin polymerization2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of tubulin polymerization.
AID427176Antiproliferative activity against mouse FM3A cells after 2 days by coulter counter method2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization.
AID1736446Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1327864Inhibition of alpha-tubulin polymerization in human A549 cells assessed as destruction of tubulin network at 2 times IC50 after 12 hrs by DAPI/FITC-dual staining based fluorescence microscopic analysis
AID474642Induction of apoptosis in human HeLa cells assessed as cells containing hypodiploid DNA at 0.2 uM after 24 hrs by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1352574Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Synthesis and biological evaluation of 4,6-diphenyl-2-(1H-pyrrol-1-yl)nicotinonitrile analogues of crolibulin and combretastatin A-4.
AID1421775Selectivity index, ratio of IC50 for mouse L929 cells to IC50 for human HT1080 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158Conformation impacts on the bioactivities of SMART analogues.
AID1458855Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining after 150 mins in presence of NADPH by UV-based HPLC-MS/MS analysis2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1729877Inhibition of bovine brain tubulin polymerization incubated for 30 mins by turbidimetric assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Methylsulfanylpyridine based diheteroaryl isocombretastatin analogs as potent anti-proliferative agents.
AID1231332Cytotoxicity against human NCM460 cells assessed as reduction in cell proliferation after 48 hrs by WST-1 assay2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4.
AID93839Compound was tested for cell arrest at G2/M phase at 50 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID1174854Cytotoxicity against human A549 cells after 72 hrs by MTT assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin.
AID1727329Inhibition of tubulin polymerization (unknown origin) assessed as microtubule assembly preincubated for 30 mins by microplate based assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation.
AID1294482Growth inhibition of human A498 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID617015Relative resistance ratio of IC50 for beta3-tubulin overexpressing human HeLa cells to IC50 for human HeLa cells2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID629680Cytotoxicity against human HT-29 cells2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID150354Evaluated for cell growth inhibition of the mouse leukemia P388 cells in 10% horse serum/Fisher media2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.
AID1399375Antiproliferative activity against human SKOV3-MDR1-M6/6 cells after 72 hrs by sulforhodamine B assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and preclinical evaluation of 5-methyl-N
AID1612615Antiproliferative activity against human H22 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID273279Antiproliferative activity against human CEM cells2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.
AID349338Cytotoxicity against human HeLa cells after 72 hrs by XTT assay2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Naphthylphenstatins as tubulin ligands: synthesis and biological evaluation.
AID1863088Antiproliferative activity against human KYSE-450 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway.
AID569518Cell cycle arrest in human MCF7 cells assessed as accumulation at G0 phase at 5 uM after 24 hrs using propidium iodide staining by flow cytometry relative to control2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents.
AID319825Cytotoxicity against human MDA-MB-231 cells2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and antitumor activity of benzils related to combretastatin A-4.
AID685364Growth inhibition of human PC3 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1612623Antiproliferative activity against human VCR-resistant K562/VCR cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID502727Growth inhibition of human SNB75 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1352572Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Synthesis and biological evaluation of 4,6-diphenyl-2-(1H-pyrrol-1-yl)nicotinonitrile analogues of crolibulin and combretastatin A-4.
AID1057113Drug metabolism in PBS at pH 7.4 assessed as product-2 level after 6.5 hrs by HPLC analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID273080Antiproliferative activity against human Molt3 cells after 72 hrs2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and structure-activity relationships of carbazole sulfonamides as a novel class of antimitotic agents against solid tumors.
AID1400377Antiproliferative activity against CYP1A1 expressing human MCF7 cells after 72 hrs by SRB assay2018Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
4-(3-Alkyl-2-oxoimidazolidin-1-yl)-N-phenylbenzenesulfonamides as new antimitotic prodrugs activated by cytochrome P450 1A1 in breast cancer cells.
AID1917037Cytotoxicity against human A549 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Recent advances in combretastatin A-4 codrugs for cancer therapy.
AID1317594Antiproliferative activity against human HaCaT cells measured after 72 hrs by MTT assay2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID280068Inhibition of proliferation of human H460 cells2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID1647031Toxicity in ICR mouse xenografted with mouse H22 cells assessed as effect on lung damage or inflammation at 30 mg/kg, iv administered once daily for 21 consecutive days measured after 21 days by hematoxylin-eosin staining based fluorescence microscopy2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID106321Cell growth inhibition against MES-SA human uterine cancer cells using MTS assay2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
AID1070878Inhibition of purified pig brain tubulin polymerization at 2 to 3 uM by spectrophotometry2013Journal of natural products, Oct-25, Volume: 76, Issue:10
The bat flower: a source of microtubule-destabilizing and -stabilizing compounds with synergistic antiproliferative actions.
AID214002Concentration required to inhibit the extent of glutamate-dependent tubulin polymerization by 50% at 37 degrees C(1.0 mM MgCl2)1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions.
AID449214Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
AID1351636Induction of apoptosis in human HeLa cells assessed as increase in histone-associated DNA fragments in oligonucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1399379Resistance index, ratio of IC50 for human HeLa cells to IC50 for human wild-type Hela-beta3 cells2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and preclinical evaluation of 5-methyl-N
AID619858Antiproliferative activity against ER expressing human MCF7 cells assessed as cell death at 10 uM after 72 hrs by MTT assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID657607Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Synthesis, biological evaluation, and molecular docking studies of 2,6-dinitro-4-(trifluoromethyl)phenoxysalicylaldoxime derivatives as novel antitubulin agents.
AID735512Inhibition of bovine brain tubulin polymerization preincubated for 15 mins by turbidimetric analysis2013European journal of medicinal chemistry, Apr, Volume: 62(E)-4-aryl-4-oxo-2-butenoic acid amides, chalcone-aroylacrylic acid chimeras: design, antiproliferative activity and inhibition of tubulin polymerization.
AID539833Inhibition of bovine tubulin polymerization in cell-free system2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Design, synthesis, and biological evaluation of novel N-γ-carboline arylsulfonamides as anticancer agents.
AID1533703Antiangiogenic activity in Leghorn chicken embryo chorioallantoic membrane assessed as effect on blood vessel length at 2.5 nmol after 6 hrs by light microscopic analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163New naphthopyran analogues of LY290181 as potential tumor vascular-disrupting agents.
AID1600471Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 72 hrs by MTS assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1064423Growth inhibition of human HOP92 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1351594Cytotoxicity against human SKOV3 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1462292Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis of different heterocycles-linked chalcone conjugates as cytotoxic agents and tubulin polymerization inhibitors.
AID1435094Induction of cytoplasmic microtubule network disassembly in human A549 cells at 0.05 uM after 1 hr by confocal fluorescence microscopic method relative to control2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1064406Growth inhibition of human SNB75 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID502719Growth inhibition of human HCT116 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1126006Cell cycle arrest in human HeLa cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 61.60%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1865672Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.
AID442971Cytotoxicity against HUVEC after 72 hrs by crystal violet staining2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Vascular disrupting activity of tubulin-binding 1,5-diaryl-1H-imidazoles.
AID474628Cytotoxicity against human T24 cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1276121Cytotoxicity against human GBM10 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1351603Cell cycle arrest in human HaCaT cells assessed as accumulation of cells at G2/M phase at 0.1 to 1 uM after 24 hrs by propidium iodide staining-based FACS analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID461023Inhibition of tubulin polymerization by turbidimetry2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
A boronic acid chalcone analog of combretastatin A-4 as a potent anti-proliferation agent.
AID629601Displacement of [3H]colchicine from bovine brain tubulin at 5 uM by DEAE-cellulose filter method2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID697458Antitumor activity against human HT1080 cells xenografted in chicken chorioallantoic membrane assessed as inhibition of tumor growth at 1 ug per egg, iv administered on day 11 measured on day 17 by CAM assay2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Synthesis, biological evaluation, and structure-activity relationships of novel substituted N-phenyl ureidobenzenesulfonate derivatives blocking cell cycle progression in S-phase and inducing DNA double-strand breaks.
AID1458824Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1646994Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1064417Growth inhibition of human COLO205 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1534368Inhibition of [3H]colchicine binding to biotinylated porcine tubulin at 1 uM after 2 hrs by scintillation proximity assay relative to control2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
AID685362Growth inhibition of human TK10 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1575816Cytotoxicity against human DU145 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay2019MedChemComm, Aug-01, Volume: 10, Issue:8
Synthesis and biological evaluation of structurally diverse α-conformationally restricted chalcones and related analogues.
AID587609Displacement of [3H]colchicine from tubulin at 5 uM for 10 mins2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Antitumor agents. 284. New desmosdumotin B analogues with bicyclic B-ring as cytotoxic and antitubulin agents.
AID1183660Growth inhibition of human MCF7 cells after 72 hrs by MTT assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID685363Growth inhibition of human UO31 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID214546Concentration required to inhibit polymerization of tubulin2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.
AID1435068Cell cycle arrest in human HT29-D4 cells assessed as accumulation at G1 phase at 0.5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 24.8 +/- 3.1%)2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1351621Inhibition of tubulin polymerization in human HaCaT cells assessed as micronuclei formation at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1860528Inhibition of tubulin polymerization (unknown origin) by fluorescence based analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC.
AID251087Percentage of CFU-GEMM inhibition value after 14 days for bone marrow cells treated with compound at IC902005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Heterocyclic and phenyl double-bond-locked combretastatin analogues possessing potent apoptosis-inducing activity in HL60 and in MDR cell lines.
AID455032Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID1628257Inhibition of cell migration of human MDA-MB-231 cells at 150 nM by wound closure assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID1890475Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells in G1 phase at 10 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 74.44 %)2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
AID269724Cell cycle arrest in SHSY5Y cells by accumulation at S phase after 12 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID344539Cytotoxicity against human NCI-H460 cells after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Design, synthesis, biochemical, and biological evaluation of nitrogen-containing trifluoro structural modifications of combretastatin A-4.
AID1336764Induction of apoptosis in human A549 cells assessed as nuclei condensation at 50 nM after 48 hrs by Hoechst 33258 staining based fluorescence microscopic analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID341685Inhibition of tubulin polymerization2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Asymmetric synthesis of 2,3-dihydro-2-arylquinazolin-4-ones: methodology and application to a potent fluorescent tubulin inhibitor with anticancer activity.
AID1600488Effect on DNA synthesis in human CCRF-CEM cells assessed as DNA synthesis level at 5 times IC50 incubated for 24 hrs by propidium iodide staining-based BrdU incorporation assay (Rvb = 52.13%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID665818Cell cycle arrest in human A549 cells assessed as cell accumulation at S phase at 2 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 5.01%)2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID1706475Antiproliferative activity against human HeLa cells assessed as reduction in cell growth after 48 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Development of triazolothiadiazine derivatives as highly potent tubulin polymerization inhibitors: Structure-activity relationship, in vitro and in vivo study.
AID1508481Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, antiproliferative, anti-tubulin activity, and docking study of new 1,2,4-triazoles as potential combretastatin analogues.
AID512242Cytotoxicity against human A375 cells at 4 uM after 24 hrs by MTT assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis and biological evaluation of 3,5-diaryl-isoxazoline/isoxazole-pyrrolobenzodiazepine conjugates as potential anticancer agents.
AID1778187Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines.
AID1901290Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2022European journal of medicinal chemistry, Feb-15, Volume: 230Synthesis and biological evaluation of novel hybrids of phenylsulfonyl furoxan and phenstatin derivatives as potent anti-tumor agents.
AID1730587Inhibition of EBI binding to colchicine-binding site of beta-tubulin in human M21 cells at 100 to 1000 times IC50 preincubated for 2 hrs followed by EBI addition and measured after 1.5 hrs by Western blot analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID1771455Antiproliferative activity against human U-937 cells assessed as cell growth inhibition after 72 hrs by CCK8 assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1860524Antiproliferative activity against human HN-6 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC.
AID1689023Induction of microtubule depolymerization in human MCF7 cells at 10 nM after 16 hrs by immunofluorescence staining based confocal microscopic analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells.
AID1541866Antiproliferative activity against human KB cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
AID1882979Induction of cell cycle arrest in human MDA-MB-231 cells assessed as decrease in G1 phase cells at 10 uM incubated for 24 hrs by PI staining based flow cytometric analysis (Rvb = 74.44%)2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and evaluation of a novel series of mono-indolylbenzoquinones derivatives for the potential treatment of breast cancer.
AID1324087Cytotoxicity against human CCRF-CEM cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1635304Cytotoxicity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID404584Cytotoxicity against human HT29 cells after 72 hrs by XTT method2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Diarylmethyloxime and hydrazone derivatives with 5-indolyl moieties as potent inhibitors of tubulin polymerization.
AID1278682Displacement of [3H]colchicine from bovine brain tubulin at 1 uM after 10 mins by scintillation counting analysis2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID330407Cytotoxicity against human BXPC3 cells after 48 hrs by SRB assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID1231328Anticancer activity against human MV4-11 cells assessed as reduction in cell proliferation after 48 hrs by WST-1 assay2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4.
AID1422354Inhibition of [3H]colchicine binding to bovine brain tubulin at 1 uM after 1 hr liquid scintillation counting assay relative to control2018European journal of medicinal chemistry, Nov-05, Volume: 159Modified carbazoles destabilize microtubules and kill glioblastoma multiform cells.
AID691731Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as change in liver weight at 50 mg/kg, ip qd after 21 days relative to vehicle-treated control2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1288172Cell cycle arrest in cisplatin resistant human A2780 cells assessed as accumulation at G2/M phase at 3 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 19.63%)2016European journal of medicinal chemistry, May-23, Volume: 114Synthesis and biological evaluation of quinoline analogues of flavones as potential anticancer agents and tubulin polymerization inhibitors.
AID662346Antiproliferative activity in human SW620 cells assessed as cell viability after 72 hrs by MTT assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID326225Inhibition of rat brain tubulin polymerization2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Cytotoxic simplified tubulysin analogues.
AID716408Induction of microtubule depolymerization in human SKv-a cells at 10 '-6 M by confocal microscopy2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4.
AID1508159Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 2 uM after 48 hrs by flow cytometric analysis (Rvb = 8.1%)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID281506Displacement of [3H]colchine from tubulin at 1 uM2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Arylthioindoles, potent inhibitors of tubulin polymerization.
AID1317602Cell cycle arrest in human HepG2 cells assessed as accumulation in G2/M phase at growth inhibitory IC50 measured after 48 hrs by propidium iodide-staining based FACS analysis2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1324117Cytotoxicity against human LOXIMVI cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1327863Inhibition of pig brain tubulin polymerization measured at 1 min intervals for 90 mins by spectrophotometric analysis
AID502708Growth inhibition of human K562 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID616990Plasma protein binding in Sprague-Dawley rat at 6 umol/kg, iv2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1233617Growth inhibition of human A549 cells assessed as inhibition of cell proliferation after 24 hrs by MTT assay2015European journal of medicinal chemistry, Jun-24, Volume: 99Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin polymerization inhibitors.
AID1402070Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 1432-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.
AID1068597Growth inhibition of human OVCAR5 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1698828Cytotoxicity against human K562 cells2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Computational modeling and target synthesis of monomethoxy-substituted o-diphenylisoxazoles with unexpectedly high antimitotic microtubule destabilizing activity.
AID93837Compound was tested for cell arrest at G2/M phase at 100 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID769749Inhibition of pig brain tubulin assembly preincubated for 15 mins followed by GTP addition measured after 20 mins by spectrophotometric analysis in presence of glycerol2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.
AID1126012Inhibition of bovine brain tubulin polymerization at 1 uM after 60 mins by spectrophotometric analysis2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID471944Growth inhibition of human BxPC3 cells after 48 hrs by sulforhodamine B assay2009Journal of natural products, Sep, Volume: 72, Issue:9
Antineoplastic agents. 579. Synthesis and cancer cell growth evaluation of E-stilstatin 3: a resveratrol structural modification.
AID1353661Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 50 nM after 20 hrs by propidium iodide staining based flow cytometry (Rvb = 11 +/- 1%)2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID452622Cell cycle arrest in human K562 cells assessed as accumulation at G0/G1 phase at 10 uL after overnight incubation by propidium iodide staining-based flow cytometry2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID685197Growth inhibition of human M14 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1534544Drug metabolism in human liver microsomes assessed as cytochrome P450-mediated 2-methoxy-5-(1-(3,4,5-trimethoxyphenyl)vinyl)cyclohexa-2,5-diene-1,4-dione metabolite formation at 100 uM after 6 hrs in presence of NADPH generating system by HPLC-UV-MS analy2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID1862613Antiproliferative activity against human A549 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1741567Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Synthesis, and biological evaluation of 3,6-diaryl-[1,2,4]triazolo[4,3-a]pyridine analogues as new potent tubulin polymerization inhibitors.
AID716407Induction of microtubule depolymerization in human HaCaT cells at 10 '-6 M by confocal microscopy2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4.
AID1263272Cytotoxicity against human SK-MEL-28 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID691632Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as mortality at 50 mg/kg, ip qd after 21 days2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1698822Antimitotic activity against sea urchin embryo assessed as cleavage alteration measured 2.5 to 6 hrs post-fertilization by light microscopy analysis2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Computational modeling and target synthesis of monomethoxy-substituted o-diphenylisoxazoles with unexpectedly high antimitotic microtubule destabilizing activity.
AID1064405Growth inhibition of human U251 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1689105Toxicity in BALB/c nude mouse transfected with human HeLa cells assessed as spleen damage at 30 mg/kg/day, iv for 21 days by H&E staining based immunohistochemistry2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1518072Cytotoxicity against HUVEC assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1179505Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Synthesis, biological evaluation and molecular modeling of 1,3,4-thiadiazol-2-amide derivatives as novel antitubulin agents.
AID1729336Inhibition of PD1/PDL1 (unknown origin) protein-protein interaction measured after 15 mins by HTRF assay
AID1231331Anticancer activity against human U2OS cells assessed as reduction in cell proliferation after 48 hrs by WST-1 assay2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4.
AID1351657Inhibition of tubulin polymerization in human MDA-MB-231 cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID675714Inhibition of bovine brain tubulin assembly after 20 mins2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones and analogues: synthesis, cytotoxic activity, and study of the mechanism of action.
AID1308607Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining at 90 mins in presence of NADPH regenerating system by HPLC method2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1854155Cytotoxicity against human HeLa cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Cascade synthetic strategies opening access to medicinal-relevant aliphatic 3- and 4-membered N-heterocyclic scaffolds.
AID642535Displacement of [3H]cholchicine from bovine brain tubulin at 1 uM after 2 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. Part 2. The impact of bridging groups at position C-2.
AID288667Inhibition of tubulin polymerization2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies.
AID1534545Drug metabolism in rat liver microsomes assessed as cytochrome P450-mediated 2-methoxy-5-(1-(3,4,5-trimethoxyphenyl)vinyl)cyclohexa-2,5-diene-1,4-dione metabolite formation at 100 uM after 6 hrs in presence of NADPH generating system by HPLC-UV-MS analysi2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID281358Clearance in iv dosed Swiss Albino mouse plasma2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID685210Growth inhibition of human SKOV3 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID461784Antiproliferative activity against human HT-29 cells after 72 hrs by methylene blue dye assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors.
AID1575817Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay2019MedChemComm, Aug-01, Volume: 10, Issue:8
Synthesis and biological evaluation of structurally diverse α-conformationally restricted chalcones and related analogues.
AID691647Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as effect on WBC count at 50 mg/kg, ip qd after 21 days (Rvb = 25.38 +/- 0.22 x 10'3 mm'-3)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1847783Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 12-15, Volume: 52From natural products to HDAC inhibitors: An overview of drug discovery and design strategy.
AID1409118Resistance index, ratio of IC50 for human HeLa cells expressing wild type beta3 tubulin to IC50 for human HeLa cells2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.
AID1524383Antitumor activity mouse E0771 cells implanted in C57BL/6 mouse assessed tumor growth inhibition at 30 mg/kg, ip dosed every other day for 20 days relative to control2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents.
AID1628267Binding affinity to goat brain tubulin pre-incubated for 30 mins with 5-(Quinolin-3-yl)-4-(3,4,5-trimethoxyphenyl)-1H-imidazol-2-amine before compound exposure for 30 mins by fluorescence based assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID1765568Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM incubated for 10 mins by DEAE-cellulose filter method relative to control2021European journal of medicinal chemistry, Oct-15, Volume: 222Effects of substituent pattern on the intracellular target of antiproliferative benzo[b]thiophenyl chromone derivatives.
AID751507Inhibition of bovine brain tubulin assembly after 20 mins by spectrophotometric analysis2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.
AID1405396Antimigratory activity against human SKOV3 cells assessed as number of migrated cells at 50 nM after 24 hrs by crystal violet staining based transwell migration assay (Rvb = 49.3 to 50.7 No_unit)2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID617003Ratio of EC50 for microtubule depolymerization in human MDA-MB-435 cells to IC50 for human MDA-MB-435 cells2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID778976Cytotoxicity against human DU145 cells after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and biological evaluation of indole-based, anti-cancer agents inspired by the vascular disrupting agent 2-(3'-hydroxy-4'-methoxyphenyl)-3-(3″,4″,5″-trimethoxybenzoyl)-6-methoxyindole (OXi8006).
AID1422356Induction of bovine brain microtubule destabilization assessed as increase in free tubulin levels after 15 mins by Coomassie G-250 staining-based polyacrylamide gel electrophoresis method2018European journal of medicinal chemistry, Nov-05, Volume: 159Modified carbazoles destabilize microtubules and kill glioblastoma multiform cells.
AID1757280Antiproliferative activity against ADR-resistant human Bel-7402 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1176811Inhibition of bovine brain tubulin polymerization2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Microwave-assisted synthesis and biological evaluation of 3,4-diaryl maleic anhydride/N-substituted maleimide derivatives as combretastatin A-4 analogues.
AID486869Cytotoxicity against human DU145 cells by SRB assay2010Journal of natural products, Jun-25, Volume: 73, Issue:6
Regio- and stereospecific synthesis of mono-beta-d-glucuronic acid derivatives of combretastatin A-1.
AID1206087Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay2015European journal of medicinal chemistry, Apr-13, Volume: 94Design, synthesis and biological evaluation of novel pyrazoline-containing derivatives as potential tubulin assembling inhibitors.
AID1422818Antitumor activity against human H22 cells xenografted in ICR mouse assessed as reduction in tumor weight at 30 mg/kg, iv qd for 21 consecutive days
AID685188Growth inhibition of human KM12 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID685184Growth inhibition of human HCC2998 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID213853Binding constant at colchicine site of bovine brain tubulin2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
AID1327136Antiproliferative activity against human HT1080 cells measured after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 1224,5-Diaryl-3H-1,2-dithiole-3-thiones and related compounds as combretastatin A-4/oltipraz hybrids: Synthesis, molecular modelling and evaluation as antiproliferative agents and inhibitors of tubulin.
AID310758Antiproliferative activity against human DU145 cells2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
3-(2'-Bromopropionylamino)-benzamides as novel S-phase arrest agents.
AID607285Antiproliferative activity against human K562 cells assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID1518066Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID737014Displacement of [3H]colchicine from tubulin (unknown origin) at 5 uM after 10 mins2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Identification of diaryl 5-amino-1,2,4-oxadiazoles as tubulin inhibitors: the special case of 3-(2-fluorophenyl)-5-(4-methoxyphenyl)amino-1,2,4-oxadiazole.
AID1890477Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells in S phase at 10 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 16.61 %)2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
AID228457Inhibition of tubulin polymerization1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
Synthesis and cytotoxicity of 1,6,7,8-substituted 2-(4'-substituted phenyl)-4-quinolones and related compounds: identification as antimitotic agents interacting with tubulin.
AID1771521Induction of apoptosis in human MGC-803 cells assessed as viable cells at 2 nM measured after 48 hrs by Annexin V-APC/PI double staining based flow cytometry assay (Rvb =93.5 %)2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1330809Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Design, synthesis, anticancer, antimicrobial activities and molecular docking studies of theophylline containing acetylenes and theophylline containing 1,2,3-triazoles with variant nucleoside derivatives.
AID1737837Metabolic stability in human liver microsomes assessed as parent compound remaining at 10 uM measured after 5 mins in presence of NADPH by LC/MS/MS analysis2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID474643Induction of apoptosis in human HeLa cells assessed as cells containing hypodiploid DNA at 2.2 uM after 24 hrs by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1263273Cytotoxicity against human SK-MEL-5 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1486483Inhibition of colchicine binding to tubulin (unknown origin) up to 15 uM pretreated for 1 hr followed by colchicine addition by spectrofluorometric method2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis, biological evaluation and molecular modeling of imidazo[1,2-a]pyridine derivatives as potent antitubulin agents.
AID1728937Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 1 uM measured after 24 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.84%)2021European journal of medicinal chemistry, Mar-05, Volume: 213Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.
AID670888Cytotoxicity against human HT-29 cells after 48 hrs by resazurin assay2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
AID751509Inhibition of beta-3 tubulin (unknown origin) transfected in human HeLa cells assessed as growth inhibition after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.
AID1506488Cytotoxicity against human A549 cells after 48 hrs by MTT assay2017MedChemComm, Jan-01, Volume: 8, Issue:1
Design, synthesis, anticancer activity and docking studies of theophylline containing 1,2,3-triazoles with variant amide derivatives.
AID1628250Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 5 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 35%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID221962Compound was evaluated for cytotoxicity against human SKMEL-5 melanoma cell line.1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Synthesis and evaluation of analogues of (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene as potential cytotoxic and antimitotic agents.
AID1534522Inhibition of sheep brain tubulin polymerization by DAPI-fluorescence based fluorimetry2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID1572258Antiproliferative activity against human RS4:11 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.
AID1336747Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1757281Resistant index, ratio of IC50 for ADR-resistant human Bel-7402 cells to IC50 for human Bel-7402 cells2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1352479Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Spirohydantoins and 1,2,4-triazole-3-carboxamide derivatives as inhibitors of histone deacetylase: Design, synthesis, and biological evaluation.
AID665695Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID1773134Antiproliferative activity against human U-251 cells after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID619868Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 100 nM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 52.02+/-5.9%)2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID1518331Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.
AID404586Cytotoxicity against human HL60 cells after 72 hrs by XTT method2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Diarylmethyloxime and hydrazone derivatives with 5-indolyl moieties as potent inhibitors of tubulin polymerization.
AID455710Anticancer activity against human DU145 cells after 24 hrs by SRB assay2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Application of the McMurry coupling reaction in the synthesis of tri- and tetra-arylethylene analogues as potential cancer chemotherapeutic agents.
AID1058421Cytotoxicity against human MDA-MB-468 cells assessed as cell viability after 4 days by MTS assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation.
AID299205Antiproliferative activity against human MCF7 cells2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity relationships.
AID1338588Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of novel alkylsulfanyl-1,2,4-triazoles as cis-restricted combretastatin A-4 analogues.
AID1517170Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Potent combretastatin A-4 analogs containing 1,2,4-triazole: Synthesis, antiproliferative, anti-tubulin activity, and docking study.
AID1570335Cytotoxicity against human HuH7 cells assessed as reduction in cell viability measured after 24 hrs by cell titer blue assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.
AID348167Cytotoxicity against human MIAPaCa2 cells after 48 hrs by alamar blue assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Design, synthesis and biological evaluation of novel stilbene-based antitumor agents.
AID1200588Stability assessed as cis-trans isomerization equilibrium by mesuring remaining compound level at 1.5 x 10'-2 M exposed to UV-visible light irradiation after 22 hrs by LC-HRMS method2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Quantum chemistry calculation-aided structural optimization of combretastatin A-4-like tubulin polymerization inhibitors: improved stability and biological activity.
AID1773135Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1068607Growth inhibition of human MALME-3M cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1738824Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors.
AID319827Inhibition of tubulin assembly at 13 uM2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and antitumor activity of benzils related to combretastatin A-4.
AID1533697Antiangiogenic activity in Leghorn chicken embryo chorioallantoic membrane assessed as induction of corrosion at 2.5 nmol after 24 hrs by light microscopic analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163New naphthopyran analogues of LY290181 as potential tumor vascular-disrupting agents.
AID1863087Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway.
AID1406345Growth inhibition of human A549 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation.
AID1612655Antitumor activity against human H22 cells xenografted in ICR mouse assessed as reduction in tumor weight at 20 mg/kg/day, iv for 21 days relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1068601Growth inhibition of human UACC62 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID214166Inhibition of radiolabeled Colchicine binding to tubulin at 30 degrees C (0.25 mM MgCl2)1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions.
AID1411800Antiproliferative activity against human MCF7 cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID669463Growth inhibition of human DLD1 cells after 48 hrs by SRB assay2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID502752Growth inhibition of human BT549 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1504736Solubility of the compound in water irradiated with UV light
AID379677Inhibition of Saccharomyces cerevisiae RS321NYCp50 in galactose medium by microtiter plate assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID1435082Cell cycle arrest in human A549 cells assessed as accumulation at sub-G1 phase at 0.5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 1.3 +/- 0.4%)2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1317589Cytostatic activity against human MCF7 cells assessed as cell survival up to 25 uM measured after 72 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1757288n-Octanol/water partition coefficient, logD of the compound incubated for 24 hrs at pH 7.4 by HPLC analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1263275Cytotoxicity against human IGROV1 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1234871Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation after 72 hrs by XTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Exploring the size adaptability of the B ring binding zone of the colchicine site of tubulin with para-nitrogen substituted isocombretastatins.
AID1392073Inhibition of [3H]colchicine binding to bovine brain tubulin at 1 uM measured after 10 mins by scintillation counting method relative to control2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.
AID1126003Cytotoxicity against human HeLa cells after 72 hrs by resazurin based fluorescence assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1185205Antiproliferative activity against human CA46 cells assessed as reduction in cell viability after 72 hrs by MTT assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Novel 9'-substituted-noscapines: synthesis with Suzuki cross-coupling, structure elucidation and biological evaluation.
AID1068603Growth inhibition of human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID502740Growth inhibition of human NCI/ADR-RES cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1330810Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Design, synthesis, anticancer, antimicrobial activities and molecular docking studies of theophylline containing acetylenes and theophylline containing 1,2,3-triazoles with variant nucleoside derivatives.
AID1183659Growth inhibition of human A549 cells after 72 hrs by MTT assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID314019Antiproliferative activity against human UO31 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID567096Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues.
AID1068588Growth inhibition of human CAKI-1 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1294471Growth inhibition of human COLO205 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID103224Cell growth inhibition against MCF-7 human breast cancer cells using MTS assay2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
AID1709297Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1263252Cytotoxicity against human HOP92 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID617013Antiproliferative activity against human HeLa cells2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID616981Antiproliferative activity against human LoVo after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1263254Cytotoxicity against human NCI-H522 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1274776Antiproliferative activity against human MCF7 cells assessed as cell viability pre-incubated for 24 hrs with CO2 followed by compound addition after 72 hrs by MTT assay2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Synthesis and Biochemical Evaluation of 3-Phenoxy-1,4-diarylazetidin-2-ones as Tubulin-Targeting Antitumor Agents.
AID1285327Cell cycle arrest in human HT-29 cells assessed as accumulation at G2/M phase at 10 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 12.47%)2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID1458852Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining after 60 mins in presence of NADPH by UV-based HPLC-MS/MS analysis2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1506732Antiproliferative activity in human A549 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay2017MedChemComm, Feb-01, Volume: 8, Issue:2
Synthesis and biological evaluation of (-)-kunstleramide and its derivatives.
AID1406344Growth inhibition of human MCF7 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation.
AID474630Cytotoxicity against human SW620 cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1534362Antiproliferative activity against human KB cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
AID1421769Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Conformation impacts on the bioactivities of SMART analogues.
AID1463424Cell cycle arrest in human PC3 cells assessed as accumulation at G2/M phase at 0.05 uM incubated for 24 hrs by propidium iodide staining based FACS assay (Rvb = 14%)2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Constructing novel dihydrofuran and dihydroisoxazole analogues of isocombretastatin-4 as tubulin polymerization inhibitors through [3+2] reactions.
AID1562378Antiproliferative activity against human A2780 cells assessed as reduction in cell viability after 48 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin.
AID265409Antiproliferative activity against human HUVEC2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID635027Cytotoxicity against human NCI-H460 cells by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID486601Inhibition of bovine brain tubulin polymerization after 20 mins2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Synthesis, molecular modeling and biological evaluation of dithiocarbamates as novel antitubulin agents.
AID262912Inhibition of [3H]colchicine binding to tubulin at 5 uM2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Benzoylphenylurea sulfur analogues with potent antitumor activity.
AID1435070Cell cycle arrest in human HT29-D4 cells assessed as accumulation at G2/M phase at 0.5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 11.1 +/- 3.7%)2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1310191Growth inhibition of chicken cardiomyocytes after 48 hrs by MTT assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1555132Cytotoxicity against human NCI-H460 cells assessed as growth inhibition measured after 48 hrs by SRB assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.
AID1666246Inhibition of tubulin polymerization in human A549 cells assessed as disruption of microtubule network at 0.6 uM incubated for 18 hrs by Hoechst33342 staining based confocal microscopic analysis2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID1711849Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 50 nM measured after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 8.44 %)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID685167Cytotoxicity against human Hep2 cells after 48 hrs assessed as inhibition of cell growth at 10 uM after 48 hrs by SRB assay relative to control2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID642062Growth inhibition of doxorubicin-resistant human NCI-ADR-RES cells overexpressing P-glycoprotein after 96 hrs2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID685213Growth inhibition of human ACHN cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1727315Antiproliferative activity against human A549 cells assessed as cell viability after 24 hrs by Celltiter-Glo assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation.
AID685370Growth inhibition of human T47D cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID455991Cytotoxicity against human HeLa cells after 2 days2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of tubulin polymerization.
AID580347Antiproliferative activity against sea urchin embryo assessed as cleavage arrest after 10 to 15 mins fertilization 45 to 60 mins before first mitotic cycle completion2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Application of plant allylpolyalkoxybenzenes in synthesis of antimitotic phenstatin analogues.
AID1586012Inhibition of pig brain tubulin polymerization by spectrophotometric analysis
AID1760386Antiproliferative activity against human HeLa cells incubated for 24 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020).
AID1288162Antiproliferative activity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay2016European journal of medicinal chemistry, May-23, Volume: 114Synthesis and biological evaluation of quinoline analogues of flavones as potential anticancer agents and tubulin polymerization inhibitors.
AID340152Displacement of [3H]colchicine from microtubule associated protein rich tubulin at 5 uM2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.
AID642057Antiproliferative activity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID319838Cytotoxicity against HUVEC2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and antitumor activity of benzils related to combretastatin A-4.
AID1057117Drug metabolism in PBS at pH 7.4 assessed as product-1 level after 4 hrs by HPLC analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID281344Cytotoxicity against human DU145 cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1294487Growth inhibition of human MDA-MB-468 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1196873Displacement of [3H]colchicine from tubulin (unknown origin) at 1 uM after 30 mins by beta-counting2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID669467Inhibition of purified bovine tubulin polymerization at 5 uM measured 30 secs intervals for 60 mins by spectrophotometer analysis relative to control2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID1308606Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining at 60 mins in presence of NADPH regenerating system by HPLC method2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1873748Induction of apoptosis in human HeLa cells assessed as viable cells at 10 nM incubated for 72 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 90.1%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID1409117Antiproliferative activity against human HeLa cells expressing wild type beta3 tubulin after 48 hrs by sulforhodamine B assay2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.
AID214033Inhibition of bovine tubulin polymerization1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
Antitumor agents. 155. Synthesis and biological evaluation of 3',6,7-substituted 2-phenyl-4-quinolones as antimicrotubule agents.
AID1541864Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
AID427177Antiproliferative activity against human MOLT4 cells after 2 days by coulter counter method2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization.
AID1408396Induction of apoptosis in human K562 cells at 0.02 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.46%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1890441Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 10 uM incubated for 24 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 1.02 %)2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
AID78620Antiproliferative activity against the MDR positive human colon adenocarcinoma cell line HCT-152002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
AID1612624Drug resistance index, ratio of IC50 for VCR-resistant human K562/VCR cells to IC50 for human K562 cells2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID635028Cytotoxicity against human HT-29 cells by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID382331Cytotoxicity against human MDA-MB-231 cells assessed as [3H]thymidine incorporation after 72 hrs by microplate scintillation counter2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin.
AID1263269Cytotoxicity against human M14 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1179655Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design, synthesis and biological evaluation of (E)-3-(3,4-dihydroxyphenyl)acrylylpiperazine derivatives as a new class of tubulin polymerization inhibitors.
AID1689145Vascular disruptive effect in chicken fertilized egg chorioallantoic membrane at 5 nmol incubated for 24 hrs by CAM assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.
AID480727Induction of G1 phase arrest in Saccharomyces cerevisiae expressing TAP-tagged Clb5 assessed as down-regulation of Clb5 level at 450 uM after 3 hrs by Western blot analysis2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID101492In vitro inhibitory concentration against human chronic myelogenous leukemia K562 cell growth2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Novel benzylidene-9(10H)-anthracenones as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization.
AID616970Selectivity ratio of IC50 for HUVEC grown in absence of growth factors to IC50 for HUVEC grown in presence of growth factors2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID265438Cell cycle arrest in NCI-H460 cells by accumulation at S phase cell at 160 nM post 24 hrs treatment and 24 hrs recovery2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID450669Inhibition of calf brain tubulin polymerization at 20 uM after 20 mins by turbidimetric method2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Isocombretastatins A: 1,1-diarylethenes as potent inhibitors of tubulin polymerization and cytotoxic compounds.
AID617006Inhibition of microtubule polymerization in human MDA-MB-435 cells2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID265447Cell cycle arrest in NCI-H460 cells by accumulation at G2/M phase cell at 160 nM post 24 hrs treatment and 24 hrs recovery2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID1458851Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining after 30 mins in presence of NADPH by UV-based HPLC-MS/MS analysis2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID769829Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.
AID1906238Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 6 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 18.8%)
AID92127in vitro antitumor activity against NCI 's human tumor cell lines1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
AID151319In vitro cytotoxic activity tested against human ovarian cancer (SK-OV3) cell line2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.
AID1711842Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID306511Cell cycle arrest in human M21 cells assessed as accumulation at G2/M phase at 0.015 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1075757Displacement of [3H]colchine from tubulin (unknown origin) at 1 uM after 10 mins2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of 4-(N-cycloamino)phenylquinazolines as a novel class of tubulin-polymerization inhibitors targeting the colchicine site.
AID1727311Antiproliferative activity against human HCT116 cells assessed as cell viability after 24 hrs by Celltiter-Glo assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation.
AID1698445Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Ultrasound assisted synthesis of tetrazole based pyrazolines and isoxazolines as potent anticancer agents via inhibition of tubulin polymerization.
AID480732Induction of G1 phase arrest in alpha factor treated Saccharomyces cerevisiae expressing TAP-tagged Clb5 assessed as inhibition of Clb5 expression at 450 uM after 3 hrs by FACS analysis2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID616979Antiproliferative activity against human A375 after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID548395Cytotoxicity against estrogen receptor deficient human MDA-MB-231 cells assessed as LDH release at 10 uM2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Lead identification of conformationally restricted β-lactam type combretastatin analogues: synthesis, antiproliferative activity and tubulin targeting effects.
AID1435096Inhibition of cytoplasmic microtubule network assembly in human A549 cells assessed as cell surface occupied by fluorescent microtubule network at 0.05 uM preincubated for 4 hrs followed by compound washout measured immediately by confocal fluorescence mi2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1317606Inhibition of porcine brain tubulin polymerization at 10 uM measured every 1 min for 40 mins in presence of GTP2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID214555Inhibition of bovine tubulin polymerization1997Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
Antitumor agents. 174. 2',3',4',5,6,7-Substituted 2-phenyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.
AID474626Cytotoxicity against human cisplatin-resistant Hep2 cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1742935Inhibition of pig brain tubulin polymerization preincubated with compound followed by GTP addition and measured after 60 mins by microplate reader analysis2020European journal of medicinal chemistry, Dec-01, Volume: 207Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors.
AID635026Cytotoxicity against human MCF7 cells by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID771216Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID1405398Antimigratory activity against human SKOV3 cells assessed as number of migrated cells at 100 nM after 24 hrs by crystal violet staining based transwell migration assay (Rvb = 49.3 to 50.7 No_unit)2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID1882938Antitumor activity against human HT-29 cells xenografted in BALB/c nude mouse assessed as reduction in tumor weight at 20 mg/kg, ip administered as 2 days interval for 3 weeks and measured 3 weeks post-initial dosing relative to control2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1860249Aqueous solubility of the compound at pH 7.42022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-functional antitumor conjugates improving the anti-metastasis effect of combretastatin A4 by targeting tubulin polymerization and matrix metalloproteinases.
AID293363Antitumor activity in mouse implanted with S180 cells at 40 mg/kg, ip after 4 days2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID480723Induction of log phase growth arrest in Saccharomyces cerevisiae BY47412010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID1508552Inhibition of beta tubulin polymerisation in human HepG2 cells incubated for 2 hrs using TMB substrate by ELISA2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, antiproliferative, anti-tubulin activity, and docking study of new 1,2,4-triazoles as potential combretastatin analogues.
AID94325In vitro cytotoxic activity against human KB-VIN10 cell line overexpressing P-gp 170/MDR2004Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents.
AID1612626Antiproliferative activity against human ADR-resistant Bel7402/ADR cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1586075Displacement of [3H]-colchicine from bovine brain tubulin at 1 uM by scintillation proximity assay relative to control2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID1294480Growth inhibition of human OVCAR3 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1595696Inhibition of [3H]colchicine binding to biotinylated porcine tubulin at 1 uM in presence of GTP after 2 hrs by scintillation proximity assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID1517171Antiproliferative activity against human HL60 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Potent combretastatin A-4 analogs containing 1,2,4-triazole: Synthesis, antiproliferative, anti-tubulin activity, and docking study.
AID1460290Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM after 10 mins by scintillation counting method relative to control2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Bioreductively activatable prodrug conjugates of phenstatin designed to target tumor hypoxia.
AID1600493Inhibition of porcine brain tubulin polymerization at 10 umol measured every 60 secs by turbidometric assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID269717Cell cycle arrest in SHSY5Y cells by accumulation at G1 phase after 24 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID480725Reduction of budding index in Saccharomyces cerevisiae BY4741 at 450 uM relative to control2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID363249Growth inhibition of human DU145 after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Design, synthesis and biological evaluation of dihydronaphthalene and benzosuberene analogs of the combretastatins as inhibitors of tubulin polymerization in cancer chemotherapy.
AID657915Displacement of [3H]colchicine from tubulin at 5 uM after 10 mins2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID1285321Cell cycle arrest in human HT-29 cells assessed as accumulation at sub G1 phase at 10 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 1.00%)2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID757693Cytotoxicity against human Bel7402 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Synthesis and antitumor activity of novel 3,4-diaryl squaric acid analogs.
AID1200591Growth inhibition of human SKOV3 cells by MTT assay2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Quantum chemistry calculation-aided structural optimization of combretastatin A-4-like tubulin polymerization inhibitors: improved stability and biological activity.
AID502735Growth inhibition of human UACC62 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID569529Induction of apoptosis in human MCF7 cells assessed as increase of cleaved PARP level at 5 uM after 24 hrs by Western blotting2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents.
AID635029Cytotoxicity against human CEM cells by alamar blue assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
AID1518078Induction of apoptosis in human MDA-MB-468 cells assessed as viable cells at 100 nM after 24 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 96.8%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1411801Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID1906327Induction of microtubule disruption in human HeLa cells assessed as loss of formation of cell membrane rounding measured after 24 hrs at 2 to 5 nM by DAPI staining based laser scanning confocal microscopic analysis
AID455031Cytotoxicity against human BxPC3 cells after 48 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID474625Cytotoxicity against human Hep2 cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1690541Antiproliferative activity against human MCF7 cells measured after 48 hrs by SRB assay2020European journal of medicinal chemistry, Apr-01, Volume: 191Synthesis and structure-activity relationship study of water-soluble carbazole sulfonamide derivatives as new anticancer agents.
AID1773138Inhibition of pig brain tubulin polymerization at 1 uM by spectrometric method relative to control2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID751575Cytotoxicity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.
AID1064410Growth inhibition of human SF268 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1851427Induction of apoptosis in human K562 cells assessed as viable cells at 10 uM by AnnexinV-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 86.4%)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Synthesis and antitumor activity of a series of novel N-aryl-5-(2,2,2-trifluoroethoxy)-1,5-dihydro-2H-pyrrol-2-ones derivatives.
AID1882898Cytotoxicity against human A549/TxR cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1058422Cytotoxicity against human NCI-N87 cells assessed as cell viability after 4 days by MTS assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation.
AID1064420Growth inhibition of human NCI-H322M cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1336769Induction of apoptosis in human A549 cells assessed as necrotic cells at 100 nM after 48 hrs by Annexin-V FITC/propidium iodide staining based flow cytometry (Rvb = 0.1%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1435092Induction of cytoplasmic microtubule network disassembly in human A549 cells at 0.50 uM after 4 hrs by confocal fluorescence microscopic method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1427228Induction of microtubule disruption in human OVCAR3 cells assessed as change in microtubule architecture at 10 nM after 24 hrs by Alexa Fluor 647/DAPI staining based fluorescence microscopic method2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Combretastatin A4-β-Galactosyl Conjugates for Ovarian Cancer Prodrug Monotherapy.
AID1628247Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 5 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 49%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID1737838Metabolic stability in human liver microsomes assessed as parent compound remaining at 10 uM measured after 10 mins in presence of NADPH by LC/MS/MS analysis2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID480730Induction of G1 phase arrest in Saccharomyces cerevisiae expressing TAP-tagged Sic1 assessed as down-regulation of Sic1 level at 450 uM after 3 hrs by Western blot analysis2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
AID691637Antitumor activity against human HT-29 cells xenografted in nude BALB/c mouse assessed as decrease in tumor volume at 50 mg/kg, ip qd measured on day 21 relative to vehicle-treated control2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID94512Inhibitory concentration against taxol resistant cell line (KBs5) at a concentration of 50 nM using tetrazolium dye reduction assay (MTT)2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID1851621Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 10 uM by Annexin V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 1.02 %)2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives.
AID1317574Cytostatic activity against human MDA-MB-231 cells assessed as cell survival up to 25 uM measured after 72 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID265414Antiproliferative activity against doxorubicin-resistant human MCF7-dx cells2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID420614Displacement of [3H]colchicine from tubulin at 1 uM by turbidimetry2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Design and synthesis of 2-(3-benzo[b]thienyl)-6,7-methylenedioxyquinolin-4-one analogues as potent antitumor agents that inhibit tubulin assembly.
AID461789Displacement of [3H]colchicine from tubulin by at 5 uM scintillation proximity assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors.
AID761829Cytotoxicity against human HT-29 cells after 48 hrs by sulforhodamine B assay2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity.
AID1832149Inhibition of beta-tubulin polymerization in human HeLa cells assessed as inhibition of EBI-beta-tubulin adduct formation at 10 uM measured by Western blot-based EBI competition assay2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID1310250Cytotoxicity against fertilized white leghorn chicken embryos in CAM model assessed as lethality at 5 nmol after 24 hrs relative to control2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1518083Induction of apoptosis in human MDA-MB-468 cells assessed as early apoptotic cells at 100 nM after 48 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 0.35 to 1.25%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID403641Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID1196874Displacement of [3H]colchicine from tubulin (unknown origin) at 10 uM after 30 mins by beta-counting2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID1267532Inhibition of Tubulin polymerization in human HeLa cells assessed as decrease in dynamic tyrosinated microtubules after 2 hrs by microplate reader analysis2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Synthesis and biological evaluation of thiophene and benzo[b]thiophene analogs of combretastatin A-4 and isocombretastatin A-4: A comparison between the linkage positions of the 3,4,5-trimethoxystyrene unit.
AID376520Cytotoxicity against mouse P388 cells2000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID1518071Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1351624Induction of apoptosis in human MDA-MB-231 cells after 24 hrs by FITC Annexin V/propidium iodide staining-based FACScan flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID387312Antiproliferative activity against human Molt4/C8 cells after 2 days2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.
AID1189963Toxicity in C57BL/6 mouse assessed as interphase microtubule de-stabilizing activity by measuring leakage of rhodamine through the gut at 1 mg/kg, iv co-administered with rhodamine B by fluorimetry2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Synthesis and biological evaluation of furanoallocolchicinoids.
AID1646992Selectivity index, ratio of IC50 for cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay to IC50 for antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measure2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID474633Cell cycle arrest in human HeLa cells assessed as accumulation of cells in G0/1 phase at 0.2 uM after 24 hrs using propidium iodide by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1285338Induction of apoptosis in human HT-29 cells assessed as early apoptotic cells at 10 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb=1.30%)2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID1274779Inhibition of tubulin polymerization in human MCF7 cells assessed as loss of microtubules formation at 100 nM incubated for 16 hrs by FITC-DAPI staining based confocal microscopic analysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Synthesis and Biochemical Evaluation of 3-Phenoxy-1,4-diarylazetidin-2-ones as Tubulin-Targeting Antitumor Agents.
AID1068594Growth inhibition of human OVCAR8 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1736452Selectivity index, ratio of IC50 for drug resistant human MCF7 cells to IC50 for human MCF7 cells2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1435091Induction of cytoplasmic microtubule network disassembly in human A549 cells assessed as cell surface occupied by fluorescent microtubule network at 0.05 uM after 4 hrs by confocal fluorescence microscopic method (Rvb = 31 +/- 4%)2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1517354Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTS assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Design and synthesis of (2-(phenylamino)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone analogues as potent anti-tubulin polymerization agents.
AID1285319Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID379680Inhibition of topoisomerase 1 in Saccharomyces cerevisiae RS321N in galactose medium by microtiter plate assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID1585986Cytotoxicity against human T47D cells after 72 hrs by MTT assay
AID57710Cell growth inhibition against DU-145 human prostate cancer cells using MTS assay2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
AID1351635Induction of apoptosis in human HaCaT cells assessed as increase in histone-associated DNA fragments in oligonucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1742930Antiproliferative activity against human K562 cells assessed as inhibition of cell growth at 1 uM incubated for 72 hrs by MTT assay relative to control2020European journal of medicinal chemistry, Dec-01, Volume: 207Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors.
AID1612629Inhibition of [3H]-colchicine binding to biotinylated porcine tubulin at 1 uM after 2 hrs by SPA relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1729301Cytotoxicity against human NCM460 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
AID1693363Antiproliferative activity against human SK-OV-3 MDR-1-6/6 cells expressing Pgp assessed as decrease in cell growth measured after 48 hrs by SRB method2021Bioorganic & medicinal chemistry, 01-01, Volume: 29The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
AID471947Growth inhibition of human NCI-H460 cells after 48 hrs by sulforhodamine B assay2009Journal of natural products, Sep, Volume: 72, Issue:9
Antineoplastic agents. 579. Synthesis and cancer cell growth evaluation of E-stilstatin 3: a resveratrol structural modification.
AID452613Cytotoxicity against human K562 cells2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID546572Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Synthesis and evaluation of azetidinone analogues of combretastatin A-4 as tubulin targeting agents.
AID1324139Cytotoxicity against human MDA-MB-468 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1475518Inhibition of [3H]-colchicine binding to tubulin (unknown origin) at 5 uM after 10 mins relative to control2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
In Vivo and Mechanistic Studies on Antitumor Lead 7-Methoxy-4-(2-methylquinazolin-4-yl)-3,4-dihydroquinoxalin-2(1H)-one and Its Modification as a Novel Class of Tubulin-Binding Tumor-Vascular Disrupting Agents.
AID657877Growth inhibition of human BxPC3 cells after 48 hrs by sulforhodamine B assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID539830Inhibition of bovine tubulin polymerization in cell-free system at 3 uM2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Design, synthesis, and biological evaluation of novel N-γ-carboline arylsulfonamides as anticancer agents.
AID1126005Antimicrotubule activity in human MDA-MB-231 cells assessed as reduction of interphase microtubule network at 1 uM after 24 hrs by indirect immunofluorescence technique2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1233608Induction of microtubule depolymerization and cytoskeleton disruption in human M21 cells at 10 nM after 24 hrs by immunofluorescence assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model.
AID1408366Antiproliferative activity against human K562 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1628239Antiproliferative activity against drug resistant mouse EMT6/AR1 cells incubated for 24 hrs by sulforhodamine B assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID1487507Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B assay2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Design and synthesis of 4-morpholino-6-(1,2,3,6-tetrahydropyridin-4-yl)-N-(3,4,5-trimethoxyphenyl)-1,3,5-triazin-2-amine analogues as tubulin polymerization inhibitors.
AID1392068Antiproliferative activity against human HeLa cells expressing wild type beta3 tubulin by SRB assay2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.
AID750810Displacement of [3H]colchicine from bovine brain tubulin after 20 mins2013European journal of medicinal chemistry, Jun, Volume: 64Cytotoxic activities of substituted 3-(3,4,5-trimethoxybenzylidene)-1,3-dihydroindol-2-ones and studies on their mechanisms of action.
AID1595721Antitumor activity against mouse H22 cells allografted in ICR mouse assessed as reduction in tumour weight at 20 mg/kg, iv administered once per day for 21 days relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID1824151Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 5 nM measured after 48 hrs by flow cytometric analysis (Rvb = 69.8 + /- 8 %)2022European journal of medicinal chemistry, Feb-05, Volume: 229Branched alkyl of phenyl 4-(2-oxo-3-alkylimidazolidin-1-yl)benzenesulfonates as unique cytochrome P450 1A1-activated antimitotic prodrugs: Biological evaluation and mechanism of bioactivation.
AID1420994Antiproliferative activity against human A549 cells after 72 hrs by XTT assay
AID1351611Inhibition of tubulin polymerization in human MCF7 cells assessed as micronuclei formation at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID613282Antiproliferative activity against human KB cells after 72 hrs by methylene blue assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and biological evaluation of 1-(4'-Indolyl and 6'-Quinolinyl) indoles as a new class of potent anticancer agents.
AID1324107Cytotoxicity against human SF268 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID607532Inhibition of tubulin alpha polymerization in human HeLa cells assessed as decreased pelletable tubulin alpha fraction at 3 times IC50 value after 16 hrs by Western blotting in presence of paclitaxel2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues.
AID1310182Growth inhibition of human 518A2 cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1771458Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition after 72 hrs by SRB assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID662354Cell cycle arrest in human HuTu 80 cells assessed as reduction at sub-G1 phase at 30 nM after 72 hrs by propidium iodide-based flow cytometry (Rvb = 4.3 %)2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID685374Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 4 uM after 24 hrs by FACS analysis (Rvb = 34.88%)2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1701014Resistance index, ratio of GI50 for antiproliferation activity against human A549/Taxol cells to GI50 for antiproliferation activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
AID1381553Cytotoxicity against human Capan1 cells after 72 hrs by XTT assay2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
New somatostatin-drug conjugates for effective targeting pancreatic cancer.
AID1887835Antiproliferative activity against human HCT-8 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR.
AID605777Antivasculogenic activity against human HT1080 cells xenografted in chicken chorioallantoic membrane assessed as inhibition of tumor growth at 1 ug per egg, iv measured on day 14 by CAM assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID626628Disruption of cytoskeleton microtubule structure of human M21 cells at 5 times IC50 after 16 hrs by indirect immunofluorescence assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID1534360Antiproliferative activity against human K562 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
AID1057196Selectivity ratio of IC50 for HEK293 cells to IC50 for human MCF7 cells2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity.
AID1647042Antitumor activity against human A549 cells xenografted in immunodeficient BALB/c nude mouse assessed as tumor growth inhibition at 30 mg/kg, iv administered once daily for 29 days measured every 2 days for 29 days by electronic caliper relative to contro2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID39117Concentration which produces 50% inhibition of growth of murine melanoma B16 cell line2001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Combretoxazolones: synthesis, cytotoxicity and antitumor activity.
AID1324111Cytotoxicity against human U251 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1600486Induction of mitotic block in human CCRF-CEM cells assessed as histone H3 Ser10 phosphorylation level at 5 times antiproliferative IC50 incubated for 48 hrs by PI staining based flow cytometric analysis (Rvb = 0.97%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID461783Antiproliferative activity against human H460 cells after 72 hrs by methylene blue dye assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors.
AID1574871Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 2 to 8 uM measured after 24 hrs by CCK8 assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Synthesis and characterization of a photoresponsive doxorubicin/combretastatin A4 hybrid prodrug.
AID1711845Antiproliferative activity against human MIA Paca-2 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID1064422Growth inhibition of human NCI-H226 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1351592Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1411598Inhibition of human OATP1B3 expressed in HEK293 cells assessed as FMTX uptake after 5 mins by fluorescence assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1851620Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 10 uM by Annexin V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 4.66 %)2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives.
AID685195Growth inhibition of human LOXIMVI cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID273083Antiproliferative activity against human DU145 cells after 72 hrs2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and structure-activity relationships of carbazole sulfonamides as a novel class of antimitotic agents against solid tumors.
AID442980Vascular disrupting activity in HUVEC assessed as disorganization of microtubule at 0.1 uM after 1 hr by FITC-onjugated DAPI staining-based immunofluorescence assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Vascular disrupting activity of tubulin-binding 1,5-diaryl-1H-imidazoles.
AID607283Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID1126008Cell cycle arrest in human HeLa cells assessed as accumulation at G0/M phase at 1 uM after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 15.70%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1832107Antiproliferative activity against human A549 assessed as reduction in cell viability measured after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID1068634Growth inhibition of human K562 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID384964Antiproliferative activity against bovine microvascular endothelial cells2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
Synthesis and biological activity of fluorinated combretastatin analogues.
AID1506489Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay2017MedChemComm, Jan-01, Volume: 8, Issue:1
Design, synthesis, anticancer activity and docking studies of theophylline containing 1,2,3-triazoles with variant amide derivatives.
AID387313Antiproliferative activity against human CEM cells after 2 days2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.
AID685170Growth inhibition of human K562 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1351596Cytotoxicity against human CCD39Lu cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID366990Cytotoxicity against mouse L1210 cells after 72 hrs by MTT assay2008European journal of medicinal chemistry, Sep, Volume: 43, Issue:9
1,2,3,4-tetrahydro-2-thioxopyrimidine analogs of combretastatin-A4.
AID492263Displacement of [3H]colchicine from bovine brain tubulin at 1 uM2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Substituted 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]thiophene derivatives as potent tubulin polymerization inhibitors.
AID1420992Inhibition of bovine brain tubulin polymerization at 20 uM after 30 mins by UV-based assay relative to control
AID1873773Induction of mitochondrial membrane potential alteration in human HeLa cells assessed as early apoptotic cells at 10 nM measured after 48 hrs by JC1 staining-based flow cytometry analysis (Rvb = 9.07 %)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID670885Antimitotic activity in human HeLa cells assessed as disruption of interphase microtubule network at 3 nM after 6 hrs by DAPI staining-based immunofluorescence analysis2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
AID293334Antiproliferative activity against human HCT116 cells2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID767274Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured after 20 mins by turbidimetric analysis2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exploring natural product chemistry and biology with multicomponent reactions. 5. Discovery of a novel tubulin-targeting scaffold derived from the rigidin family of marine alkaloids.
AID391280Cytotoxicity against human H460 cells by sulforhodamine B test2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Novel A-ring and B-ring modified combretastatin A-4 (CA-4) analogues endowed with interesting cytotoxic activity.
AID1351659Inhibition of tubulin polymerization in human MCF7 cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID228451Percentage inhibition of binding of [3H]colchicine to tubulin at 5 uM2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Design, synthesis, and biological evaluation of a series of lavendustin A analogues that inhibit EGFR and Syk tyrosine kinases, as well as tubulin polymerization.
AID1524360Cell cycle arrest in human K562 cells assessed as mitotic index at 10 times IC50 by Giemsa staining-based assay (Rvb = 3%)2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents.
AID103357Inhibitory concentration to inhibit the growth of MCF-7 human breast carcinoma cells.2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
One-pot synthesis of benzo[b]furan and indole inhibitors of tubulin polymerization.
AID1334732Aqueous solubility of the compound at pH 2 measured after 4 hrs by HPLC/UV analysis2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility.
AID502743Growth inhibition of human A498 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1628236Antiproliferative activity against human MCF7 cells incubated for 48 hrs by sulforhodamine B assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID526643Aqueous solubility of the compound in water after 24 hrs by shake-flask method2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
Discovery of novel 2-aryl-4-benzoyl-imidazoles targeting the colchicines binding site in tubulin as potential anticancer agents.
AID1700958Antiproliferation activity against human A549/Taxol cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
AID1628248Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 10 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 49%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID248331Concentration required for the 50% inhibition of human lung caner (A549) cell line growth2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.
AID1194523Inhibition of tubulin polymerization (unknown origin)2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Novel hybrid nocodazole analogues as tubulin polymerization inhibitors and their antiproliferative activity.
AID1205517Inhibition of bovine brain tubulin assembly after 20 mins incubation by spectrophotometric analysis2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.
AID1731565Displacement of [3H]colchicine from bovine brain tubulin at 5 uM by DEAE-cellulose filter method relative to control2021European journal of medicinal chemistry, Mar-15, Volume: 214A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents.
AID213847Inhibition of binding of [3H]colchicine (5.0 uM) to tubulin (1.0 uM) at a concentration of 1.0 uM1999Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
Synthesis and biological evaluation of dihydrobenzofuran lignans and related compounds as potential antitumor agents that inhibit tubulin polymerization.
AID1057199Cytotoxicity against human MCF7 cells assessed as growth inhibition after 3 days by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity.
AID277278Cytotoxicity against HCT116 cell line2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Highly potent triazole-based tubulin polymerization inhibitors.
AID473860Inhibition of bovine brain tubulin assembly assessed as decrease in turbidity after 20 mins2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Synthesis, antitubulin, and antiproliferative SAR of analogues of 2-methoxyestradiol-3,17-O,O-bis-sulfamate.
AID261214Displacement of [3H]colchicine from tubulin at 65 nM2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines.
AID1157568Inhibition of FGFR1 (unknown origin) assessed as incorporation of [32P] gamma-ATP in to myelin basic protein after 30 mins by autoradiographic analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.
AID685205Growth inhibition of human OVCAR3 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID84539Cell growth inhibition against HR, human gastric cancer cells using MTS assay2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
AID1469204Growth inhibition of human A549 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1348622Antiproliferative activity against human K562R cells after 72 hrs by resazurin-based fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID1865675Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.
AID265407Inhibition of tubulin polymerization2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID1312640Inhibition of lamb brain tubulin polymerization by spectrophotometric method based microtubule assay2016European journal of medicinal chemistry, Aug-25, Volume: 119Recent developments of C-4 substituted coumarin derivatives as anticancer agents.
AID618344Inhibition of tubulin polymerization2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Design, synthesis and antiproliferative activities of biarylolefins based on polyhydroxylated and carbohydrate scaffolds.
AID1518084Induction of apoptosis in human MDA-MB-468 cells assessed as late apoptotic cells at 100 nM after 48 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 1.03 to 1.59%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID449226Selectivity index, ratio of IC50 for HSMC to IC50 for human MCF72009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
AID247255Growth inhibition against human neuroblastoma cell line (SK-N-SH)2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID515464Cytotoxicity against human vinblastine-resistant KBV1 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
4-(3-Halo/amino-4,5-dimethoxyphenyl)-5-aryloxazoles and -N-methylimidazoles that are cytotoxic against combretastatin A resistant tumor cells and vascular disrupting in a cisplatin resistant germ cell tumor model.
AID1348627Increase in PGF2alpha-induced contractile response in isolated Wistar rat aorta rings at 10 uM after 10 mins2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID637150Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3
Synthesis, biological evaluation, and molecular docking studies of cinnamic acyl 1,3,4-thiadiazole amide derivatives as novel antitubulin agents.
AID1600474Therapeutic index, ratio of IC50 for human BJ cells to IC50 for human CCRF-CEM cells2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID293337Cell cycle arrest in HMEC1 cells assessed as accumulation at G1 phase at 6.25 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID1689021Inhibition of bovine brain tubulin polymerization at 10 uM measured at 30 sec interval for 30 mins in presence of GTP by turbidimetry-based spectrophotometric method2020European journal of medicinal chemistry, Mar-01, Volume: 189β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells.
AID1518090Retention time of the compound using acetonitrile:water at ratio of 50:50 as mobile phase by reverse-phase HPLC analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1263267Cytotoxicity against human U251 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID721883Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by MTT assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID1517357Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTS assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Design and synthesis of (2-(phenylamino)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone analogues as potent anti-tubulin polymerization agents.
AID626633Antiangiogenic activity in human HT1080 cells xenografted in chicken chorioallantoic membrane assessed as vascular disruption at 1 to 3 ug, iv measured on day 17 by CAM assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID1738825Antiproliferative activity against human Daoy cells assessed as inhibition of cell growth2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors.
AID550211Antimitotic activity against Paracentrotus lividus embryo assessed as embryo spinning after 0.5 to 20 hrs post dose by sea urchin embryo assay2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Synthesis of antimitotic polyalkoxyphenyl derivatives of combretastatin using plant allylpolyalkoxybenzenes.
AID1729297Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
AID150373In vitro inhibitory activity against P388 lymphocytic leukemia cell line1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Antineoplastic agents. 291. Isolation and synthesis of combretastatins A-4, A-5, and A-6(1a)
AID1689096Induction of apoptosis in human HeLa cells assessed as cell membrane integrity loss, chromatin condensation and apoptotic body formation by measuring strengthened orange fluorescence intensity at 0.5 uM measured after 24 hrs by AO/EB dual staining based f2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1717108Solubility of compound in water at pH 7.4 by UV-HPLC method2020European journal of medicinal chemistry, Jan-15, Volume: 186Design, synthesis and bio-evaluation of novel 2-aryl-4-(3,4,5-trimethoxy-benzoyl)-5-substituted-1,2,3-triazoles as the tubulin polymerization inhibitors.
AID1906207Induction of cell cycle arrest in human HeLa cells assessed as S-phase at 3 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 23.4%)
AID214031Tested for inhibition against tubulin polymerization2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
6-Alkylamino- and 2,3-dihydro-3'-methoxy-2-phenyl-4-quinazolinones and related compounds: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.
AID455987Cytotoxicity against mouse L1210 cells after 2 days2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of tubulin polymerization.
AID622529Drug metabolism in rat microsomes assessed as metabolite formation2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1424776Inhibition of tubulin polymerization (unknown origin) preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric method2018European journal of medicinal chemistry, May-25, Volume: 152New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors.
AID1862614Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID342520Induction of morphological changes in human EA.hy 926 cells assessed as rounding up after 2 hrs2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Synthesis and biological evaluation of new disubstituted analogues of 6-methoxy-3-(3',4',5'-trimethoxybenzoyl)-1H-indole (BPR0L075), as potential antivascular agents.
AID1717458Antiproliferative activity against human SGC-7901 cells measured after 72 hrs by MTT assay
AID515462Cytotoxicity against human HL60 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
4-(3-Halo/amino-4,5-dimethoxyphenyl)-5-aryloxazoles and -N-methylimidazoles that are cytotoxic against combretastatin A resistant tumor cells and vascular disrupting in a cisplatin resistant germ cell tumor model.
AID1353629Antiproliferative activity against human HT-29 cells after 2 days by MTT assay2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID1310251Cytotoxicity against fertilized white leghorn chicken embryos in CAM model assessed as lethality at 2.5 nmol after 24 hrs relative to control2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1324120Cytotoxicity against human OVCAR3 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1860230Cell cycle arrest in human HepG2 cells assessed as accumulation of cells in G2/M phase at 100 nM measured after 12 hrs by flow cytometry method (Rvb = 12.21%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-functional antitumor conjugates improving the anti-metastasis effect of combretastatin A4 by targeting tubulin polymerization and matrix metalloproteinases.
AID1233572Antiproliferative activity against human M21 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model.
AID737111Cytotoxicity against human SEM cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID1403593Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
AID1402688Antiproliferative activity against HEK293 cells after 24 hrs by SRB assay
AID269720Cell cycle arrest in SHSY5Y cells by accumulation at G2 phase after 12 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID1637522Cell cycle arrest in human HeLa cells assessed as accumulation at S phase at 40 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 3.52%)2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID269713Induction of tubulin depolymerization at 1.6 nM after 24 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID1276335Inhibition of bovine tubulin assembly after 15 mins by turbidimetric analysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Novel Microtubule-Targeting 7-Deazahypoxanthines Derived from Marine Alkaloid Rigidins with Potent in Vitro and in Vivo Anticancer Activities.
AID1437255Cytotoxicity against human K562 cells assessed as growth inhibition after 5 days by MTT assay2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Tubulin-binding dibenz[c,e]oxepines: Part 2. Structural variation and biological evaluation as tumour vasculature disrupting agents.
AID1154743Growth inhibition of wild type human HeLa cells after 96 hrs incubation by sulforhodamine B technique2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential.
AID1435069Cell cycle arrest in human HT29-D4 cells assessed as accumulation at S phase at 0.5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 63.3 +/- 6.5%)2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1068633Growth inhibition of human MOLT4 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1882907Displacement of [3H] colchicine from tubulin (unknown origin) at 2.5 uM measured after 2 hrs by scintillation counting analysis relative to control2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1198453Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents.
AID1600466Cytotoxicity against human K562-TAX cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1637523Cell cycle arrest in human HeLa cells assessed as accumulation at S phase at 60 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 3.52%)2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID1351619Inhibition of tubulin polymerization in human HeLa cells assessed as micronuclei formation at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID94010Inhibitory concentration against VP16 resistant cell line (KB-7D) using tetrazolium dye reduction assay (MTT)2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID290175Antiproliferative activity against human MCF7 cells2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents.
AID536485Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 10 mins2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.
AID1508152Induction of intrinsic apoptosis in human MCF7 cells assessed as effect on mitochondrial membrane depolarization at 2 uM after 18 hrs by DiOC6 staining-based FACS analysis (Rvb = 2%)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1809273Antiproliferative activity against human MCF7/ADR cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
AID1198456Inhibition of bovine brain tubulin polymerization incubated for 20 mins by spectrophotometry2015European journal of medicinal chemistry, Mar-26, Volume: 93Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents.
AID214539Compound was evaluated for inhibition of tubulin polymerization2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
The synthesis and tubulin binding activity of thiophene-based analogues of combretastatin A-4.
AID1285316Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID250050Percentage of mitosis after 8 hr exposure of HL60 cells to the compound at 2.5 nM2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Heterocyclic and phenyl double-bond-locked combretastatin analogues possessing potent apoptosis-inducing activity in HL60 and in MDR cell lines.
AID1635267Induction of microtubule depolymerization in human A10 cells incubated for 18 hrs by indirect immunofluorescence analysis2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID685181Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1538716Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition and measured for 20 mins by turbidimetry-based spectrophotometric method2019European journal of medicinal chemistry, Sep-15, Volume: 178Evaluating the effects of fluorine on biological properties and metabolic stability of some antitubulin 3-substituted 7-phenyl-pyrroloquinolinones.
AID642114Induction apoptosis in human HeLa cells assessed as caspase -3 activity at 100 nM after 24 hrs by single-cell immunofluorescence assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1064381Growth inhibition of human PC3 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID214037The compound was evaluated for the anti-tubulin activity.1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel combretastatin analogues effective against murine solid tumors: design and structure-activity relationships.
AID644554Inhibition of bovine tubulin polymerization at 5 uM measured every 3 secs for 60 mins by spectrophotometry relative to control2012Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5
Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A-1.
AID1297648Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured after 20 mins by spectrophotometric method2016European journal of medicinal chemistry, Jun-30, Volume: 116Triazole tethered C5-curcuminoid-coumarin based molecular hybrids as novel antitubulin agents: Design, synthesis, biological investigation and docking studies.
AID1552972Antiproliferative activity against human COLO205 cells assessed as reduction in cell viability by MTT assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Synthesis and biological evaluation of 7-methoxy-1-(3,4,5-trimethoxyphenyl)-4,5-dihydro-2H-benzo[e]indazoles as new colchicine site inhibitors.
AID721877Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition by trypan blue exclusion assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID1285325Cell cycle arrest in human HT-29 cells assessed as accumulation at S phase at 10 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 3.02%)2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID444161Relative resistance, ratio of IC50 for human SKOV3 expressing adenoviral MDR1 cells to IC50 for human SKOV3 cells2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID449232Selectivity index, ratio of IC50 for HUVEC to IC50 for human MCF7 cells2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
AID1727312Antiproliferative activity against human K562 cells assessed as cell viability after 24 hrs by Celltiter-Glo assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation.
AID1686595Growth inhibition of human A2780 cells2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Potent Antitumor Activities and Structure Basis of the Chiral β-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin.
AID1689081Induction of apoptosis in human HeLa cells assessed as upregulation of PARP protein expression at 0.5 uM measured after 24 hrs by western blot analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1064393Growth inhibition of human OVCAR5 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID340150Inhibition of microtubule associated protein rich tubulin polymerization2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.
AID1742929Antiproliferative activity against human K562 cells assessed as inhibition of cell growth at 10 uM incubated for 72 hrs by MTT assay relative to control2020European journal of medicinal chemistry, Dec-01, Volume: 207Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors.
AID1891180Cytotoxicity against HEK293 cells assessed as inhibition of cell growth by MTT assay
AID1534543Drug metabolism in rat liver microsomes assessed as cytochrome P450-mediated 4-(1-(3-hydroxy-4-methoxyphenyl)vinyl)-2,6-dimethoxyphenol metabolite formation at 100 uM after 6 hrs in presence of NADPH generating system by HPLC-UV-MS analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID1518080Induction of apoptosis in human MDA-MB-468 cells assessed as late apoptotic cells at 100 nM after 24 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 1.03 to 1.59%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1421774Selectivity index, ratio of IC50 for mouse L929 cells to IC50 for human A549 cells2018European journal of medicinal chemistry, Oct-05, Volume: 158Conformation impacts on the bioactivities of SMART analogues.
AID1917033Cytotoxicity against human A549 cells assessed as cell growth inhibition2022European journal of medicinal chemistry, Nov-05, Volume: 241Recent advances in combretastatin A-4 codrugs for cancer therapy.
AID1421776Inhibition of porcine tubulin polymerization preincubated for 1 min and measured for 82 mins by fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Conformation impacts on the bioactivities of SMART analogues.
AID1348623Inhibition of sheep brain tubulin polymerization assessed as reduction in rate of microtubule assembly by DAPI-fluorescence based assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID214197The compound was tested for the % inhibition of [3H]colchicine binding to tubulin at a concentration of 5 uM1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Antitumor agents. 181. Synthesis and biological evaluation of 6,7,2',3',4'-substituted-1,2,3,4-tetrahydro-2-phenyl-4-quinolones as a new class of antimitotic antitumor agents.
AID247822Inhibition of tubulin polymerization interacting at the colchicine binding site.2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Antimitotic activity and reversal of breast cancer resistance protein-mediated drug resistance by stilbenoids from Bletilla striata.
AID502728Growth inhibition of human U251 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID735511Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 10 mins by scintillation counting analysis2013European journal of medicinal chemistry, Apr, Volume: 62(E)-4-aryl-4-oxo-2-butenoic acid amides, chalcone-aroylacrylic acid chimeras: design, antiproliferative activity and inhibition of tubulin polymerization.
AID619856Antiproliferative activity against ER expressing human MCF7 cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID1064401Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1741597Inhibition of pig brain tubulin polymerization at 10 uM measured at 1 min interval for 20 mins by spectrophotometric method relative to control2020European journal of medicinal chemistry, Oct-15, Volume: 204Synthesis, and biological evaluation of 3,6-diaryl-[1,2,4]triazolo[4,3-a]pyridine analogues as new potent tubulin polymerization inhibitors.
AID757686Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Synthesis and antitumor activity of novel 3,4-diaryl squaric acid analogs.
AID1196872Cell cycle arrest in human SH-SY5Y cells assessed as accumulation at S phase at IC50 after 16 hrs by flow cytometry (Rvb = 10.6 %)2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID1666244Cytotoxicity against mouse HT22 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID1917034Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition2022European journal of medicinal chemistry, Nov-05, Volume: 241Recent advances in combretastatin A-4 codrugs for cancer therapy.
AID1432891Inhibition of beta-tubulin polymerization in human MDA-MB-231 cells at 50 nM after 1 hr by NucBlue staining based immunofluorescence microscopic assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Development of a novel near-infrared fluorescent theranostic combretastain A-4 analogue, YK-5-252, to target triple negative breast cancer.
AID1285320Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID1595690Antiproliferative activity against human KB cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID685185Growth inhibition of human HCT116 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1317618Induction of apoptosis in human EAhy926 cells assessed as early apoptotic cells at 0.11 uM measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1637521Cell cycle arrest in human HeLa cells assessed as accumulation at G1 phase at 60 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 73.28%)2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID1572256Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.
AID1906231Induction of apoptosis in human HeLa cells assessed as viable cells at 3 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 75.5%)
AID622526Inhibition of bovine brain tubulin polymerization after 30 mins by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID265423Cell cycle arrest in NCI-H460 cells by accumulation at G1/0 phase cell at 3 nM post 24 hrs treatment and 24 hrs recovery2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID1906265Resistant factor, ratio of IC50 for antiproliferative activity against human HeLa/DDP cells to IC50 for human HeLa cells
AID442545Cytotoxicity against human HL60 cells after 72 hrs by XTT assay2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Exploring the effect of 2,3,4-trimethoxy-phenyl moiety as a component of indolephenstatins.
AID761819Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Correlation of hydrogen-bonding propensity and anticancer profile of tetrazole-tethered combretastatin analogues.
AID1535579Cytotoxicity against mouse primary hepatocytes after 24 hrs by MTT assay2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Synthesis, biological evaluation and molecular docking of benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives as novel tubulin polymerization inhibitors.
AID403645Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID685203Growth inhibition of human UACC62 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1637520Cell cycle arrest in human HeLa cells assessed as accumulation at G1 phase at 40 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 73.28%)2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID1689099Toxicity in BALB/c nude mouse transfected with human HeLa cells assessed as heart damage at 30 mg/kg/day, iv for 21 days by H&E staining based immunohistochemistry2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1875869Induction of microtubule fragmentation in human 518A2 cells at 25 nM measured after 24 hrs by immunofluorescence assay
AID1773166Induction of apoptosis in human A549 cells assessed as increase in necrotic cells at 500 nM measured after 24 hrs by PI/FITC analysis (Rvb = 0.365%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1771059Binding affinity to immobilized bovine brain tubulin by SPR assay
AID1399376Resistance index, ratio of IC50 for human SKOV3-MDR1-M6/6 cells to IC50 for human SKOV3 cells2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and preclinical evaluation of 5-methyl-N
AID84469The compound was evaluated for its cytotoxic potency against HT-29 cell line2000Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22
Design, synthesis and cytotoxic activities of naphthyl analogues of combretastatin A-4.
AID317728Inhibition of HIV1 reverse transcriptase2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID1600473Cytotoxicity against human MCR5 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID379679Inhibition of pRAD52 recombination repair gene/topoisomerase 1 deficient Saccharomyces cerevisiae RS321N carrying pRAD52 in glucose medium by microtiter plate assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID1427229Induction of microtubule disruption in human OVCAR3 cells assessed as nuclear contraction at 10 nM after 24 hrs by Alexa Fluor 647/DAPI staining based fluorescence microscopic method2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Combretastatin A4-β-Galactosyl Conjugates for Ovarian Cancer Prodrug Monotherapy.
AID449229Growth inhibition of rat A10 cells2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
AID382334Cytotoxicity against human OVCAR cells assessed as [3H]thymidine incorporation after 72 hrs by microplate scintillation counter2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin.
AID1508162Induction of apoptosis in human MCF7 cells assessed as viable cells at 2 uM after 24 hrs by Annexin-V FITC/propidium iodide staining-based FACS analysis (Rvb = 93.9%)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1514434Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth after 48 hrs by MTT assay
AID617010Antiproliferative activity against human SKOV3 cells2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID1608959Antiproliferative activity against human SEM cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.
AID1324106Cytotoxicity against human SW620 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1162830Induction of microtubule network disruption in human A549 cells at 25 nM incubated for 48 hrs by immunohistochemistry2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID737116Cytotoxicity against human A549 cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID68933Compound was evaluated against Human cell line pharynx FADU1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID269712Inhibition of tubulin polymerization2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID1285336Induction of apoptosis in human HT-29 cells assessed as viable cells at 10 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb=93.82%)2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID297425Inhibition of tubulin polymerization in presence of microtubule associated proteins after 30 mins2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
4- and 5-aroylindoles as novel classes of potent antitubulin agents.
AID1399372Induction of microtubule depolymerization in rat A10 cells after 18 hrs by indirect immunofluorescence method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and preclinical evaluation of 5-methyl-N
AID1435074Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 0.5 uM after 24 hrs by propidium iodide staining-based flow cytometric method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1317625Cell cycle arrest in human HepG2 cells assessed as decrease in G0/G1 phase at growth inhibitory IC50 measured after 24 hrs by propidium iodide-staining based FACS analysis2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1651877Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 5 uM incubated for 10 mins by scintillation counting relative to control2020Journal of natural products, 04-24, Volume: 83, Issue:4
Bioreductively Activatable Prodrug Conjugates of Combretastatin A-1 and Combretastatin A-4 as Anticancer Agents Targeted toward Tumor-Associated Hypoxia.
AID1401816Inhibition of porcine brain tubulin polymerization at 10 uM after 61 mins by spectroscopic analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis, and biological evaluation of 1,3-diarylisoquinolines as novel topoisomerase I catalytic inhibitors.
AID444160Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID455989Cytotoxicity against human Molt4/C8 cells after 2 days2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of tubulin polymerization.
AID1586358Antiproliferative activity against human HT-29 cells by MTT assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4.
AID1906242Induction of apoptosis in human HeLa cells assessed as late apoptotic cells at 1.5 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 5.22%)
AID1308544Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID567095Antiproliferative activity against human HCT15 cells after 72 hrs by MTS assay2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues.
AID1736453Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1766186Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Design, synthesis and biological evaluation of novel acridine and quinoline derivatives as tubulin polymerization inhibitors with anticancer activities.
AID1231337Inhibition of porcine brain tubulin polymerization at 3 uM measured for 1 hr by spectrofluorometer analysis2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4.
AID306519Cell cycle arrest in human M21 cells assessed as accumulation at G2/M phase at 0.125 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1411590Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1514432Cytotoxicity against human HeLa cells assessed as inhibition of cell growth after 48 hrs by MTT assay
AID1742933Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors.
AID143037Concentration required to inhibit proliferation of Human lung carcinoma NCI-H460 cell line2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.
AID214330Inhibition of colchicine binding to tubulin was evaluated only when polymerization IC50 <=1.0 uM1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
Antitumor agents. 155. Synthesis and biological evaluation of 3',6,7-substituted 2-phenyl-4-quinolones as antimicrotubule agents.
AID1401723Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and biological evaluation of N-substituted 3-oxo-1,2,3,4-tetrahydro-quinoxaline-6-carboxylic acid derivatives as tubulin polymerization inhibitors.
AID1330811Cytotoxicity against human A375 cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Design, synthesis, anticancer, antimicrobial activities and molecular docking studies of theophylline containing acetylenes and theophylline containing 1,2,3-triazoles with variant nucleoside derivatives.
AID1406348Cytotoxicity against HEK293T cells assessed as reduction in cell viability after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation.
AID243598Inhibition of 1 uM [3H]colchicine binding to tubulin at 5 uM2005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
AID502711Growth inhibition of human SR cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID691725Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as effect on ALP level at 50 mg/kg, ip qd after 21 days (Rvb = 107.6 +/- 0.8 IU/L)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID201880Compound was evaluated against Human cell line thyroid SW17361999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID1403590Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
AID494827Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 30 uM after 24 hrs by FACS analysis2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
Synthesis and anti-cancer activity of chalcone linked imidazolones.
AID778978Cytotoxicity against human SKOV3 cells after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and biological evaluation of indole-based, anti-cancer agents inspired by the vascular disrupting agent 2-(3'-hydroxy-4'-methoxyphenyl)-3-(3″,4″,5″-trimethoxybenzoyl)-6-methoxyindole (OXi8006).
AID40025Compound was evaluated against Human cell line pancreas BXPC-31999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID1832110Inhibition of tubulin polymerization (unknown origin) assessed as fluorescence intensity measured for 90 mins by DAPI based microplate reader2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID552573Induction of cell cycle arrest in human KB cells assessed as accumulation at G0/G1phase at 20 nM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 72.9%)2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis of antiproliferative flavones from calycopterin, major flavonoid of Calycopteris floribunda Lamk.
AID617009Displacement of [3H]colchicine from bovine brain tubulin in A-10 cells at 5 uM2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID1411796Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID1324091Cytotoxicity against human RPMI8226 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID314015Antiproliferative activity against human UACC62 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID383965Cytotoxicity against human MDA-MB-435 cells2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
2-(6-aryl-3(Z)-hexen-1,5-diynyl)anilines as a new class of potent antitubulin agents.
AID1832130Induction of apoptosis in human HeLa cells assessed as viable cells at 5 nM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 98.5 %)2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID1666248Inhibition of tubulin polymerization in human A549 cells assessed as disassembly of microtubule network at 0.6 uM incubated for 18 hrs by Hoechst33342 staining based confocal microscopic analysis2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID492259Antiproliferative activity against human Molt4/C8 cells after 2 days by coulter counting2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Substituted 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]thiophene derivatives as potent tubulin polymerization inhibitors.
AID444157Relative aqueous solubility at pH 7.4 by filter plate assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID494823Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs by FACS analysis2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
Synthesis and anti-cancer activity of chalcone linked imidazolones.
AID1809275Antiproliferative activity against human L-O2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
AID662352Inhibition of porcine brain tubulin polymerization after 30 mins by spectrophotometry2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID1647035Antitumor immunity against mouse H22 cells expressing TDO xenografted in ICR mouse assessed as increase in CD4+/CD8+ T-cell infiltration in tumor at 30 mg/kg, iv administered once daily for 21 consecutive days and measured after 21 days by immunohistochem2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1231333Anticancer activity against human U2OS cells assessed as reduction in cell proliferation at 2.5 to 5 uM after 48 hrs by WST-1 assay2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4.
AID1399378Antiproliferative activity against human wild-type Hela-beta3 cells after 72 hrs by sulforhodamine B assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and preclinical evaluation of 5-methyl-N
AID1608963Displacement of [3H]-colchicine from bovine brain tubulin at 5 uM incubated for 1 hr by relative to control2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.
AID94873Compound was evaluated against Human cell line colon KM20L21999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID1422793Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
AID502709Growth inhibition of human MOLT4 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1068612Growth inhibition of human SNB19 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1416659Cell cycle arrest in human A549 cells assessed as accumulation after 24 hrs by propidium iodide staining based flow cytometry2017MedChemComm, , Volume: 8, Issue:11
Design, Synthesis and Structure-Activity Relationships of (±)-Isochaihulactone Derivatives.
AID626624Cell cycle arrest in human M21 cells assessed as accumulation at G0/G1 phase at 5 times IC50 after 24 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 61%)2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID665830Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 2 uM after 48 hrs by annexin-V FITC/propidium iodide staining based FACS analysis2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID613263Antiproliferative activity against human HT-29 cells after 72 hrs by methylene blue assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and biological evaluation of 1-(4'-Indolyl and 6'-Quinolinyl) indoles as a new class of potent anticancer agents.
AID1206086Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay2015European journal of medicinal chemistry, Apr-13, Volume: 94Design, synthesis and biological evaluation of novel pyrazoline-containing derivatives as potential tubulin assembling inhibitors.
AID1550337Antiproliferative activity against human HT1080 cells measured after 72 hrs by MTT assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and bioevaluation of diarylpyrazoles as antiproliferative agents.
AID605778Antivasculogenic activity against human HT1080 cells xenografted in chicken chorioallantoic membrane assessed as inhibition of tumor growth at 3 ug per egg, iv measured on day 14 by CAM assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID1336755Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 100 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 78.5%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1757279Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1689097Induction of apoptosis in human HeLa cells assessed as mitochondrial membrane potential dissipation by measuring increase in green fluorescence intensity at 0.5 uM incubated for 24 hrs by JC-1 staining based fluorescence microscopic analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID286484Antiproliferative effect against mouse L210 cells after 2 days2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID1886256Antitumor activity against mouse H22 cells allografted in ICR mouse assessed as inhibition of tumor growth at 20 mg/kg, iv administered qd for 21 days measured after 12 days2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1126016Plasma concentration in C57BL/6 mouse at 5 mg/kg, po after 1 hr2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1338082Antiproliferative activity against human LoVo cells measured after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of cyclic-indole derivatives as anti-tumor agents via the inhibition of tubulin polymerization.
AID546571Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Synthesis and evaluation of azetidinone analogues of combretastatin A-4 as tubulin targeting agents.
AID490285Displacement of [3H]colchicine from tubulin2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
Structural determinants of resveratrol for cell proliferation inhibition potency: experimental and docking studies of new analogs.
AID1862612Antiproliferative activity against human SK-OV-3 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID771199Cell cycle arrest in human HT-29 cells assessed as accumulation at S phase at 25 nM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 24.39%)2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID1278673Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID1420993Antiproliferative activity against human HL60 cells after 72 hrs by XTT assay
AID670882Cytotoxicity against human HeLa cells after 48 hrs by WST-8 assay2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
AID658259Cytotoxicity against human HCT116 cells after 72 hrs using resazurin dye by microtiter plate fluorimeter analysis2012European journal of medicinal chemistry, Jun, Volume: 52Conformationnally restricted naphthalene derivatives type isocombretastatin A-4 and isoerianin analogues: synthesis, cytotoxicity and antitubulin activity.
AID1205510Antiproliferative activity against human HT-29 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.
AID1183717Cytotoxicity against human MESSA cells assessed as growth inhibition after 72 hrs by CellTitre-Glo assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID54295Inhibition of tubulin polymerization was determined at 1.2 mg/mL concentration2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis, anticancer activity, and inhibition of tubulin polymerization by conformationally restricted analogues of lavendustin A.
AID1308559Cytotoxicity against human A549/CDDP cells assessed as growth inhibition after 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1472470Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM after 10 mins by DEAE-cellulose filter method relative to control2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Quinazolinone-Based Anticancer Agents: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Tubulin Co-crystal Structure.
AID1647001Induction of apoptosis in human HepG2 cells assessed as live cells at 0.1 uM measured after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 95 %)2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID342519Cytotoxicity against mouse B16 cells assessed as cell viability after 48 hrs by MTT test2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Synthesis and biological evaluation of new disubstituted analogues of 6-methoxy-3-(3',4',5'-trimethoxybenzoyl)-1H-indole (BPR0L075), as potential antivascular agents.
AID1865676Inhibition of Arylsulfatase (unknown origin) using potassium p-nitrophenyl sulfate as substrate incubated for 5 mins2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.
AID1572257Antiproliferative activity against human Jurkat cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.
AID1906244Induction of apoptosis in human HeLa cells assessed as late apoptotic cells at 6 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 5.22%)
AID1336756Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 100 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 9.4%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID314020Antiproliferative activity against human PC3 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID479716Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Synthesis and antitumor activity of 1,5-disubstituted 1,2,4-triazoles as cis-restricted combretastatin analogues.
AID1411610Substrate activity at human OATP2B1 expressed in HEK293 cells assessed as compound uptake by HPLC-UV method relative to control2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID595725Inhibition of lamb tubulin assembly assessed as half inhibitory molar ratio of compound to tubulin by fluorimetry2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Synthesis and biological evaluation of 4-arylcoumarin analogues of combretastatins. Part 2.
AID1205513Antiproliferative activity against human MCF7 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.
AID1195358Displacement of [3H]colchicine from bovine brain tubulin assembly at 1 uM2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID290172Cytotoxicity against human CEM cells2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents.
AID1233618Growth inhibition of human HepG2 cells assessed as inhibition of cell proliferation after 24 hrs by MTT assay2015European journal of medicinal chemistry, Jun-24, Volume: 99Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin polymerization inhibitors.
AID1688957Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by alamar blue assay2020European journal of medicinal chemistry, Mar-01, Volume: 189β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells.
AID388079Cytotoxicity against human HBL100 cells after 72 hrs by MTT assay2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Synthesis and biological evaluation of polymethoxylated 4-heteroarylcoumarins as tubulin assembly inhibitor.
AID1402064Antiproliferative activity against mouse FM3A cells after 2 days by Coulter counter method2018European journal of medicinal chemistry, Jan-01, Volume: 1432-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.
AID273086Antiproliferative activity against human DMS79 cells after 72 hrs2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and structure-activity relationships of carbazole sulfonamides as a novel class of antimitotic agents against solid tumors.
AID306516Induction of apoptosis in human M21 cells at 0.125 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID643533Displacement of [3H]colchicine from bovine tubulin at 5 uM by DEAE-cellulose filter method2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Synthesis and evaluation of 1,5-disubstituted tetrazoles as rigid analogues of combretastatin A-4 with potent antiproliferative and antitumor activity.
AID1276129Inhibition of of bovine brain tubulin polymerization measured every 1 min for 30 mins by fluorescence assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID348407Displacement of [3H]colchicine from bovine brain tubulin at 5 uM2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID1408401Antitumor activity against mouse H22 cells implanted in ICR mouse assessed as tumor growth inhibition at 15 mg/kg, iv administered once daily for 21 consecutive days relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1886174Antiproliferative activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1400395Cell cycle arrest in CYP1A1 expressing human MCF7 cells assessed as accumulation at G0/G1 phase at 0.0010 uM after 24 hrs by flow cytometry (Rvb = 69%)2018Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
4-(3-Alkyl-2-oxoimidazolidin-1-yl)-N-phenylbenzenesulfonamides as new antimitotic prodrugs activated by cytochrome P450 1A1 in breast cancer cells.
AID1487504Antiproliferative activity against human HeLa cells after 48 hrs by sulforhodamine B assay2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Design and synthesis of 4-morpholino-6-(1,2,3,6-tetrahydropyridin-4-yl)-N-(3,4,5-trimethoxyphenyl)-1,3,5-triazin-2-amine analogues as tubulin polymerization inhibitors.
AID1778188Antiproliferative activity against human T47D cells assessed as cell growth inhibition after 48 hrs by MTT assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines.
AID281360Stability in phosphate buffer at pH 7.42007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1411591Cytotoxicity against human DU145 cells assessed as reduction in cell viability up to 20 uM after 24 hrs by MTT assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID474639Cell cycle arrest in human HeLa cells assessed as accumulation of cells in G2/M phase at 0.2 uM after 24 hrs using propidium iodide by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID397293Inhibition of tubulin polymerization assessed as blockade of microtubule assembly2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Isocombretastatins a versus combretastatins a: the forgotten isoCA-4 isomer as a highly promising cytotoxic and antitubulin agent.
AID590610Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 1 uM after 48 hrs by flow cytometric analysis2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Design, synthesis, and biological evaluation of novel γ-carboline ketones as anticancer agents.
AID502714Growth inhibition of human NCI-H322M cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1552971Inhibition of bovine brain tubulin polymerization measured every 1 min for 60 mins by turbidimetry based microplate reader analysis2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Synthesis and biological evaluation of 7-methoxy-1-(3,4,5-trimethoxyphenyl)-4,5-dihydro-2H-benzo[e]indazoles as new colchicine site inhibitors.
AID1595697Inhibition of [3H]colchicine binding to biotinylated porcine tubulin at 5 uM in presence of GTP after 2 hrs by scintillation proximity assay relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID266932Inhibition of tubulin polymerization in bovine brain by tubulin assembly assay2006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-5-aryl thiophenes as a new class of potent antitubulin agents.
AID492262Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetry analysis2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Substituted 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]thiophene derivatives as potent tubulin polymerization inhibitors.
AID1351614Inhibition of tubulin polymerization in human SKOV3 cells assessed as micronuclei formation at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID415689Inhibition of sheep tubulin polymerization2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
Synthesis and biological evaluation of cis-locked vinylogous combretastatin-A4 analogues: derivatives with a cyclopropyl-vinyl or a cyclopropyl-amide bridge.
AID1317613Induction of apoptosis in human HepG2 cells assessed as increase in apoptotic cells at growth inhibitory IC50 measured after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1403613Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 100 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.7%)2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
AID427175Antiproliferative activity against mouse L1210 cells after 2 days by coulter counter method2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization.
AID1064418Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID761831Cytotoxicity against human MCF7 cells after 96 hrs by sulforhodamine B assay2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity.
AID779090Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
The synthesis and anticancer activity of analogs of the indole phytoalexins brassinin, 1-methoxyspirobrassinol methyl ether and cyclobrassinin.
AID780970Displacement of [3H]-colchicine from biotin-labeled tubulin (unknown origin) after 2 hrs by scintillation proximity assay2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Furanylazaindoles: potent anticancer agents in vitro and in vivo.
AID1637524Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 40 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 17.56%)2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID751508Resistance ratio of IC50 for human HeLa cells expressing beta-3 tubulin to IC50 for human HeLa cells2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.
AID1773151Cell cycle arrest in human U-251 cells assessed as G0/G1 phase at 200 nM measured after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 67.34%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1906175Antiproliferation activity against human SiHa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
AID1486480Inhibition of tubulin polymerization in human HT-29 cells assessed as microtubule disruption by measuring scattered short microtubule fragment in cytoplasm at 20 nM after 24 hrs by DAPI staining based immunofluorescence microscopic analysis2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis, biological evaluation and molecular modeling of imidazo[1,2-a]pyridine derivatives as potent antitubulin agents.
AID1585988Cytotoxicity against human Hs578T cells after 72 hrs by MTT assay
AID379682Inhibition of Saccharomyces cerevisiae RS188 expressing wild type erg6 by agar diffusion assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID1126001Cytotoxicity against human MDA-MB-231 cells after 72 hrs by resazurin based fluorescence assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID397289Cytotoxicity against human HCT116 cells after 72 hrs2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
Isocombretastatins a versus combretastatins a: the forgotten isoCA-4 isomer as a highly promising cytotoxic and antitubulin agent.
AID1162816Cytotoxicity against human A549 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID1862615Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID45940Compound was evaluated against Human cell line CNS SF-2951999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID1711841Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID607526Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 1 uM after 48 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues.
AID1334730Antiproliferative activity against human HepG2 assessed as reduction in cell viability measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility.
AID730211Cell cycle arrest in human A549 cells assessed as accumulation at G1 phase at 0.01 uM after 24 hrs by propidium iodide staining-based FACS flow cytometric analysis (Rvb = 53.57%)2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Synthesis and structure-activity relationships of N-methyl-5,6,7-trimethoxylindoles as novel antimitotic and vascular disrupting agents.
AID1698825Binding affinity to tubulin (unknown origin) assessed as change in gibbs free energy2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Computational modeling and target synthesis of monomethoxy-substituted o-diphenylisoxazoles with unexpectedly high antimitotic microtubule destabilizing activity.
AID214178Inhibition of radiolabeled [3H]colchicine binding to tubulin at a concentration of 5 uM of the compound2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.
AID1381555Cytotoxicity against human PANC1 cells after 72 hrs by XTT assay2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
New somatostatin-drug conjugates for effective targeting pancreatic cancer.
AID1891177Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth by MTT assay
AID1276119Cytotoxicity against human HT1080 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1068590Growth inhibition of human A498 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1068605Growth inhibition of human SK-MEL-2 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
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Antineoplastic agents. 578. Synthesis of stilstatins 1 and 2 and their water-soluble prodrugs.
AID1055625Cytotoxicity against human DU145 cells after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis of structurally diverse benzosuberene analogues and their biological evaluation as anti-cancer agents.
AID1832148Metabolic stability in human liver microsomes assessed as half life2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID214709Inhibition of [3H]colchicine binding to tubulin at a concentration of 5.0 uM2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
The synthesis and tubulin binding activity of thiophene-based analogues of combretastatin A-4.
AID340146Growth inhibition of human KB cells after 72 hrs by methylene blue dye assay2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.
AID1064396Growth inhibition of human UACC257 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1882980Induction of cell cycle arrest in human MDA-MB-231 cells assessed as decrease in S phase cells at 10 uM incubated for 24 hrs by PI staining based flow cytometric analysis (Rvb = 16.61%)2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and evaluation of a novel series of mono-indolylbenzoquinones derivatives for the potential treatment of breast cancer.
AID256880Cell cycle arrest in A431 cells by accumulation at G2/M phase cell at 0.1uM2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors.
AID382336Cytotoxicity against human WM239 cells assessed as [3H]thymidine incorporation after 72 hrs by microplate scintillation counter2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin.
AID1689070Inhibition of tubulin polymerization in human HeLa cells assessed as disruption of microtubule network organization at 0.5 uM measured after 24 hrs by DAPI staining based immunofluorescence method2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID685208Growth inhibition of human OVCAR8 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1572259Inhibition of bovine brain tubulin polymerization after 20 mins2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.
AID1565957Metabolic stability in Sprague-Dawley rat liver microsomes assessed as parent compound remaining after 90 mins in presence of NADPH by HPLC-UV-MS analysis
AID427181Displacement of [3H]colchicine from bovine brain tubulin at 1 uM2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization.
AID1240942Antiproliferative activity against human KB cells assessed as cell growth inhibition by SRB assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines as tubulin polymerization inhibitors.
AID1183724Induction of apoptosis in human HeLa cells assessed as short, aberrantly shaped, tripolar or multipolar microtubule microtubule at 20 nM by immunofluorescence analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID1195357Inhibition of bovine brain tubulin assembly2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID1851619Induction of apoptosis in human MDA-MB-231 cells assessed as viable cells at 10 uM by Annexin V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 93.6 %)2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives.
AID1646993Antiproliferative activity against human U87 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1646998Cell cycle arrest in human HepG2 cells assessed as accumulation at G1 phase at 0.1 uM measured after 24 hrs by RNase A/propidium iodide staining based flow cytometry (Rvb = 60.73 %)2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID269722Cell cycle arrest in SHSY5Y cells by accumulation at S phase after 4 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID449216Inhibition of [3H]colchicine binding to bovine tubulin at 1 uM after 10 mins by DEAE-cellulose filter method2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
AID421857Antitumor activity against human BxPC3 cells by sulforhodamine B assay2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Antineoplastic agents. 578. Synthesis of stilstatins 1 and 2 and their water-soluble prodrugs.
AID1353631Antiproliferative activity against human HeLa cells after 2 days by MTT assay2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID1709306Inhibition of bovine brain tubulin assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by turbidimetry-based spectrophotometric method2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1462792Inhibition of tubulin (unknown origin) polymerization2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Triazole tethered isatin-coumarin based molecular hybrids as novel antitubulin agents: Design, synthesis, biological investigation and docking studies.
AID1514435Cytotoxicity against HEK293 cells assessed as inhibition of cell growth after 48 hrs by MTT assay
AID293351Cell cycle arrest in HMEC1 cells assessed as accumulation at S phase at 100 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID452431Cell cycle arrest in human K562 cells assessed as accumulation at G0/G1 phase at 20 nM after 24 hrs by propidium iodide staining-based flow cytometry2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: synthesis and biological evaluation of antivascular activity.
AID685169Growth inhibition of human CCRF-CEM cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1400394Cell cycle arrest in CYP1A1 expressing human MCF7 cells assessed as accumulation at sub-G1 phase at 0.0010 uM after 24 hrs by flow cytometry (Rvb = 2.9%)2018Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
4-(3-Alkyl-2-oxoimidazolidin-1-yl)-N-phenylbenzenesulfonamides as new antimitotic prodrugs activated by cytochrome P450 1A1 in breast cancer cells.
AID1773153Cell cycle arrest in human U-251 cells assessed as S phase at 200 nM measured after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 18.23%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1188096Inhibition of tubulin (unknown origin) polymerization after 1 hr by spectrophotometry2014European journal of medicinal chemistry, Oct-06, Volume: 85Chalcone based azacarboline analogues as novel antitubulin agents: design, synthesis, biological evaluation and molecular modelling studies.
AID1757286Aqueous solubility of the compound in phosphate buffer at pH 7.4 by HPLC-UV analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1686598Growth inhibition of human HeLa cells2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Potent Antitumor Activities and Structure Basis of the Chiral β-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin.
AID1600492Inhibition of tubulin polymerization in human HCT116 cells assessed as multipolar spindle formation at antiproliferative IC50 incubated for 24 hrs by DAPI staining based spinning disk confocal microscopic method2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID43459In vitro cytotoxic activity tested against human breast cancer MCF/ADR cell line2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.
AID613261Antiproliferative activity against human KB-VIN10 cells over-expressing P-gp 170/MDR1 after 72 hrs by methylene blue assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and biological evaluation of 1-(4'-Indolyl and 6'-Quinolinyl) indoles as a new class of potent anticancer agents.
AID1200590Growth inhibition of human HT-29 cells by MTT assay2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Quantum chemistry calculation-aided structural optimization of combretastatin A-4-like tubulin polymerization inhibitors: improved stability and biological activity.
AID214343Percent inhibitory activity (5 uM) against colchicine binding to tubulin in mitosis in MCF-7 breast cancer cells2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Antineoplastic agents. 487. Synthesis and biological evaluation of the antineoplastic agent 3,4-methylenedioxy-5,4'-dimethoxy-3'-amino-Z-stilbene and derived amino acid amides.
AID474623Inhibition of tubulin polymerization at 20 uM relative to control2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1689080Induction of apoptosis in human HeLa cells assessed as upregulation of caspase-3 protein expression at 0.5 uM measured after 24 hrs by western blot analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID271658Inhibition of tubulin polymerization2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents.
AID106302Cytotoxic activity against MEL-28 cell line2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
A new family of quinoline and quinoxaline analogues of combretastatins.
AID1330808Cytotoxicity against human A549 cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Design, synthesis, anticancer, antimicrobial activities and molecular docking studies of theophylline containing acetylenes and theophylline containing 1,2,3-triazoles with variant nucleoside derivatives.
AID218986Inhibitory activity was determined against tubulin polymerization of bovine brain tubulin1998Bioorganic & medicinal chemistry letters, Dec-01, Volume: 8, Issue:23
Novel B-ring modified combretastatin analogues: syntheses and antineoplastic activity.
AID746668Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Design, synthesis, cytotoxic evaluation and tubulin inhibitory activity of 4-aryl-5-(3,4,5-trimethoxyphenyl)-2-alkylthio-1H-imidazole derivatives.
AID1401725Antiproliferative activity against human K562 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and biological evaluation of N-substituted 3-oxo-1,2,3,4-tetrahydro-quinoxaline-6-carboxylic acid derivatives as tubulin polymerization inhibitors.
AID1711844Antiproliferative activity against human COLO 205 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID1325846Inhibition of tubulin polymerization in human MCF7 cells assessed as suppression of protein assembly after 15 mins by spectrophotometric analysis2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Scaffold-Hopping of Aurones: 2-Arylideneimidazo[1,2-
AID1317578Growth inhibition of human K562 cells measured after 72 hrs by MTT assay2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1906190Vascular disruptive activity against HUVEC-formed vascular tube assessed as damage of vascular tube on matrigel substratum at 0.2 uM measured after 2 hrs
AID442546Cytotoxicity against human A549 cells after 72 hrs by XTT assay2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Exploring the effect of 2,3,4-trimethoxy-phenyl moiety as a component of indolephenstatins.
AID1466670Inhibition of tubulin polymerization in interphase stage of human MDA-MB-231 cells at 0.2 uM after 24 hrs by DAPI staining based confocal microscopic analysis2017Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12
Antitubulin effects of aminobenzothiophene-substituted triethylated chromones.
AID1200595Antitumor activity against human HT-29 cells xenografted in BALB/c mouse assessed as reduction in tumor volume at 50 mg/kg, ip administered once daily for 18 days2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Quantum chemistry calculation-aided structural optimization of combretastatin A-4-like tubulin polymerization inhibitors: improved stability and biological activity.
AID1730576Cell cycle arrest in human M21 cells assessed as accumulation at G2/M phase at 11 nM measured after 24 hrs by DAPI staining based flow cytometry (Rvb = 13.4%)2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID780973Inhibition of bovine brain MAP-rich tubulin polymerization measured every 30 secs for 30 mins by turbidometric method2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Furanylazaindoles: potent anticancer agents in vitro and in vivo.
AID1153044Inhibition of bovine brain tubulin polymerization after 15 mins by spectrophotometry2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis, biological evaluation and molecular docking studies of trans-indole-3-acrylamide derivatives, a new class of tubulin polymerization inhibitors.
AID1352577Induction of microtubule depolymerization in human A549 cells assessed as scattered short microtubule fragment formation in cytoplasm at 30 nM after 24 hrs by DAPI staining based immunofluorescence microscopic method2018European journal of medicinal chemistry, Feb-25, Volume: 146Synthesis and biological evaluation of 4,6-diphenyl-2-(1H-pyrrol-1-yl)nicotinonitrile analogues of crolibulin and combretastatin A-4.
AID1411602Cytotoxicity against HEK293 cells assessed as reduction in cell viability up to 200 uM after 10 mins by MTT assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID387315Displacement of [3H]colchicine from bovine brain tubulin at 1 uM2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.
AID293333Antiproliferative activity against human HL60 cells2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID1773137Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1233573Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model.
AID1064426Growth inhibition of human A549 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1736457Inhibition of tubulin polymerization (unknown origin) measured every 2 mins for 60 mins by spectrophotometric method2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID340151Displacement of [3H]colchicine from microtubule associated protein rich tubulin at 1 uM2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.
AID1402685Antiproliferative activity against human HeLa cells after 24 hrs by SRB assay
AID695148Inhibition of pig tubulin polymerization by spectrophotometry2012Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21
Novel cyanocombretastatins as potent tubulin polymerisation inhibitors.
AID617012Relative resistance ratio of IC50 for MDR-1-6/6 overexpressing human SKOV3 cells to IC50 for human SKOV3 cells2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID1233596Induction of cell cycle arrest in human M21 cells assessed as cells accumulation at G0/G1 phase at 10 nM after 24 hrs by flow cytometry (Rvb = 54.5%)2015European journal of medicinal chemistry, Jul-15, Volume: 100Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model.
AID1057195Antiangiogenic activity in human HT-29 cells assessed as inhibition of VEGF production at < IC50 after 72 hrs by ELISA relative to control2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity.
AID143034Antiproliferative activity against the human non small cell lung carcinoma cell line NCI-H4602002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
AID1310201Cell cycle arrest in combretastatin A-4 resistant human HT-29 cells assessed as accumulation at G2 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 15.6 +/- 0.1%)2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1126010Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at S phase at 1 uM after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 25.70%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID512243Cell cycle arrest in human A375 cells assessed as accumulation at G0/G1 phase at 4 uM after 24 hrs using propidium iodide staining by FACS2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis and biological evaluation of 3,5-diaryl-isoxazoline/isoxazole-pyrrolobenzodiazepine conjugates as potential anticancer agents.
AID1736445Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID514406Displacement [3H]colchicine from tubulin at 50 uM2010Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents.
AID1550335Antiproliferative activity against human SGC7901 cells measured after 72 hrs by MTT assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and bioevaluation of diarylpyrazoles as antiproliferative agents.
AID1809277Induction of microtubule depolymerization in human MCF7 cells at 10 uM measured every 5 mins for 60 mins by spectrophotometric method
AID1064413Growth inhibition of human HT-29 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1694123Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects.
AID1891178Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by MTT assay
AID1597924Inhibition of tubulin polymerization (unknown origin) by spectrophotometric method2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.
AID1157576Cytotoxicity against human NCI-ADR-RES cells assessed as inhibition of cell proliferation by SRB assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.
AID746667Cytotoxicity against human HT-29 cells assessed as growth inhibition after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Design, synthesis, cytotoxic evaluation and tubulin inhibitory activity of 4-aryl-5-(3,4,5-trimethoxyphenyl)-2-alkylthio-1H-imidazole derivatives.
AID657908Displacement of [3H]colchicine from tubulin at 1 uM after 10 mins2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID1637527Inhibition of porcine brain tubulin polymerization measured at 1 min interval for 1 hr by fluorescence plate reader assay2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID1647043Toxicity in immunocompetent BALB/c nude mouse xenografted with human A549 cells assessed as effect on body weight at 30 mg/kg, iv administered once daily for 29 consecutive days measured every 2 days for 29 days2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1886188Inhibition of tubulin polymerization (unknown origin) preincubated for 15 mins followed by PEG and GTP addition measured after 30 mins by spectrophotometric method2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID1334734Antiproliferative activity against human MCF7 assessed as reduction in cell viability measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility.
AID771205Inhibition of tubulin (unknown origin) polymerization measured for 60 mins2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID1324134Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID319828Inhibition of tubulin assembly2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and antitumor activity of benzils related to combretastatin A-4.
AID729787Growth inhibition of human NCI60 cells2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Identification of diaryl 5-amino-1,2,4-oxadiazoles as tubulin inhibitors: the special case of 3-(2-fluorophenyl)-5-(4-methoxyphenyl)amino-1,2,4-oxadiazole.
AID1757885Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 5 uM relative to control2021Bioorganic & medicinal chemistry letters, 06-01, Volume: 41Novel pyrazolo[4,3-d]pyrimidine microtubule targeting agents (MTAs): Synthesis, structure-activity relationship, in vitro and in vivo evaluation as antitumor agents.
AID281355Cmax in iv dosed Swiss Albino mouse plasma2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1064374Growth inhibition of human MDA-MB-468 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1179654Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design, synthesis and biological evaluation of (E)-3-(3,4-dihydroxyphenyl)acrylylpiperazine derivatives as a new class of tubulin polymerization inhibitors.
AID1760384Antiproliferative activity against human MCF7 cells incubated for 24 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020).
AID150221Compound was evaluated against P388 mouse Leukemia cell line1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID1336751Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1726857Antiproliferative activity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay2020European journal of medicinal chemistry, Feb-01, Volume: 187The discovery of novel indazole derivatives as tubulin colchicine site binding agents that displayed potent antitumor activity both in vitro and in vivo.
AID771208Cytotoxicity against vincristine-resistant human KB cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID1535572Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Synthesis, biological evaluation and molecular docking of benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives as novel tubulin polymerization inhibitors.
AID761820Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Correlation of hydrogen-bonding propensity and anticancer profile of tetrazole-tethered combretastatin analogues.
AID1686596Growth inhibition of human MDA-MB-231 cells2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Potent Antitumor Activities and Structure Basis of the Chiral β-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin.
AID721881Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID221812Cytotoxicity against human HT-29 colon cell line.1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Synthesis and evaluation of analogues of (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene as potential cytotoxic and antimitotic agents.
AID1689134Cytotoxicity against multidrug resistant human KB-V1 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.
AID616983Antiproliferative activity against human BT549 after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1717479Cell cycle arrest in human HT-1080 cells assessed as accumulation at G0/G1 phase at 0.025 uM measured after 12 hrs by propidium iodide staining based flow cytometry (Rvb = 43.79%)
AID605780Toxicity against fertilized chicken embryo assessed as mortality at 3 ug per egg, iv by CAM assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID1435071Cell cycle arrest in human HT29-D4 cells assessed as accumulation at G1 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1435084Cell cycle arrest in human HT29-D4 cells assessed as accumulation at sub-G1 phase at 0.5 uM after 24 hrs by propidium iodide staining-based flow cytometric method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID727481Cytotoxicity against mouse B16 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
Synthesis and biological evaluation of enantiomerically pure cyclopropyl analogues of combretastatin A4.
AID536484Displacement of [3H]colchicine from bovine brain tubulin at 1 uM after 10 mins2010Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance.
AID1917301Antiproliferative activity against human HT-29 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID1294619Cytotoxicity against human MCF7 cells assessed as reduction in cell growth after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, biological evaluation and molecular docking studies of 2-amino-3,4,5-trimethoxyaroylindole derivatives as novel anticancer agents.
AID1757274Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1317576Growth inhibition of human HepG2 cells measured after 72 hrs by MTT assay2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID685359Growth inhibition of human Caki1 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1475519Inhibition of [3H]-colchicine binding to tubulin (unknown origin) at 1 uM after 10 mins relative to control2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
In Vivo and Mechanistic Studies on Antitumor Lead 7-Methoxy-4-(2-methylquinazolin-4-yl)-3,4-dihydroquinoxalin-2(1H)-one and Its Modification as a Novel Class of Tubulin-Binding Tumor-Vascular Disrupting Agents.
AID214171Effect on the binding of radiolabeled [3H]colchicine to tubulin1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization.
AID403642Cytotoxicity against human BxPC3 cells after 48 hrs by sulforhodamine B assay2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID657909Displacement of [3H]colchicine from tubulin at 10 uM after 10 mins2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID1235365Displacement of 82.8 +/- 0.9 uM of [3H]colchicine from biotin-labeled tubulin (unknown origin) after 2 hrs by scintillation proximity assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes.
AID1875870Induction of microtubule fragmentation in human 518A2 cells assessed as appearance of area with dorsal stress fibre at 25 nM measured after 24 hrs by immunofluorescence assay
AID1165179Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Design and synthesis of pironetin analogue/combretastatin A-4 hybrids containing a 1,2,3-triazole ring and evaluation of their cytotoxic activity.
AID1435088Induction of mitosis in human HT29-D4 cells at 0.5 uM after 24 hrs by Draq5 staining-based confocal fluorescence microscopic method (Rvb = 3 +/- 0.6%)2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1500305Inhibition of tubulin polymerization (unknown origin)2017European journal of medicinal chemistry, Sep-29, Volume: 138An overview of benzo[b]thiophene-based medicinal chemistry.
AID281365Apoptosis in strongly adherent human ECV304 cells at 100 nM assessed as DNA fragmentation2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1534369Inhibition of [3H]colchicine binding to biotinylated porcine tubulin at 5 uM after 2 hrs by scintillation proximity assay relative to control2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
AID1517356Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTS assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Design and synthesis of (2-(phenylamino)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone analogues as potent anti-tubulin polymerization agents.
AID1458815Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1198222Antivascular activity in human EAhy926 cells assessed as concentration require to adopt rounding shape after 2 hrs by microscopic analysis2015European journal of medicinal chemistry, Mar-26, Volume: 93Antivascular and anti-parasite activities of natural and hemisynthetic flavonoids from New Caledonian Gardenia species (Rubiaceae).
AID265417Antiproliferative activity against human IGROV1 cells2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID1693359Antiproliferative activity against human HeLa cells assessed as decrease in cell growth measured after 48 hrs by SRB method2021Bioorganic & medicinal chemistry, 01-01, Volume: 29The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
AID461025Inhibition of tubulin in rat A10 cells assessed as induction of cellular microtubule disassembly after 18 hrs by indirect immunofluorescence technique2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
A boronic acid chalcone analog of combretastatin A-4 as a potent anti-proliferation agent.
AID1612613Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1235360Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes.
AID1689094Induction of apoptosis in human HeLa cells assessed as late apoptotic cells at 0.5 uM measured after 24 hrs by Annexin-V-FITC and PI staining based flow cytometry (Rvb = 0.199%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1294483Growth inhibition of human Caki1 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID721884Cytotoxicity against human MCF7 cells assessed as growth inhibition by trypan blue exclusion assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID247231Growth inhibition against human lung-NSC NCI-H460 cell line2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID1773175Induction of apoptosis in human U-251 cells assessed as increase in viable cells at 200 nM measured after 24 hrs by PI/FITC analysis (Rvb = 98.3%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID383959Cytotoxicity against human K562 cells2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
2-(6-aryl-3(Z)-hexen-1,5-diynyl)anilines as a new class of potent antitubulin agents.
AID1917303Antiproliferative activity against human NCI-H1299 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID1064390Growth inhibition of human NCI-ADR-RES cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1285323Cell cycle arrest in human HT-29 cells assessed as accumulation at G0/G1 phase at 10 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 83.01%)2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID1628400Growth inhibition of human PC3 cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Design, Synthesis, and Biological Evaluation of 1-Methyl-1,4-dihydroindeno[1,2-c]pyrazole Analogues as Potential Anticancer Agents Targeting Tubulin Colchicine Binding Site.
AID643528Cytotoxicity against human HL60 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Synthesis and evaluation of 1,5-disubstituted tetrazoles as rigid analogues of combretastatin A-4 with potent antiproliferative and antitumor activity.
AID607281Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID1757278Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1647033Toxicity in ICR mouse xenografted with mouse H22 cells assessed as effect on heart damage or inflammation at 30 mg/kg, iv administered once daily for 21 consecutive days measured after 21 days by hematoxylin-eosin staining based fluorescence microscopy2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID617008Displacement of [3H]colchicine from bovine brain tubulin in A-10 cells at 1 uM2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID1411609Substrate activity at human OATP1B3 expressed in HEK293 cells assessed as compound uptake by HPLC-UV method2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1713788Induction of cell cycle arrest in human KB-VIN cells assessed as abnormal multipolar spindles at 0.2 uM incubated for 24 hrs by DAPI staining based confocal microscopy2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Triethylated chromones with substituted naphthalenes as tubulin inhibitors.
AID1585984Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
AID1157569Inhibition of Abl1 (unknown origin) assessed as incorporation of [32P] gamma-ATP in to myelin basic protein after 30 mins by autoradiographic analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.
AID1263263Cytotoxicity against human SF295 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1411607Substrate activity at human OAT1 expressed in HEK293 cells assessed as compound uptake by HPLC-UV method2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1059985Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured for 20 mins by turbidometric analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
AID1119739Displacement of [3H]-Colchicine from tubulin (unknown origin) at 5 uM relative to control2012MedChemComm, Jun, Volume: 3, Issue:6
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
AID1688959Selectivity index, ratio of IC50 for human MCF7 cells to IC50 for human HT-29 cells assessed as reduction in cell viability after 72 hrs by alamar blue assay2020European journal of medicinal chemistry, Mar-01, Volume: 189β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells.
AID93838Compound was tested for cell arrest at G2/M phase at 25 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID1882894Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID502707Growth inhibition of human HL-60(TB) cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1555136Cytotoxicity against human DU145 cells assessed as growth inhibition measured after 48 hrs by SRB assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.
AID1057119Chemical stability of the compound in PBS at pH 7.4 assessed as compound remaining after 6.5 hrs by HPLC analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID269711Cytotoxicity against SHSY5Y cell line by MTT assay2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID1435065Cytotoxicity against human HT29-D4 cells assessed as growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID1766187Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Design, synthesis and biological evaluation of novel acridine and quinoline derivatives as tubulin polymerization inhibitors with anticancer activities.
AID502755Inhibition of tubulin polymerization2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID502733Growth inhibition of human SK-MEL-28 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID474637Cell cycle arrest in human HeLa cells assessed as accumulation of cells in S phase at 2.2 uM after 24 hrs using propidium iodide by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1736449Antiproliferative activity against human LO2 cells incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1906250Induction of apoptosis in human HeLa cells assessed as necrotic cells at 6 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 0.45%)
AID674209Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Discovery and optimization of a series of 2-aryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazoles as novel anticancer agents.
AID685379Inhibition of c-Jun protein expression in human MCF7 cells at 4 uM after 24 hrs by Western blot analysis2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1317588Antiproliferative activity against CA-4-resistant human A549 cells measured after 72 hrs by MTT assay2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1737818Metabolic stability in human liver microsomes assessed as parent compound remaining at 10 uM measured after 60 mins in presence of NADPH by LC/MS/MS analysis2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID1535574Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Synthesis, biological evaluation and molecular docking of benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives as novel tubulin polymerization inhibitors.
AID1738823Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors.
AID277279Cytotoxicity against ZR-75-1 cell line2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Highly potent triazole-based tubulin polymerization inhibitors.
AID730210Inhibition of tubulin polymerization in human A549 cells at 0.1 uM after 6 hrs by Western blotting analysis (Rvb = 46%)2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Synthesis and structure-activity relationships of N-methyl-5,6,7-trimethoxylindoles as novel antimitotic and vascular disrupting agents.
AID1635272Inhibition of [3H]colchicine binding to tubulin in bovine brain homogenate at 5 uM incubated for 10 mins by DEAE-cellulose filter assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID403646Cytotoxicity against human KM20L2 cells after 48 hrs by sulforhodamine B assay2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID1399377Antiproliferative activity against human HeLa cells after 72 hrs by sulforhodamine B assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and preclinical evaluation of 5-methyl-N
AID1432893Growth inhibition of human MCF10A cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Development of a novel near-infrared fluorescent theranostic combretastain A-4 analogue, YK-5-252, to target triple negative breast cancer.
AID1518088Induction of apoptosis in human MDA-MB-468 cells assessed as late apoptotic cells at 100 nM after 72 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 1.03 to 1.59%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1205509Antiproliferative activity against human A549 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.
AID1068591Growth inhibition of human ACHN cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1351604Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells at G2/M phase at 0.1 to 1 uM after 24 hrs by propidium iodide staining-based FACS analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1427221Cytotoxicity against human OVCAR3 cells assessed as reduction in cell viability after 72 hrs by WST8 assay2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Combretastatin A4-β-Galactosyl Conjugates for Ovarian Cancer Prodrug Monotherapy.
AID751512Inhibition of MDR1 (unknown origin) transfected in human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.
AID1873681Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID1237726Cytotoxicity against human MESSA/DX5 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID1064383Growth inhibition of human RXF393 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1886189Inhibition of [3H]Colchicine binding to tubulin (unknown origin) at 1 uM measured after 2 hrs by scintillation counting method relative to control2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID617005Antiproliferative activity against human MDA-MB-435 cells by SRB assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID1533680Antiangiogenic activity in Leghorn chicken embryo chorioallantoic membrane assessed as disruption of bigger blood vessels at 2.5 nmol after 6 hrs by light microscopic analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163New naphthopyran analogues of LY290181 as potential tumor vascular-disrupting agents.
AID1694127Cytotoxicity against human WI-38 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects.
AID1741568Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Synthesis, and biological evaluation of 3,6-diaryl-[1,2,4]triazolo[4,3-a]pyridine analogues as new potent tubulin polymerization inhibitors.
AID256881Cell cycle arrest in A431 cells by accumulation at G2/M phase cell2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors.
AID1064428Growth inhibition of human SR cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1068616Growth inhibition of human KM12 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1585995Cell cycle arrest in human BT549 cells assessed as accumulation of cells at G0/G1 phase at 8 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 65.28%)
AID1612628Inhibition of porcine brain tubulin polymerization preincubated for 30 mins and measured every 2 mins for 60 mins by spectrophotometric analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID616975Antiproliferative activity against human DU145 after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID643530Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Synthesis and evaluation of 1,5-disubstituted tetrazoles as rigid analogues of combretastatin A-4 with potent antiproliferative and antitumor activity.
AID492257Antiproliferative activity against mouse L1210 cells after 2 days by coulter counting2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Substituted 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]thiophene derivatives as potent tubulin polymerization inhibitors.
AID247272Growth inhibition against human pancreas carcinoma cell line (BxPC-3)2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID1351617Inhibition of tubulin polymerization in human MCF7 cells assessed as micronuclei formation at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID78604Inhibition of human HCT-15 (human colon adenocarcinoma, MDR positive) cell growth2002Journal of medicinal chemistry, Apr-11, Volume: 45, Issue:8
Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation.
AID1338587Cytotoxicity against human HT-29 cells assessed as growth inhibition after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of novel alkylsulfanyl-1,2,4-triazoles as cis-restricted combretastatin A-4 analogues.
AID15180921-Octanol/water partition coefficient, log P of compound at 1 mg after 1 hr by HPLC analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID767880Inhibition of bovine brain tubulin polymerization after 20 mins2013Journal of natural products, Sep-27, Volume: 76, Issue:9
Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.
AID1628411Displacement of [3H]colchicine from biotinylated porcine tubulin at 5 uM incubated for 2 hrs by competition scintillation proximity2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Design, Synthesis, and Biological Evaluation of 1-Methyl-1,4-dihydroindeno[1,2-c]pyrazole Analogues as Potential Anticancer Agents Targeting Tubulin Colchicine Binding Site.
AID1600481Induction of cell cycle arrest in human CCRF-CEM cells assessed as accumulation at S phase at antiproliferative IC50 incubated for 24 hrs by PI staining based flow cytometric analysis (Rvb = 46%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1195359Displacement of [3H]colchicine from bovine brain tubulin assembly at 5 uM2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID1771468Inhibition of tubulin polymerization (unknown origin) measured after 1 min by fluorescence assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID629599Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetry2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID1637515Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID306515Cell cycle arrest in human M21 cells assessed as accumulation at G2/M phase at 0.050 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1405395Antimigratory activity against human SKOV3 cells assessed as wound closure at 160 nM after 24 hrs by microscopy based scratch wound assay (Rvb = 79.5 +/- 2.8%)2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID474635Cell cycle arrest in human HeLa cells assessed as accumulation of cells in S phase at 0.02 uM after 24 hrs using propidium iodide by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID685204Growth inhibition of human IGROV1 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1906176Antiproliferation activity against human MS751 cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
AID1711865Induction of mitochondrial membrane potential loss in human MCF7 cells assessed as cell population with mitochondrial membrane potential collapse at 50 nM measured after 48 hrs by JC-1 staining based flow cytometry (Rvb = 0.7 %)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID1351654Inhibition of tubulin polymerization in human A431 cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1431178Growth inhibition of human HeLa cells over expressing beta3-tubulin measured after 96 hrs by sulforhodamine B assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
AID1351618Inhibition of tubulin polymerization in human MDA-MB-231 cells assessed as micronuclei formation at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1508161Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells at 2 uM after 24 hrs by Annexin-V FITC/propidium iodide staining-based FACS analysis (Rvb = 0.5%)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1753047Antiangiogenic activity in endothelial cells assessed as inhibition of tube formation incubated for 18 hrs by matrigel-based inverted microscopic analysis2021Journal of natural products, 02-26, Volume: 84, Issue:2
Arenarosides A-G, Polyhydroxylated Oleanane-Type Saponins from
AID622613Inhibition of bovine brain tubulin polymerization at 37 degC after 0.3 hrs by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1068620Growth inhibition of human HCC2998 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1534367Inhibition of porcine brain tubulin polymerization measured every 2 mins for 60 mins by spectrophotometric analysis2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
AID1057123Displacement of [3H]colchicine from tubulin (unknown origin) at 3 uM after 30 mins by scintillation counting2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID1233598Induction of cell cycle arrest in human M21 cells assessed as cells accumulation at G2/M phase at 10 nM after 24 hrs by flow cytometry (Rvb = 22.1%)2015European journal of medicinal chemistry, Jul-15, Volume: 100Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model.
AID1351595Cytotoxicity against human HaCaT cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID310759Antiproliferative activity against human PC3 cells2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
3-(2'-Bromopropionylamino)-benzamides as novel S-phase arrest agents.
AID1059052Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis, cytotoxic evaluation and molecular docking study of 2-alkylthio-4-(2,3,4-trimethoxyphenyl)-5-aryl-thiazoles as tubulin polymerization inhibitors.
AID1882900Resistance index, ratio of IC50 for human A549/TxR cells to IC50 for human A549 cells2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID616969Antiproliferative activity against HUVEC grown in absence of growth factors after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID455036Cytotoxicity against human KM20L2 cells after 48 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID1906326Induction of microtubule disruption in human HeLa cells assessed as loss of cellular structure measured after 24 hrs at 2 to 5 nM by DAPI staining based laser scanning confocal microscopic analysis
AID265408Displacement of [3H]colchicine from tubulin by scintillation proximity assay2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID616973Selectivity ratio of IC50 for human HAAE1 grown in absence of growth factors to IC50 for human HAAE1 grown in presence of growth factors2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1324110Cytotoxicity against human SNB75 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID281343Cytotoxicity against human HT29 cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1367974Antiproliferative activity against human HCT116 cells by MTT assay
AID1637517Antiproliferative activity against human DU145 cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID305463Cell cycle arrest in human HepG2 cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and cytotoxic activities of 4,5-diarylisoxazoles.
AID691730Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as change in kidney weight at 50 mg/kg, ip qd after 21 days relative to vehicle-treated control2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1064429Growth inhibition of human MOLT4 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID299208Antiproliferative activity against human DND1 cells2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity relationships.
AID1064425Growth inhibition of human HOP62 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1657523Cytotoxicity against human KB3-1 cells after 68 hrs by MTT assay2020Journal of natural products, 05-22, Volume: 83, Issue:5
Synthesis and Cytotoxicity Studies of Stilbene Long-Chain Fatty Acid Conjugates.
AID1308546Cytotoxicity against human HCT8 cells assessed as cell viability after 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID685191Growth inhibition of human SF539 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID629594Antiproliferative activity against mouse L1210 cells after 2 days by coulter counter analysis2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID1064435Antimitotic activity against sea urchin embryo model assessed as cleavage arrest of fertilized egg compound treated at 8 to 20 mins post-fertilization and 45 to 55 mins prior to first mitotic cycle completion measured 2.5 to 5.5 hrs post-fertilization2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID767878Displacement of [3H]colchicine from tubulin (unknown origin) at 5 uM2013Journal of natural products, Sep-27, Volume: 76, Issue:9
Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.
AID622532Inhibition of bovine brain tubulin polymerization incubated for 15 mins at 30 degC, cooled followed by 0.3 hr acquisition at 30 degC by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1730583Disruption of microtubule polymerization in human M21 cells assessed as induction of mitotic abnormalities at 10 nM measured after 24 hrs by DAPI staining based immunofluorescence microscopic analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID1613397Inhibition of porcine brain tubulin polymerization
AID379678Inhibition of pRAD52 recombination repair gene/topoisomerase 1 deficient Saccharomyces cerevisiae RS321N carrying pRAD52 in galactose medium by microtiter plate assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID1458817Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1727313Antiproliferative activity against human K562R cells assessed as cell viability after 24 hrs by Celltiter-Glo assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation.
AID1308542Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1276336Displacement of [3H]colchicine from tubulin (unknown origin) by DEAE-cellulose filter method2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Novel Microtubule-Targeting 7-Deazahypoxanthines Derived from Marine Alkaloid Rigidins with Potent in Vitro and in Vivo Anticancer Activities.
AID1324097Cytotoxicity against human NCI-H23 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1466247Antiproliferative activity against HEK293 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Synthesis and biological evaluation of novel indole-pyrimidine hybrids bearing morpholine and thiomorpholine moieties.
AID769827Relative resistance, ratio of IC50 for beta3 tubulin overexpressed in human HeLa cells to IC50 for human HeLa cells2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.
AID1742932Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors.
AID221950Cytotoxicity against human MLM melanoma cell line.1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Synthesis and evaluation of analogues of (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene as potential cytotoxic and antimitotic agents.
AID1126014Inhibition of bovine brain tubulin polymerization at 10 uM after 60 mins by spectrophotometric analysis2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1064391Growth inhibition of human OVCAR8 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID761835Inhibition of bovine brain tubulin polymerization incubated for 15 mins prior to GTP addition measured after 20 mins by spectrophotometry2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity.
AID85940Cytotoxic activity against HT-29 cell line2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
A new family of quinoline and quinoxaline analogues of combretastatins.
AID669455Cell cycle arrest in human SKOV3 cells assessed as accumulation at G2/M phase at 5 nM by FACS analysis2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID674208Antiproliferative activity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Discovery and optimization of a series of 2-aryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazoles as novel anticancer agents.
AID1688958Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by alamar blue assay2020European journal of medicinal chemistry, Mar-01, Volume: 189β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells.
AID1402686Antiproliferative activity against human A549 cells after 24 hrs by SRB assay
AID1317607Induction of porcine brain tubulin polymerization assessed as time required to reach maxium effect at 10 uM measured every 1 min for 40 mins in presence of GTP2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1637514Antiproliferative activity against human HeLa cells after 48 hrs by sulforhodamine B assay2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID379683Inhibition of Saccharomyces cerevisiae RS321 expressing Rad52.erg6.top1 by agar diffusion assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID384963Inhibition of tubulin aggregation2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
Synthesis and biological activity of fluorinated combretastatin analogues.
AID486600Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
Synthesis, molecular modeling and biological evaluation of dithiocarbamates as novel antitubulin agents.
AID1164799Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Synthesis and biological evaluation of novel 3,4-diaryl-1,2,5-selenadiazol analogues of combretastatin A-4.
AID1717464Inhibition of tubulin polymerization in human SGC-7901 cells assessed as reduction of interphase microtubule network wrapped around the cell nucleus at 0.032 uM measured after 48 hrs by DAPI/immunofluorescence staining based fluorescence microscopic analy
AID1550343Induction of microtubule depolymerization in human SGC7901 cells assessed as change in microtubule morphology at 2 fold antiproliferative IC50 measured after 24 hrs by DAPI staining based fluorescence microscopy2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and bioevaluation of diarylpyrazoles as antiproliferative agents.
AID293357Effect on body weight in mouse implanted with S180 cells at 40 mg/kg, ip after 4 days2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID1731558Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents.
AID737097Displacement of [3H]colchicine from bovine brain tubulin at 1 uM after 20 mins by turbidimetric analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID1757959Resistance ratio of IC50 for antiproliferative activity against human NCI/ADR-RES cells expressing Pgp to IC50 for antiproliferative activity against human OVCAR-8 cells2021Bioorganic & medicinal chemistry letters, 06-01, Volume: 41Novel pyrazolo[4,3-d]pyrimidine microtubule targeting agents (MTAs): Synthesis, structure-activity relationship, in vitro and in vivo evaluation as antitumor agents.
AID314007Antiproliferative activity against human EKVX cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID93844Compound was tested for cell arrest at S phase at 25 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID665694Cytotoxicity against human A375 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID474640Cell cycle arrest in human HeLa cells assessed as accumulation of cells in G2/M phase at 2.2 uM after 24 hrs using propidium iodide by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID293343Cell cycle arrest in HMEC1 cells assessed as accumulation at G2/M phase at 12.5 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID317989Antiproliferative activity against mouse FM3A cells2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors.
AID1570342Cytotoxicity against human HuH7 cells assessed as cell doubling time by cell titer blue assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.
AID297426Displacement of [3H]colchicine from tubulin at 5 uM2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
4- and 5-aroylindoles as novel classes of potent antitubulin agents.
AID1550345Inhibition of microtubule formation in human SGC7901 cells at 2 fold IC50 concentration measured after 24 hrs by DAPI staining based fluorescence microscopy2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and bioevaluation of diarylpyrazoles as antiproliferative agents.
AID479715Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Synthesis and antitumor activity of 1,5-disubstituted 1,2,4-triazoles as cis-restricted combretastatin analogues.
AID737099Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetric analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID771203Cell cycle arrest in human HT-29 cells assessed as accumulation at G0/G1 phase at 25 nM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 68.24%)2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID1324135Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1862606Antiproliferative activity against human NCI-N87 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID1125803Cytotoxicity against human KB cells after 72 hrs by methylene blue assay2014European journal of medicinal chemistry, Apr-22, Volume: 77Antimitotic and vascular disrupting agents: 2-hydroxy-3,4,5-trimethoxybenzophenones.
AID273281Inhibition of [3H]colchicine binding to tubulin at 1 uM2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.
AID502748Growth inhibition of human PC3 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1068608Growth inhibition of human LOXIMVI cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID502715Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1487506Antiproliferative activity against human A549 cells after 48 hrs by sulforhodamine B assay2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Design and synthesis of 4-morpholino-6-(1,2,3,6-tetrahydropyridin-4-yl)-N-(3,4,5-trimethoxyphenyl)-1,3,5-triazin-2-amine analogues as tubulin polymerization inhibitors.
AID1565956Metabolic stability in Sprague-Dawley rat liver microsomes assessed as parent compound remaining after 60 mins in presence of NADPH by HPLC-UV-MS analysis
AID214015Inhibition of tubulin polymerization1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
AID1348619Antiproliferative activity against human K562 cells after 72 hrs by resazurin-based fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID1235371Toxicity in HUVEC assessed as cell viability at 20 nM after 4 hrs relative to control2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes.
AID1535613Toxicity in mouse xenografted with rat H22 cells assessed as weight loss at 3 mg/kg, ip measured after 28 days2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Synthesis, biological evaluation and molecular docking of benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives as novel tubulin polymerization inhibitors.
AID1351653Inhibition of tubulin polymerization in human MCF7 cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1890442Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 10 uM incubated for 24 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 4.66 %)2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
AID685200Growth inhibition of human SK-MEL-28 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID723246Cytotoxicity against human QGY cells after 48 hrs by MTT assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Design and synthesis of cyclopropylamide analogues of combretastatin-A4 as novel microtubule-stabilizing agents.
AID1310240Antivascular activity in human EAhy926 cells assessed as disruption of preformed blood vessel lke network at 100 nM after 16 hrs by matrigel based tube formation assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID691724Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as effect on ALP level at 30 mg/kg, ip qd after 21 days (Rvb = 107.6 +/- 0.8 IU/L)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1068585Growth inhibition of human UO31 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID455034Cytotoxicity against human SF268 cells after 48 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID1174858Inhibition of colchicine binding to tubulin (unknown origin)2015European journal of medicinal chemistry, Jan-07, Volume: 89Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin.
AID1336753Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 50 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 9.4%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1635332Antiproliferative activity against multidrug resistant human SKOV3 cells expressing MDR1-M6/6 after 48 hrs by SRB assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID384970Induction of apoptosis in human NCI-H460 cells assessed as subG1 phase accumulation after 24 hrs by flow cytometry2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
Synthesis and biological activity of fluorinated combretastatin analogues.
AID669462Growth inhibition of human PC3 cells after 48 hrs by SRB assay2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID1185443Inhibition of tubulin (unknown origin) polymerization by spectrophotometry2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Concise syntheses of 7-anilino-indoline-N-benzenesulfonamides as antimitotic and vascular disrupting agents.
AID567092Cytotoxicity against mouse B16 cells assessed as reduction in cell viability after 48 hrs by MTT assay2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues.
AID1196882Metabolic stability in human liver microsomes assessed as peak area after 30 mins by LC-UV analysis in presence of NADPH and UDPGA2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID721882Displacement of [3H]colchicine from tubulin (unknown origin) at 5 uM after 10 mins by DEAE-cellulose filter method2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID202478Compound was evaluated against Human cell line neuroblast SK-N-SH1999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID1518070Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID444152Antiproliferative activity against mouse B16F0 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID691636Antitumor activity against human HT-29 cells xenografted in nude BALB/c mouse assessed as decrease in tumor volume at 30 mg/kg, ip qd measured on day 21 relative to vehicle-treated control2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1486472Cytotoxicity against human A549 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis, biological evaluation and molecular modeling of imidazo[1,2-a]pyridine derivatives as potent antitubulin agents.
AID1308543Cytotoxicity against human Bel7402 cells assessed as cell viability after 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1308539Inhibition of [3H]-colchicine binding to porcine brain tubulin at 1 uM relative to control2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID383963Cytotoxicity against human OVCAR-3 cells2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
2-(6-aryl-3(Z)-hexen-1,5-diynyl)anilines as a new class of potent antitubulin agents.
AID444158Relative resistance, ratio of IC50 for human HeLa cells expressing wild type beta3 tubulin to IC50 for human HeLa cells2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID622609Inhibition of bovine brain tubulin polymerization incubated for 15 mins at 37 degC, cooled followed by 20 mins acquisition at 37 degree C by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1183667Inhibition of bovine brain tubulin polymerization by turbidimetry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID1263278Cytotoxicity against human NCI/ADR-RES cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1325845Cell cycle arrest in human MCF7 cells assessed as accumulation at G0 phase at 2000 nM after 48 hrs by propidium iodide-staining based FACS analysis2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Scaffold-Hopping of Aurones: 2-Arylideneimidazo[1,2-
AID636398Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Design, synthesis, biological evaluation and molecular modeling of 1,3,4-oxadiazoline analogs of combretastatin-A4 as novel antitubulin agents.
AID1882981Induction of cell cycle arrest in human MDA-MB-231 cells assessed as increase in G2 phase cells at 10 uM incubated for 24 hrs by PI staining based flow cytometric analysis (Rvb = 8.95%)2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and evaluation of a novel series of mono-indolylbenzoquinones derivatives for the potential treatment of breast cancer.
AID1886257Antitumor activity against mouse H22 cells allografted in ICR mouse assessed as reduction in tumor volume growth rate at 20 mg/kg, iv administered qd for 21 days measured after 12 days2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID310757Antiproliferative activity against human Bel7402 cells2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
3-(2'-Bromopropionylamino)-benzamides as novel S-phase arrest agents.
AID1324121Cytotoxicity against human OVCAR4 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1628264Binding affinity to goat brain tubulin assessed as reduction in binding of 5-(Quinolin-3-yl)-4-(3,4,5-trimethoxyphenyl)-1H-imidazol-2-amine to tubulin incubated for 15 mins by fluorescence based assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID314003Antiproliferative activity against human HL60 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID669465Growth inhibition of human MRC5 cells after 48 hrs by SRB assay2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID737115Cytotoxicity against human HeLa cells after 72 hrs by MTT assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID1463422Cell cycle arrest in human PC3 cells assessed as accumulation at G0/G1 phase at 0.05 uM incubated for 24 hrs by propidium iodide staining based FACS assay (Rvb = 62.5%)2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Constructing novel dihydrofuran and dihydroisoxazole analogues of isocombretastatin-4 as tubulin polymerization inhibitors through [3+2] reactions.
AID612422Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetric analysis2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Synthesis, biological evaluation, and molecular modeling of cinnamic acyl sulfonamide derivatives as novel antitubulin agents.
AID1200592Inhibition of bovine brain tubulin polymerization incubated for 60 mins by microplate reader based turbidimetry2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Quantum chemistry calculation-aided structural optimization of combretastatin A-4-like tubulin polymerization inhibitors: improved stability and biological activity.
AID314010Antiproliferative activity against human HCT15 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID452618Antiproliferative activity against mouse P388 cells after 5 days by MTT assay2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID1411612Substrate activity at human OCT2 expressed in HEK293 cells assessed as compound uptake by HPLC-UV method2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID452623Cell cycle arrest in human K562 cells assessed as accumulation at S phase at 10 uL after overnight incubation by propidium iodide staining-based flow cytometry2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID256879Inhibition of tubulin polymerization in bovine brain at 10 uM2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors.
AID1068635Growth inhibition of human HL-60(TB) cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1724511Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay2020Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19
A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors.
AID722281Inhibition of tubulin assembly (unknown origin) pre-incubated with compound for 15 mins before GTP addition measured after 20 mins at 30 degC post GTP addition by turbidimetry2013Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
Synthesis and biological evaluation of N-alkyl-N-(4-methoxyphenyl)pyridin-2-amines as a new class of tubulin polymerization inhibitors.
AID1324138Cytotoxicity against human BT549 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1535576Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM2019Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
Synthesis, biological evaluation and molecular docking of benzimidazole grafted benzsulfamide-containing pyrazole ring derivatives as novel tubulin polymerization inhibitors.
AID1251951Displacement of [3H]colchicine from bovine brain tubulin at 5 uM2015Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
Novel 3-Substituted 7-Phenylpyrrolo[3,2-f]quinolin-9(6H)-ones as Single Entities with Multitarget Antiproliferative Activity.
AID619860Inhibition of bovine tubulin polymerization at 10 uM after 60 mins by spectrophotometric analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID281350Cytotoxicity against human ECV304 cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID319824Cytotoxicity against human H1299 cells2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and antitumor activity of benzils related to combretastatin A-4.
AID1263276Cytotoxicity against human OVCAR3 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID214525Percentage control on Tubulin- Dependent GTP hydrolysis was evaluated at 50 micro M concentration1999Bioorganic & medicinal chemistry letters, Apr-19, Volume: 9, Issue:8
A new anti-tubulin agent containing the benzo[b]thiophene ring system.
AID1263270Cytotoxicity against human MDA-MB-435 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1240944Antiproliferative activity against human DU145 cells assessed as cell growth inhibition by SRB assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines as tubulin polymerization inhibitors.
AID262911Inhibition of tubulin polymerization2006Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
Benzoylphenylurea sulfur analogues with potent antitumor activity.
AID1765553Inhibition of tubulin polymerization in human PC-3 cells assessed as abnormal centrosomal amplification with immature spindles in p-H3 positive cells at 200 nM incubated for 24 hrs by staining based confocal fluorescence microscopy2021European journal of medicinal chemistry, Oct-15, Volume: 222Effects of substituent pattern on the intracellular target of antiproliferative benzo[b]thiophenyl chromone derivatives.
AID1736451Antiproliferative activity against drug-resistant human MCF7 cells incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID665826Induction of apoptosis in human A549 cells assessed as necrotic cells at 2 uM after 48 hrs by annexin-V FITC/propidium iodide staining based FACS analysis2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID273082Antiproliferative activity against human MCF7 cells after 72 hrs2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and structure-activity relationships of carbazole sulfonamides as a novel class of antimitotic agents against solid tumors.
AID730213Cytotoxicity against human A549 cells after 72 hrs by CCK-8 assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Synthesis and structure-activity relationships of N-methyl-5,6,7-trimethoxylindoles as novel antimitotic and vascular disrupting agents.
AID1541868Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
AID1348620Antiproliferative activity against human U87 cells after 72 hrs by resazurin-based fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID642097Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 20 nM after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 0.10 %)2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1730138Inhibition of bovine brain tubulin assembly by turbidimetry based spectrophotometric method2021European journal of medicinal chemistry, Feb-15, Volume: 212Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors.
AID273276Antiproliferative activity against mouse L1210 cells2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.
AID314008Antiproliferative activity against human HOP92 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID1198454Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents.
AID644550Cell cycle arrest in human SKOV3 cells assessed as accumulation at G2/M phase at 5 nM by flow cytometry (Rvb = 14%)2012Bioorganic & medicinal chemistry, Mar-01, Volume: 20, Issue:5
Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A-1.
AID685211Growth inhibition of human 786-0 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID606034Cytotoxicity against mouse B16 cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
A novel class of trans-methylpyrazoline analogs of combretastatins: synthesis and in-vitro biological testing.
AID1906208Induction of cell cycle arrest in human HeLa cells assessed as S-phase at 6 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 23.4%)
AID1628402Growth inhibition of human A549 cells incubated for 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Design, Synthesis, and Biological Evaluation of 1-Methyl-1,4-dihydroindeno[1,2-c]pyrazole Analogues as Potential Anticancer Agents Targeting Tubulin Colchicine Binding Site.
AID674222Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetric analysis2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Discovery and optimization of a series of 2-aryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazoles as novel anticancer agents.
AID1757282Antiproliferative activity against taxol-resistant human HCT-8 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1285334Induction of apoptosis in human HT-29 cells assessed as late apoptotic cells at 10 nM after 48 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb=4.06%)2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID314005Antiproliferative activity against human RPMI8226 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID1432886Retention time of the compound at 200 uM in presence of 50 mM GSH by HPLC analysis2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Development of a novel near-infrared fluorescent theranostic combretastain A-4 analogue, YK-5-252, to target triple negative breast cancer.
AID1119741Growth inhibition of human NCI-H460 cells by sulforhodamine B assay2012MedChemComm, Jun, Volume: 3, Issue:6
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
AID626629Toxicity against fertilized chicken embryo assessed as mortality at 1 ug, iv by CAM assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID420615Displacement of [3H]colchicine from tubulin at 5 uM by turbidimetry2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Design and synthesis of 2-(3-benzo[b]thienyl)-6,7-methylenedioxyquinolin-4-one analogues as potent antitumor agents that inhibit tubulin assembly.
AID1732757Induction of cell cycle arrest in human RL cells assessed as increase in accumulation in subG0/G1 phase at 10 nM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 4.5 %)2021European journal of medicinal chemistry, Apr-05, Volume: 215Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies.
AID1774980Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Lead Optimization: Synthesis and Biological Evaluation of PBT-1 Derivatives as Novel Antitumor Agents.
AID444168Inhibition of bovine brain tubulin polymerization by spectrophotometric analysis2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID214719Percent inhibition of colchicine binding(ICB) at 5 uM [3H]colchicine concentration2001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Antitumor Agents. 211. Fluorinated 2-phenyl-4-quinolone derivatives as antimitotic antitumor agents.
AID622411Cytotoxicity against human HL60 cells after 48 hrs by sulforhodamine B assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1917307Antiproliferative activity against human U-251 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID669454Antivascular activity against HUVEC after 24 hrs by xCELLigence assays2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID1600487Effect on DNA synthesis in human CCRF-CEM cells assessed as DNA synthesis level at IC50 incubated for 24 hrs by propidium iodide-staining based BrdU incorporation assay (Rvb = 52.13%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1231330Anticancer activity against human Saos2 cells assessed as reduction in cell proliferation after 48 hrs by WST-1 assay2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4.
AID1600479Induction of cell cycle arrest in human CCRF-CEM cells assessed as accumulation at G0/G1 phase at antiproliferative IC50 incubated for 24 hrs by PI staining based flow cytometric analysis (Rvb = 40.89%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID665825Induction of apoptosis in human A549 cells assessed as increase in caspase3 activity using AFC-conjugated Ac-DEVD as substrate at 2 uM after 48 hrs by fluorescence assay relative to control2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID219710Percentage inhibition of colchicine binding(1: 1 ratio of inhibitor: colchicine)1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
Synthesis and cytotoxicity of 1,6,7,8-substituted 2-(4'-substituted phenyl)-4-quinolones and related compounds: identification as antimitotic agents interacting with tubulin.
AID280074Antiproliferative activity against drug resistant HCT15 cell line expressing MDR1 by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID1766199Inhibition of pig brain tubulin polymerization by spectrophotometric method2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Design, synthesis and biological evaluation of novel acridine and quinoline derivatives as tubulin polymerization inhibitors with anticancer activities.
AID1068626Growth inhibition of human NCI-H226 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1574868Phototoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 2 to 8 uM irradiated with 50 mW cm'-2 UV light for 6 mins and measured after 24 hrs by CCK8 assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Synthesis and characterization of a photoresponsive doxorubicin/combretastatin A4 hybrid prodrug.
AID1862608Antiproliferative activity against human HCT-116 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID317992Inhibition of bovine tubulin polymerization after 20 mins2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors.
AID1518326Disruption of microtubule network in human SW620 cells assessed as microtubule disorganization at 50 nM for 18 hrs by FITC/DAPI staining-based confocal microscopic analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.
AID1474402Inhibition of porcine brain tubulin polymerization at 10 uM measured at 1 min interval for 40 mins by spectrophotometric method2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of novel chalcone derivatives as a new class of microtubule destabilizing agents.
AID1586074Inhibition of bovine brain tubulin polymerization measured every 30 secs for 30 mins by turbidimetric assay2019European journal of medicinal chemistry, Jan-15, Volume: 1621-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase.
AID721876Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID619929Cell cycle arrest in human MCF7 cells assessed as appearance of polyploidy at 100 nM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 8.33+/-2.5%)2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID658916Binding affinity to bovine tubulin after 1 hr by spectrofluorometric analysis2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
AID273360Antiproliferative activity against human KB cell line by methylene blue dye assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
AID314014Antiproliferative activity against human SK-MEL-5 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID452616Antiproliferative activity against human K562 cells after 5 days by MTT assay2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID1757884Antiproliferative activity against human MDA-MB-435 cells2021Bioorganic & medicinal chemistry letters, 06-01, Volume: 41Novel pyrazolo[4,3-d]pyrimidine microtubule targeting agents (MTAs): Synthesis, structure-activity relationship, in vitro and in vivo evaluation as antitumor agents.
AID1366861Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by SRB cell proliferation assay2017Bioorganic & medicinal chemistry letters, 12-15, Volume: 27, Issue:24
Potential anti-proliferative agents from 1,4-benzoxazinone-quinazolin-4(3H)-one templates.
AID1276115Cytotoxicity against human SKBR3 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID474638Cell cycle arrest in human HeLa cells assessed as accumulation of cells in G2/M phase at 0.02 uM after 24 hrs using propidium iodide by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID622511Cytotoxicity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID349334Inhibition of calf brain tubulin polymerization at 20 uM relative to control2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Naphthylphenstatins as tubulin ligands: synthesis and biological evaluation.
AID1420995Antiproliferative activity against human HeLa cells after 72 hrs by XTT assay
AID616978Antiproliferative activity against human A431 after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID213848Inhibition of binding of [3H]colchicine (5.0 uM) to tubulin (1.0 uM) at a concentration of 5.0 uM1999Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
Synthesis and biological evaluation of dihydrobenzofuran lignans and related compounds as potential antitumor agents that inhibit tubulin polymerization.
AID1402689Cell cycle arrest in human HeLa cells assessed as accumulation of cells at G2/M phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 16.4%)
AID1162827Inhibition of tubulin (unknown origin) polymerization at 3 uM incubated for 1 hr by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID1195291Antiproliferative activity against human HeLa cells after 48 hrs by sulforhodamine B assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID314002Antiproliferative activity against human CCRF-CEM cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID594375Displacement [3H]colchicine from tubulin at 1 uM after 10 mins2011Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
Synthesis of novel antimitotic agents based on 2-amino-3-aroyl-5-(hetero)arylethynyl thiophene derivatives.
AID1058420Cytotoxicity against HUVEC assessed as cell viability after 4 days by MTS assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation.
AID1689056Metabolic stability in human liver microsomes assessed as UGT-mediated N-glucuronidation by measuring half life at 3 uM measured up to 45 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells.
AID685176Growth inhibition of human HOP62 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1334731Aqueous solubility of the compound at pH 7.4 measured after 4 hrs by HPLC/UV analysis2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility.
AID1508157Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 2 uM after 48 hrs by flow cytometric analysis (Rvb = 34.2%)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1906180Inhibition of pig brain tubulin polymerization by spectrophotometeric analysis
AID730201Antiproliferative activity against activated HUVECs after 48 hrs by CCK-8 assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Synthesis and structure-activity relationships of N-methyl-5,6,7-trimethoxylindoles as novel antimitotic and vascular disrupting agents.
AID1176810Cytotoxicity against human KB cells assessed as cell growth inhibition after 72 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Microwave-assisted synthesis and biological evaluation of 3,4-diaryl maleic anhydride/N-substituted maleimide derivatives as combretastatin A-4 analogues.
AID1324093Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID765488Competitive inhibition of [3H]colchicine binding to tubulin (unknown origin) at 5 uM after 10 mins by radioligand displacement assay2013European journal of medicinal chemistry, Sep, Volume: 67N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines: a novel class of antitumor agents targeting the colchicine site on tubulin.
AID1686599Inhibition of pig brain tubulin polymerization incubated for 20 mins by spectrophotometry2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Potent Antitumor Activities and Structure Basis of the Chiral β-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin.
AID1068606Growth inhibition of human M14 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1709305Resistant index, ratio of IC50 for cytotoxicity against human SK-OV-3 cells over expressing MDR1-6/6 cells to IC50 for cytotoxicity against human SK-OV-3 cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1294468Growth inhibition of human A549/ATCC cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1381554Cytotoxicity against human PANC1 cells after 48 hrs by XTT assay2018Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13
New somatostatin-drug conjugates for effective targeting pancreatic cancer.
AID1263287Cytotoxicity against human Hs578T cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID247835Concentration required to inhibit human T-lymphoblast CEM cell line proliferation2005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
AID659050Cytotoxicity against HUVEC after 48 hrs using resazurin by microplate fluorometer analysis2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
AID1267533Antiproliferative activity against human IC8 cells after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, Jan-01, Volume: 26, Issue:1
Synthesis and biological evaluation of thiophene and benzo[b]thiophene analogs of combretastatin A-4 and isocombretastatin A-4: A comparison between the linkage positions of the 3,4,5-trimethoxystyrene unit.
AID1324130Cytotoxicity against human SN12C cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1635333Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID502726Growth inhibition of human SF539 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1183726Induction of apoptosis in human HeLa cells assessed as failure of MT elongation at 100 nM by immunofluorescence analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID1774978Antiproliferative activity against human KB cells assessed as cell growth inhibition measured after 72 hrs by SRB assay2021ACS medicinal chemistry letters, Dec-09, Volume: 12, Issue:12
Lead Optimization: Synthesis and Biological Evaluation of PBT-1 Derivatives as Novel Antitumor Agents.
AID1647034Toxicity in ICR mouse xenografted with mouse H22 cells assessed as effect on kidney damage or inflammation at 30 mg/kg, iv administered once daily for 21 consecutive days measured after 21 days by hematoxylin-eosin staining based fluorescence microscopy2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID280070Cytotoxicity against human PC3 cells2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID103367Cytotoxicity against human MCF-7 breast cancer cell line.1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Synthesis and evaluation of analogues of (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene as potential cytotoxic and antimitotic agents.
AID1294481Growth inhibition of human NCI-ADR-RES cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1851428Induction of apoptosis in human K562 cells assessed as early apoptotic cells at 10 uM by AnnexinV-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 2.56%)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Synthesis and antitumor activity of a series of novel N-aryl-5-(2,2,2-trifluoroethoxy)-1,5-dihydro-2H-pyrrol-2-ones derivatives.
AID88796Evaluated for growth inhibition (anticancer activity) of Human CNS cancer SF-295 cell line2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID1059994Cytotoxicity against mouse FM3A/0 cells assessed as growth inhibition after 48 hrs by coulter counting analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
AID1469218Growth inhibition of human HepG2/DOX cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1886182Inhibition of HDAC in human HeLa cells using BOC-K(Ac)-AMC as substrate at 1 uM measured after 30 mins by fluorescence based microtiter plate reader assay relative to control2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.
AID214724Percentage inhibition of [3H]colchicine binding to tubulin was evaluated at 10 micro M concentration1999Bioorganic & medicinal chemistry letters, Apr-19, Volume: 9, Issue:8
A new anti-tubulin agent containing the benzo[b]thiophene ring system.
AID452614Inhibition of tubulin assembly by immunofluorescence assay2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID1057198Cytotoxicity against HEK293 cells assessed as growth inhibition after 3 days by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity.
AID293342Cell cycle arrest in HMEC1 cells assessed as accumulation at G2/M phase at 6.25 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID662353Cell cycle arrest in human HuTu 80 cells assessed as reduction at sub-G1 phase at 30 nM after 48 hrs by propidium iodide-based flow cytometry (Rvb = 3.3 %)2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID1778219Inhibition of tubulin polymerization (unknown origin) at 10 uM measured after 30 mins every 1 min for 20 mins by spectrophotometric method2021European journal of medicinal chemistry, Aug-05, Volume: 220Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines.
AID1294475Growth inhibition of human SF295 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID1064431Growth inhibition of human CCRF-CEM cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1351637Induction of apoptosis in human MCF7 cells assessed as increase in histone-associated DNA fragments in oligonucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1462291Antiproliferative activity against human HCT15 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis of different heterocycles-linked chalcone conjugates as cytotoxic agents and tubulin polymerization inhibitors.
AID1304312Antiproliferative activity against human K562 cells assessed as reduction in cell proliferation after 3 days by 3H-thymidine incorporation assay2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
Synthesis and biological activity of pyrrole analogues of combretastatin A-4.
AID1308556Resistance index, ratio of IC50 for human A2780/TAX cells to IC50 for human A2780 cells2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1463415Cytotoxicity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Constructing novel dihydrofuran and dihydroisoxazole analogues of isocombretastatin-4 as tubulin polymerization inhibitors through [3+2] reactions.
AID273361Antiproliferative activity against human KB-VIN10 cell line by methylene blue dye assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
AID1562381Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin.
AID605714Displacement of N,N'-ethylenebis(iodoacetamide) from colchicine-binding site of beta-tubulin in human MDA-MB-231 cells at 1000 times IC50 preincubated for after 2 hrs before N,N'-ethylenebis(iodoacetamide) addition measured after 1.5 hrs by chemiluminesce2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID1486470Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15
Synthesis, biological evaluation and molecular modeling of imidazo[1,2-a]pyridine derivatives as potent antitubulin agents.
AID1508154Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 2 uM after 24 hrs by flow cytometric analysis (Rvb = 18.4%)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1185206Cell cycle arrest in human CA46 cells assessed as accumulation at G2/M phase at 5 times IC50 by flow cytometry2014European journal of medicinal chemistry, Sep-12, Volume: 84Novel 9'-substituted-noscapines: synthesis with Suzuki cross-coupling, structure elucidation and biological evaluation.
AID382335Cytotoxicity against human WM35 cells assessed as [3H]thymidine incorporation after 72 hrs by microplate scintillation counter2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin.
AID1728927Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G1 phase at 1 uM measured after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 74.39%)2021European journal of medicinal chemistry, Mar-05, Volume: 213Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.
AID403057Increase in mitotic index in human MCF7 cells at 10 times the IC50 concentration after 16 hrs2005Journal of natural products, Aug, Volume: 68, Issue:8
Antineoplastic agents. 515. Synthesis of human cancer cell growth inhibitors derived from 3,4-methylenedioxy-5,4'-dimethoxy-3'-amino-Z-stilbene.
AID1348304Induction of apoptosis in human HeLa cells at 0.1 uM after 24 to 48 hrs by propidium iodide/annexin V/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Targeting tubulin polymerization by novel 7-aryl-pyrroloquinolinones: Synthesis, biological activity and SARs.
AID1408571Cell cycle arrest in human PC3 cells assessed as accumulation at G2/M phase at 200 nM after 24 hrs by propidium iodide staining based flow cytometry2018European journal of medicinal chemistry, Sep-05, Volume: 1575'-Chloro-2,2'-dihydroxychalcone and related flavanoids as treatments for prostate cancer.
AID1585996Cell cycle arrest in human BT549 cells assessed as accumulation of cells at S phase at 8 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 25.84%)
AID451272Cytotoxicity against human K562 cells after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Synthesis and biological evaluation of 3,4-diaryl-5-aminoisoxazole derivatives.
AID1647009Induction ROS generation in human HepG2 cells assessed as intracellular ROS level at 0.1 uM measured after 24 hrs by DCFH-DA probe based flow cytometry (Rvb = 7.86 %)2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1657526Cytotoxicity against human MCF7 cells after 68 hrs by MTT assay2020Journal of natural products, 05-22, Volume: 83, Issue:5
Synthesis and Cytotoxicity Studies of Stilbene Long-Chain Fatty Acid Conjugates.
AID1458854Metabolic stability in Sprague-Dawley rat liver microsomes assessed as compound remaining after 120 mins in presence of NADPH by UV-based HPLC-MS/MS analysis2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID404582Inhibition of calf brain tubulin polymerization after 20 mins2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Diarylmethyloxime and hydrazone derivatives with 5-indolyl moieties as potent inhibitors of tubulin polymerization.
AID330411Cytotoxicity against human KM20L2 cells after 48 hrs by SRB assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID1068595Growth inhibition of human NCI-ADR-RES cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID281354Half life in iv dosed Swiss Albino mouse plasma2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1534364Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
AID1700955Antiproliferation activity against human HCT116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
AID1612627Drug resistance index, ratio of IC50 for ADR-resistant human Bel7402/ADR cells to IC50 for human Bel7402 cells2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1517360Inhibition of colchicine binding to pig brain tubulin assessed as decrease in fluorescence of colchicine-tubulin complex incubated for 1.5 hrs by fluorescence based assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Design and synthesis of (2-(phenylamino)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone analogues as potent anti-tubulin polymerization agents.
AID1771460Antiproliferative activity against human HeLa cells assessed as cell growth inhibition after 72 hrs by SRB assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID421856In vivo antitumor activity against mouse P388 cells2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Antineoplastic agents. 578. Synthesis of stilstatins 1 and 2 and their water-soluble prodrugs.
AID1157567Inhibition of EGFR (unknown origin) assessed as incorporation of [32P] gamma-ATP in to myelin basic protein after 30 mins by autoradiographic analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.
AID1757283Resistant index, ratio of IC50 for taxol-resistant human HCT-8 cells to IC50 for human HCT-8 cells2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1351664Inhibition of tubulin polymerization in human SKOV3 cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1336775Induction of mitochondrial membrane potential loss in human A549 cells at 100 nM after 48 hrs by JC-1 staining based flow cytometry (Rvb = 3.8%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID685180Growth inhibition of human NCI-H322M cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1873711Induction of apoptosis in human HeLa cells assessed as necrotic cells at 10 nM incubated for 24 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 1.14 %)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID281346Cytotoxicity against human L132 cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1646996Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1891179Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth by MTT assay
AID1162828Inhibition of tubulin (unknown origin) polymerization incubated for 1 hr by fluorescence assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID1524339Inhibition of bovine brain tubulin polymerization after 20 mins by spectrophotometric analysis2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents.
AID685187Growth inhibition of human HT-29 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1555137Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 1 uM measured after 10 mins by beckman scintillation counting method relative to control2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.
AID1729298Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
AID214556Inhibition of tubulin polymerization (ITP)2001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Antitumor Agents. 211. Fluorinated 2-phenyl-4-quinolone derivatives as antimitotic antitumor agents.
AID1324116Cytotoxicity against human UACC62 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID451274Cytotoxicity against human A549 cells after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Synthesis and biological evaluation of 3,4-diaryl-5-aminoisoxazole derivatives.
AID1506733Antiproliferative activity in human HeLa cells assessed as reduction in cell number incubated for 48 hrs by SRB assay2017MedChemComm, Feb-01, Volume: 8, Issue:2
Synthesis and biological evaluation of (-)-kunstleramide and its derivatives.
AID1724513Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay2020Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19
A 2-step synthesis of Combretastatin A-4 and derivatives as potent tubulin assembly inhibitors.
AID1737840Metabolic stability in human liver microsomes assessed as parent compound remaining at 10 uM measured after 30 mins in presence of NADPH by LC/MS/MS analysis2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID1408385Cell cycle arrest in human K562 cells assessed as accumulation at S phase at 0.01 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 49.41%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1534363Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
AID691661Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as effect on ALT level at 30 mg/kg, ip qd after 21 days (Rvb = 28 +/- 0.4 IU/L)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1651883Cytotoxicity against human A549 cells incubated for 4 hrs in anoxic condition followed by oxic exposure for 48 hrs by sulforhodamine B assay2020Journal of natural products, 04-24, Volume: 83, Issue:4
Bioreductively Activatable Prodrug Conjugates of Combretastatin A-1 and Combretastatin A-4 as Anticancer Agents Targeted toward Tumor-Associated Hypoxia.
AID1240943Antiproliferative activity against human vincristine-resistant KBVIN cells expressing P-glycoprotein assessed as cell growth inhibition by SRB assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines as tubulin polymerization inhibitors.
AID1809272Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
AID1757277Antiproliferative activity against mouse H22 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID240662Inhibition of tubulin polymerization2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.
AID305460Cytotoxicity against human OVACAR3 cells2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and cytotoxic activities of 4,5-diarylisoxazoles.
AID757688Cytotoxicity against human SW1990 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Synthesis and antitumor activity of novel 3,4-diaryl squaric acid analogs.
AID567094Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues.
AID642093Growth inhibition of rat A10 cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1276116Cytotoxicity against human MCF7 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1832109Antiproliferative activity against human HCT-116 assessed as reduction in cell viability measured after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID1873729Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 10 nM incubated for 48 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 6.01%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID665696Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID1409115Inhibition of [3H]-colchicine binding to tubulin (unknown origin) at 0.5 uM relative to control2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.
AID1205507Antiproliferative activity against human HeLa cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.
AID1057112Drug metabolism in PBS at pH 7.4 assessed as product-2 level after 24 hrs by HPLC analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID286485Antiproliferative effect against mouse FM3A cells after 2 days2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID515466Cytotoxicity against human H12.1 cells after 96 hrs by SRB assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
4-(3-Halo/amino-4,5-dimethoxyphenyl)-5-aryloxazoles and -N-methylimidazoles that are cytotoxic against combretastatin A resistant tumor cells and vascular disrupting in a cisplatin resistant germ cell tumor model.
AID1882903Inhibition of porcine brain tubulin polymerization measured at 1 min interval for 60 mins by fluorescence assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1586367Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 0.2 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 28 +/- 0.6%)2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4.
AID1514433Cytotoxicity against human HCT116 cells assessed as inhibition of cell growth after 48 hrs by MTT assay
AID494821Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 10 uM after 24 hrs by FACS analysis2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
Synthesis and anti-cancer activity of chalcone linked imidazolones.
AID293346Cell cycle arrest in HMEC1 cells assessed as accumulation at G2/M phase at 100 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID721885Inhibition of tubulin (unknown origin) polymerization preincubated for 15 mins by spectrophotometry2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID1773163Induction of apoptosis in human A549 cells assessed as increase in viable cells at 500 nM measured after 24 hrs by PI/FITC analysis (Rvb = 98.4%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1059042Inhibition of sheep brain tubulin polymerization at 10 uM after 15 mins2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis, cytotoxic evaluation and molecular docking study of 2-alkylthio-4-(2,3,4-trimethoxyphenyl)-5-aryl-thiazoles as tubulin polymerization inhibitors.
AID1873774Induction of mitochondrial membrane potential alteration in human HeLa cells assessed as late apoptotic cells at 10 nM measured after 48 hrs by JC1 staining-based flow cytometry analysis (Rvb = 0.009%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID663559Cell cycle arrest in human CA46 cells assessed as mitotic cells at 10 times IC50 (Rvb = 2 to 4%)2012ACS medicinal chemistry letters, Jan-12, Volume: 3, Issue:1
Steroidomimetic Tetrahydroisoquinolines for the Design of New Microtubule Disruptors.
AID1534524Antiproliferative activity against human U87MG cells after 72 hrs by MTS assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID1760383Antiproliferative activity against human A549 cells incubated for 24 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020).
AID80252Concentration which produces 50% inhibition of growth of human colon tumor HCT 1162001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Combretoxazolones: synthesis, cytotoxicity and antitumor activity.
AID1324095Cytotoxicity against human HOP62 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1741565Antiproliferative activity against human HeLa cells measured after 48 hrs by MTT assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Synthesis, and biological evaluation of 3,6-diaryl-[1,2,4]triazolo[4,3-a]pyridine analogues as new potent tubulin polymerization inhibitors.
AID665823Inhibition of tubulin polymerization after 1 hr by fluorescence assay2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID622419Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID685212Growth inhibition of human A498 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1570341Cytotoxicity against human HeLa cells assessed as cell doubling time by cell titer blue assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.
AID1637518Cell cycle arrest in human HeLa cells assessed as accumulation at G0 phase at 40 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 5.64%)2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID779084Cytotoxicity against HUVEC assessed as cell viability after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
The synthesis and anticancer activity of analogs of the indole phytoalexins brassinin, 1-methoxyspirobrassinol methyl ether and cyclobrassinin.
AID1906218Induction of cell cycle arrest in human HeLa cells assessed as >4N cells at 1.5 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis relative to control
AID1597716Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-01, Volume: 1771-Phenyl-dihydrobenzoindazoles as novel colchicine site inhibitors: Structural basis and antitumor efficacy.
AID1698448Inhibition of tubulin polymerization in human A549 cells assessed as decrease in polymerized fraction of tubulin content at 1 uM after 48 hrs by Western blot analysis relative to control2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Ultrasound assisted synthesis of tetrazole based pyrazolines and isoxazolines as potent anticancer agents via inhibition of tubulin polymerization.
AID280069Cytotoxicity against human HT29 cells2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID1317586Antiproliferative activity against CA-4-resistant human HT-29 cells measured after 72 hrs by MTT assay2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1677373Inhibition of [3H]colchicine binding to bovine brain tubulin at 5 uM relative to control
AID1466166Inhibition of porcine brain tubulin polymerization preincubated for 1 min followed by addition of tubulin measured every 60 s for 90 min by DAPI staining-based fluorescence assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
The synthesis and evaluation of new butadiene derivatives as tubulin polymerization inhibitors.
AID1392069Induction of microtubule depolymerization in rat A10 cells by indirect immunofluorescence method2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.
AID1693358Inhibition of [3H]colchicine binding to bovine tubulin at 1 uM measured after 10 mins by scintillation counting2021Bioorganic & medicinal chemistry, 01-01, Volume: 29The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
AID266930Antiproliferative activity against human K562 cell line2006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-5-aryl thiophenes as a new class of potent antitubulin agents.
AID1550353Inhibition of porcine brain tubulin polymerization at 4 uM preincubated before GTP addition and measured at 1 min intervals for 90 mins by fluorescence based assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and bioevaluation of diarylpyrazoles as antiproliferative agents.
AID366989Cytotoxicity against mouse B16 cells after 72 hrs by MTT assay2008European journal of medicinal chemistry, Sep, Volume: 43, Issue:9
1,2,3,4-tetrahydro-2-thioxopyrimidine analogs of combretastatin-A4.
AID1126004Antimicrotubule activity in human HeLa cells assessed as reduction of interphase microtubule network at 1 uM after 24 hrs by indirect immunofluorescence technique2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1706476Antiproliferative activity against human A549 cells assessed as reduction in cell growth after 48 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Development of triazolothiadiazine derivatives as highly potent tubulin polymerization inhibitors: Structure-activity relationship, in vitro and in vivo study.
AID8847Cytotoxic activity against A-549 cell line2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
A new family of quinoline and quinoxaline analogues of combretastatins.
AID1126011Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/M phase at 1 uM after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 15.50%)2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1317608Inhibition of porcine brain tubulin polymerization at 50 uM measured every 1 min for 40 mins in presence of GTP2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1533679Antiangiogenic activity in Leghorn chicken embryo chorioallantoic membrane assessed as induction of hemorrhages at 2.5 nmol after 24 hrs by light microscopic analysis2019European journal of medicinal chemistry, Feb-01, Volume: 163New naphthopyran analogues of LY290181 as potential tumor vascular-disrupting agents.
AID1403614Induction of apoptosis in human HeLa cells assessed as late apoptotic cells at 100 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2%)2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
AID1422795Cytotoxicity against human LO2 cells after 72 hrs by MTT assay
AID685189Growth inhibition of human SF268 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1862628Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule network polymerization after 30 mins by immunofluorescence analysis2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID455041Inhibition of tubulin polymerization2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID1235359Antiproliferative activity against human KB cells after 72 hrs by methylene blue assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes.
AID455033Cytotoxicity against human SF295 cells after 48 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID387310Antiproliferative activity against mouse L1210 cells after 2 days2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.
AID1064415Growth inhibition of human HCC2998 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID669459Growth inhibition of paclitaxel-resistant human SKOV3 cells after 48 hrs by SRB assay2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID1534526Antiproliferative activity against human K562R cells after 72 hrs by MTS assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID590611Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 1 uM after 48 hrs by flow cytometric analysis2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Design, synthesis, and biological evaluation of novel γ-carboline ketones as anticancer agents.
AID145214Inhibition of human NCI-H460 (human lung large cell carcinoma, MDR negative) cell growth2002Journal of medicinal chemistry, Apr-11, Volume: 45, Issue:8
Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation.
AID627393Antiproliferative activity against human M21 cells after 48 hrs by SRB assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID403644Cytotoxicity against human SF268 cells after 48 hrs by sulforhodamine B assay2005Journal of natural products, Oct, Volume: 68, Issue:10
Antineoplastic agents. 509: synthesis of fluorcombstatin phosphate and related 3-halostilbenes(1).
AID314024Antiproliferative activity against human SF539 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID552572Induction of cell cycle arrest in human KB cells assessed as accumulation at subG1 phase at 20 nM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 0.7%)2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis of antiproliferative flavones from calycopterin, major flavonoid of Calycopteris floribunda Lamk.
AID1411615Toxicity in ip dosed DBA/2 mouse assessed as reduction in 15% body weight administered as daily dose for 3 days2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID214196The compound was tested for the % inhibition of [3H]colchicine binding to tubulin at a concentration of 1 uM1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Antitumor agents. 181. Synthesis and biological evaluation of 6,7,2',3',4'-substituted-1,2,3,4-tetrahydro-2-phenyl-4-quinolones as a new class of antimitotic antitumor agents.
AID1757336Antitumor activity against human H22 cells xenografted in ICR mouse assessed as reduction of tumor weight at 20 mg/kg/day, iv for 21 days2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID658921Induction of cell cycle arrest in human HeLa cells assessed as accumulation at S phase at 10 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 39.9 %)2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
AID1832144Metabolic stability in human liver microsomes assessed as parent compound remaining after 15 mins2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID1263286Cytotoxicity against human MDA-MB-231 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID642112Induction apoptosis in human HeLa cells at 10 nM after 24 hrs by Annexin V-based flow cytometry analysis2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1324099Cytotoxicity against human NCI-H522 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1711856Induction of apoptosis in human MCF7 cells assessed as live cells at 50 nM measured after 48 hrs by annexinV-FITC/propidium iodide staining based flow cytometry (Rvb = 0.6 %)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID1324133Cytotoxicity against human ACHN cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID595054Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetry2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis, biological evaluation, and molecular docking studies of resveratrol derivatives possessing chalcone moiety as potential antitubulin agents.
AID1524341Inhibition of [3H]colchicine binding to bovine brain tubulin at 50 uM after 20 mins relative to control2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents.
AID1736448Antiproliferative activity against human HEK293T cells incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID502720Growth inhibition of human HCT15 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1737826Inhibition of tubulin polymerization in human HeLa cells assessed as disorganized fibrous microtubule structure with reduced density at 10 nM incubated for 24 hrs by immunofluorescence assay2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID314018Antiproliferative activity against human RXF393 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID730202Antiproliferative activity against quesicent HUVECs after 48 hrs by CCK-8 assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Synthesis and structure-activity relationships of N-methyl-5,6,7-trimethoxylindoles as novel antimitotic and vascular disrupting agents.
AID1064407Growth inhibition of human SF539 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1424793Growth inhibition of human NCI/ADR-RES cells after 96 hrs by trypan blue exclusion assay2018European journal of medicinal chemistry, May-25, Volume: 152New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors.
AID685165Cytotoxicity against human IMR32 cells after 48 hrs assessed as inhibition of cell growth at 10 uM after 48 hrs by SRB assay relative to control2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID746664Cell cycle arrest in mouse NIH/3T3 cells assessed as accumulation at G0/G1 phase at 0.05 uM after 24 hrs by propidium iodide staining-based FACS flow cytometric analysis (Rvb = 39.91%)2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Design, synthesis, cytotoxic evaluation and tubulin inhibitory activity of 4-aryl-5-(3,4,5-trimethoxyphenyl)-2-alkylthio-1H-imidazole derivatives.
AID665693Cytotoxicity against human A549 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID1274781Inhibition of porcine tubulin polymerization assessed as inhibition of tubulin assembly Vmax rate at 10 uM by spectrophotometric analysis2016Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1
Synthesis and Biochemical Evaluation of 3-Phenoxy-1,4-diarylazetidin-2-ones as Tubulin-Targeting Antitumor Agents.
AID415687Cytotoxicity against human MCF7 cells after 72 hrs by MTS assay2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
Synthesis and biological evaluation of cis-locked vinylogous combretastatin-A4 analogues: derivatives with a cyclopropyl-vinyl or a cyclopropyl-amide bridge.
AID1352873Antimitotic activity against Paracentrotus lividus embryo assessed as embryo spinning after 15 mins to 20 hrs by light microscopy2018European journal of medicinal chemistry, Feb-25, Volume: 146Regioselective synthesis of 3,4-diaryl-5-unsubstituted isoxazoles, analogues of natural cytostatic combretastatin A4.
AID636066Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetry2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Design, synthesis, biological evaluation and molecular modeling of 1,3,4-oxadiazoline analogs of combretastatin-A4 as novel antitubulin agents.
AID685207Growth inhibition of human OVCAR4 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1771520Induction of apoptosis in human MGC-803 cells assessed as necrotic cells at 2 nM measured after 48 hrs by Annexin V-APC/PI double staining based flow cytometry assay (Rvb = 0.44%)2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID455990Cytotoxicity against human CEM cells after 2 days2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of tubulin polymerization.
AID1057116Drug metabolism in PBS at pH 7.4 assessed as product-1 level after 24 hrs by HPLC analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID1158428Inhibition of [3H]colchicine binding to pig brain tubulin at 5 uM2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
AID1059990Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by coulter counting analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
AID1586359Antiproliferative activity against human MCF7 cells by MTT assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4.
AID657879Growth inhibition of human SF268 cells after 48 hrs by sulforhodamine B assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID1518089Induction of apoptosis in human MDA-MB-468 cells assessed as necrotic cells at 100 nM after 72 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 0.97 to 1.29%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID616982Antiproliferative activity against human AU565 after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1196878Cell cycle arrest in human SH-SY5Y cells assessed as accumulation at G2/M phase at 3 times IC50 after 16 hrs by flow cytometry (Rvb = 18.5 %)2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID1406347Growth inhibition of human HeLa cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation.
AID737098Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 20 mins by turbidimetric analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b]thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents.
AID769830Relative resistance, ratio of IC50 for M6-6 in human SKOV3 cells to IC50 for human SKOV3 cells2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.
AID662349Antiproliferative activity in human SK-N-BE cells assessed as cell viability after 72 hrs by MTT assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID455038Cytotoxicity against human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
AID1068622Growth inhibition of human NCI-H522 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1689083Inhibition of IDO1 expression in hIFNgamma-stimulated human HeLa cells at 0.5 uM measured after 24 hrs by western blot assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1757894Antiproliferative activity against human NCI/ADR-RES cells overexpressing Pgp2021Bioorganic & medicinal chemistry letters, 06-01, Volume: 41Novel pyrazolo[4,3-d]pyrimidine microtubule targeting agents (MTAs): Synthesis, structure-activity relationship, in vitro and in vivo evaluation as antitumor agents.
AID214162Ability to inhibit colchicine binding1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antitumor agents. 150. 2',3',4',5',5,6,7-substituted 2-phenyl-4-quinolones and related compounds: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.
AID745605Darktoxicity against human MCF7 cells incubated for 24 hrs followed by 30 mins incubation in dark measured after 3 days by MTT assay2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Site-specific and far-red-light-activatable prodrug of combretastatin A-4 using photo-unclick chemistry.
AID550210Antimitotic activity against Paracentrotus lividus embryo assessed as cleavage arrest after 2.5 to 6 hrs post fertilization by sea urchin embryo assay2010Journal of natural products, Nov-29, Volume: 73, Issue:11
Synthesis of antimitotic polyalkoxyphenyl derivatives of combretastatin using plant allylpolyalkoxybenzenes.
AID1179657Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetric method2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Design, synthesis and biological evaluation of (E)-3-(3,4-dihydroxyphenyl)acrylylpiperazine derivatives as a new class of tubulin polymerization inhibitors.
AID1348626Induction of basal contraction tone in isolated Wistar rat aorta rings at 10 uM after 10 mins in presence K60 solution (Rvb = 0.2 +/- 0.2%)2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID1917300Antiproliferative activity against human SW620 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID1585987Cytotoxicity against human MDA-MB-468 cells after 72 hrs by MTT assay
AID1324131Cytotoxicity against human UO31 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1906259Antimigratory activity against human HeLa cells at 3 nM measured after 24 hrs by scratch wound healing based fluorescence inverted microscopic analysis
AID1595692Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID403051Inhibition of bovine brain tubulin assembly2005Journal of natural products, Aug, Volume: 68, Issue:8
Antineoplastic agents. 515. Synthesis of human cancer cell growth inhibitors derived from 3,4-methylenedioxy-5,4'-dimethoxy-3'-amino-Z-stilbene.
AID1637529Inhibition of tubulin polymerization in human HeLa cells assessed as induction of microtubule disruption at 60 nM after 48 hrs by confocal microscopic analysis2016Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18
Design and synthesis of cis-restricted benzimidazole and benzothiazole mimics of combretastatin A-4 as antimitotic agents with apoptosis inducing ability.
AID1689025Binding affinity to tubulin in human MCF7 cells assessed as inhibition of tubulin-EBI adduct formation preincubated for 2 hrs followed by EBI addition and measured after 1.5 hrs by Western blotting analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells.
AID502753Growth inhibition of human T47D cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1711859Induction of apoptosis in human MCF7 cells assessed as necrotic cells at 50 nM measured after 48 hrs by annexinV-FITC/propidium iodide staining based flow cytometry (Rvb = 0.1 %)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID1353660Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 50 nM after 20 hrs by propidium iodide staining based flow cytometry (Rvb = 16 +/- 1%)2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID1887833Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR.
AID391278Cytotoxicity against BMEC by sulforhodamine B test2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Novel A-ring and B-ring modified combretastatin A-4 (CA-4) analogues endowed with interesting cytotoxic activity.
AID1119742Growth inhibition of human DU145 cells by sulforhodamine B assay2012MedChemComm, Jun, Volume: 3, Issue:6
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
AID1819034Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G2/M phase incubated for 24 hrs by propidium iodide staining based flow cytometric analysis2022Journal of natural products, 01-28, Volume: 85, Issue:1
Chemical Space Expansion of Flavonoids: Induction of Mitotic Inhibition by Replacing Ring B with a 10π-Electron System, Benzo[
AID1757290Inhibition of [3H]colchicine binding to biotinylated pig brain tubulin at 1 uM incubated for 2 hrs in presence of GTP by competitive scintillation proximity assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1506734Antiproliferative activity in human MCF7 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay2017MedChemComm, Feb-01, Volume: 8, Issue:2
Synthesis and biological evaluation of (-)-kunstleramide and its derivatives.
AID1689068Anticancer activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID319822Cytotoxicity against human HCT116 cells2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and antitumor activity of benzils related to combretastatin A-4.
AID384967Cell cycle arrest in human NCI-H460 cells assessed as G0/G1 phase accumulation after 24 hrs by flow cytometry2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
Synthesis and biological activity of fluorinated combretastatin analogues.
AID1778191Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition after 48 hrs by MTT assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines.
AID1294474Growth inhibition of human HT-29 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID276455Cytotoxicity against NCI-H460 cells2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
Novel imidazole-based combretastatin A-4 analogues: evaluation of their in vitro antitumor activity and molecular modeling study of their binding to the colchicine site of tubulin.
AID1422817Antitumor activity against human H22 cells xenografted in ICR mouse assessed as reduction in tumor weight at 15 mg/kg, iv qd for 21 consecutive days
AID616890Inhibition of tubulin polymerization by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1534361Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
AID1068614Growth inhibition of human SF268 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID685369Growth inhibition of human BT549 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1873710Induction of apoptosis in human HeLa cells assessed as late apoptotic cells at 10 nM incubated for 24 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 0.05%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID376522Cytotoxicity against mouse L1210 cells2000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID1890478Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells in G2/G1 phase at 10 uM incubated for 24 hrs by PI staining based flow cytometry analysis (Rvb = 1.80 %)2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
AID452621Antiproliferative activity against human A2780 cells after 5 days by MTT assay2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID1766188Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Design, synthesis and biological evaluation of novel acridine and quinoline derivatives as tubulin polymerization inhibitors with anticancer activities.
AID691651Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as effect on lymphocyte count at 30 mg/kg, ip qd after 21 day (Rvb = 15.88 +/- 0.41 x 10'3 mm'-3)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1409112Induction of microtubule depolymerization in rat A10 cells assessed as cellular microtubule loss incubated for 18 hrs by DAPI staining-based indirect immunofluorescence assay2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.
AID1732752Antiproliferative activity against multidrug-resistant human MES-SA/Dx5 cells assessed as reduction in cell viability incubated for 72 hrs by prestoblue dye based assay2021European journal of medicinal chemistry, Apr-05, Volume: 215Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies.
AID629597Antiproliferative activity against human CEM cells after 2 days by coulter counter analysis2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID1392077Antiproliferative activity against human HeLa cells by SRB assay2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.
AID1183714Cytotoxicity against human HCT15 cells assessed as growth inhibition after 72 hrs by CellTitre-Glo assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID1635335Relative ratio of IC50 for human SKOV3 cells expressing MDR1-M6/6 to IC50 for human SKOV3 cells2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID52671Antitumor activity at dose 160 mg/kg in murine colon26 cells1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel combretastatin analogues effective against murine solid tumors: design and structure-activity relationships.
AID376523Inhibition of bovine tubulin polymerization2000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID1185444Displacement of [3H]colchicine from long-chain biotin-labeled tubulin (unknown origin) at 1 uM after 2 hrs by competition-binding scintillation proximity assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Concise syntheses of 7-anilino-indoline-N-benzenesulfonamides as antimitotic and vascular disrupting agents.
AID526642Aqueous solubility of the compound in buffer at pH 7 after 24 hrs by shake-flask method2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
Discovery of novel 2-aryl-4-benzoyl-imidazoles targeting the colchicines binding site in tubulin as potential anticancer agents.
AID1628403Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Design, Synthesis, and Biological Evaluation of 1-Methyl-1,4-dihydroindeno[1,2-c]pyrazole Analogues as Potential Anticancer Agents Targeting Tubulin Colchicine Binding Site.
AID1906236Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 1.5 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 18.8%)
AID1064404Growth inhibition of human MALME-3M cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID622608Inhibition of bovine brain tubulin polymerization pre-incubated for 15 mins at 30 degC, cooled followed by 0.3 hr acquisition at 30 degC by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1731994Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Novel diaryl-2H-azirines: Antitumor hybrids for dual-targeting tubulin and DNA.
AID1351598Inhibition of porcine tubulin polymerization after 1 hr by spectrophotometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1158424Induction of pig brain tubulin depolymerization by spectrophotometric analysis2014Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
AID1392075Antiproliferative activity against human SKOV3-MDR1-M6/6 cells by SRB assay2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.
AID1376365Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured after 20 mins by spectrophotometric method
AID1524380Antitumor activity mouse B16-BL6 cells implanted in C57BL/6 mouse assessed tumor growth inhibition at 30 mg/kg, ip dosed every other day for 18 days relative to control2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents.
AID658922Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 10 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 16.2 %)2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
AID1873728Induction of apoptosis in human HeLa cells assessed as viable cells at 10 nM incubated for 48 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 85.5%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID1068617Growth inhibition of human HT-29 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1593626Activation factor, ratio of antiproliferative IC50 of ER positive human MCF7 cells expressing low level of CYP to antiproliferative IC50 of TCCD-induced ER positive human MCF7 cells expressing CYP1A12019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells.
AID1408395Induction of apoptosis in human K562 cells at 0.001 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.46%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1698446Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Ultrasound assisted synthesis of tetrazole based pyrazolines and isoxazolines as potent anticancer agents via inhibition of tubulin polymerization.
AID1824149Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 5 nM measured after 48 hrs by flow cytometric analysis (Rvb = 17.9 + /- 6 %)2022European journal of medicinal chemistry, Feb-05, Volume: 229Branched alkyl of phenyl 4-(2-oxo-3-alkylimidazolidin-1-yl)benzenesulfonates as unique cytochrome P450 1A1-activated antimitotic prodrugs: Biological evaluation and mechanism of bioactivation.
AID685171Growth inhibition of human MOLT4 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID717160Antiproliferative activity against human Jurkat cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
AID1647037Toxicity in ICR mouse xenografted with mouse H22 cells assessed as change in spleen weight at 30 mg/kg, iv administered once daily for 21 consecutive days2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1336776Induction of mitochondrial membrane potential loss in human A549 cells assessed as intact mitochondrial membrane at 100 nM after 48 hrs by JC-1 staining based flow cytometry (Rvb = 95.9%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID685162Cytotoxicity against human A549 cells assessed as inhibition of cell growth at 10 uM after 48 hrs by SRB assay relative to control2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1231335Induction of apoptosis in human MV4-11 cells assessed as phosphatidylserine externalization at 0.0075 and 5 uM after 48 hrs by AnnexinV/propidium iodide staining based Tali-image based cytometry2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4.
AID1205514Antiproliferative activity against human HL60 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.
AID1689092Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G1 phase at 0.5 uM measured after 24 hrs by propidium iodide/RNAse staining based flow cytometry (Rvb = 61.5%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1677374Inhibition of bovine brain tubulin assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by turbidimetry-based spectrophotometric method
AID662343Antiproliferative activity in human HuTu 80 cells assessed as cell viability after 72 hrs by MTT assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID665814Cell cycle arrest in human A549 cells assessed as cell accumulation at subG1 phase at 2 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 1.09%)2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Synthesis of chalcone-amidobenzothiazole conjugates as antimitotic and apoptotic inducing agents.
AID1689135Cytotoxicity against human HCT-116 p53 mutant cells assessed as inhibition of cell growth after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.
AID1408389Cell cycle arrest in human K562 cells assessed as accumulation at G2 phase at 0.02 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 9.51%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1064375Growth inhibition of human Hs578T cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID376527Antibacterial activity against Neisseria gonorrhoeae by disk susceptibility test2000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID1487505Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay2017Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
Design and synthesis of 4-morpholino-6-(1,2,3,6-tetrahydropyridin-4-yl)-N-(3,4,5-trimethoxyphenyl)-1,3,5-triazin-2-amine analogues as tubulin polymerization inhibitors.
AID1064376Growth inhibition of human BT549 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID305459Cytotoxicity against human HepG2 cells2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and cytotoxic activities of 4,5-diarylisoxazoles.
AID1475517Inhibition of tubulin (unknown origin) assembly preincubated for 15 mins followed by GTP addition measured after 20 mins by turbidimetric method2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
In Vivo and Mechanistic Studies on Antitumor Lead 7-Methoxy-4-(2-methylquinazolin-4-yl)-3,4-dihydroquinoxalin-2(1H)-one and Its Modification as a Novel Class of Tubulin-Binding Tumor-Vascular Disrupting Agents.
AID214019Inhibition of tubulin polymerization reported as IC502002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.
AID1126018Displacement of colchicine from tubulin (unknown origin) at 0.1 to 125 uM after 1 hr by HPLC-MS/MS analysis2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1757291Inhibition of [3H]colchicine binding to biotinylated pig brain tubulin at 5 uM incubated for 2 hrs in presence of GTP by competitive scintillation proximity assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1906260Antimigratory activity against human HeLa cells at 6 nM measured after 24 hrs by scratch wound healing based fluorescence inverted microscopic analysis
AID1562380Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin.
AID421862Antitumor activity against human DU145 cells by sulforhodamine B assay2009Journal of natural products, Mar-27, Volume: 72, Issue:3
Antineoplastic agents. 578. Synthesis of stilstatins 1 and 2 and their water-soluble prodrugs.
AID1628399Growth inhibition of human HeLa cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Design, Synthesis, and Biological Evaluation of 1-Methyl-1,4-dihydroindeno[1,2-c]pyrazole Analogues as Potential Anticancer Agents Targeting Tubulin Colchicine Binding Site.
AID1597715Antiproliferative activity against human COLO205 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Sep-01, Volume: 1771-Phenyl-dihydrobenzoindazoles as novel colchicine site inhibitors: Structural basis and antitumor efficacy.
AID666749Antivascular activity against human EAhy926 cells assessed as the minimum concentration required to elicit rounding up of cells after 2 hrs by microscopic analysis2012European journal of medicinal chemistry, Aug, Volume: 54In vitro and in vivo biological evaluation of new 4,5-disubstituted 1,2,3-triazoles as cis-constrained analogs of combretastatin A4.
AID1689072Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 0.5 uM measured after 24 hrs by propidium iodide/RNAse staining based flow cytometry (Rvb = 10.7%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID771206Cytotoxicity against taxol-resistant human MX1 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID269719Cell cycle arrest in SHSY5Y cells by accumulation at G2 phase after 8 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID1518079Induction of apoptosis in human MDA-MB-468 cells assessed as early apoptotic cells at 100 nM after 24 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 0.35 to 1.25%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1570322Antiviral activity against Zika virus infected in human HuH7 cells assessed as reduction in viral titer at 5 uM measured after 24 hrs by Cell-Titer Glo luminescent assay relative to control2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.
AID1647044Toxicity in immunocompetent BALB/c nude mouse xenografted with human A549 cells assessed as effect on liver damage or inflammation at 30 mg/kg, iv administered once daily for 29 consecutive days measured after 29 days by hematoxylin-eosin staining based f2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1860222Selectivity index, ratio of IC50 for human L02 cells to IC50 for human HepG2 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-functional antitumor conjugates improving the anti-metastasis effect of combretastatin A4 by targeting tubulin polymerization and matrix metalloproteinases.
AID404579Inhibition of calf brain tubulin polymerization at 20 uM after 20 mins2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Diarylmethyloxime and hydrazone derivatives with 5-indolyl moieties as potent inhibitors of tubulin polymerization.
AID103369Inhibitory activity against tubulin (1.0 mg/mL) assembly was determined2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Antineoplastic agents. 487. Synthesis and biological evaluation of the antineoplastic agent 3,4-methylenedioxy-5,4'-dimethoxy-3'-amino-Z-stilbene and derived amino acid amides.
AID1711848Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 50 nM measured after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 3.1 %)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID442973Growth inhibition of human NCI-H460 cells after 3 days by crystal violet staining2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Vascular disrupting activity of tubulin-binding 1,5-diaryl-1H-imidazoles.
AID658919Inhibition of bovine brain tubulin polymerization by thermostatic spectrophotometer2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
AID1162817Cytotoxicity against human ACHN cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID1285329Inhibition of porcine brain tubulin polymerization after 1 hr by fluorescence assay2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID280077Antiproliferative activity against drug resistant H69AR cell line expressing MRP1 by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID452432Cell cycle arrest in human K562 cells assessed as accumulation at S phase at 20 nM after 24 hrs by propidium iodide staining-based flow cytometry2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: synthesis and biological evaluation of antivascular activity.
AID437550Anticancer activity against human CCRF-CEM cells after 72 hrs2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines).
AID376524Displacement of [3H]colchicine from bovine tubulin at inhibitor to colchicine ratio of 0.2:12000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID1586368Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 0.2 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 10 +/- 0.8%)2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4.
AID746670Inhibition of sheep brain microtubule polymerization at 2 uM after 15 mins by UV-vis spectrophotometric analysis2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Design, synthesis, cytotoxic evaluation and tubulin inhibitory activity of 4-aryl-5-(3,4,5-trimethoxyphenyl)-2-alkylthio-1H-imidazole derivatives.
AID1612617Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID761832Cytotoxicity against human 786 cells after 48 hrs by sulforhodamine B assay2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity.
AID1334735Antiproliferative activity against human Bel7402 assessed as reduction in cell viability measured after 48 hrs by SRB assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility.
AID1064373Growth inhibition of human T47D cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1353643Inhibition of calf brain tubulin polymerization in glycerol-assembly buffer assessed as critical concentration for tubulin assembly at 27.5 uM measured every 30 secs for 2 hrs in presence of GTP (Rvb = 8+/- 1 uM)2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID1351663Inhibition of tubulin polymerization in human MDA-MB-231 cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1667131Inhibition of tubulin polymerization (unknown origin) at 10 uM relative to control2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological evaluation of novel pyrazolo[3,4-b]pyridines as cis-restricted combretastatin A-4 analogues.
AID1593629Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 96 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells.
AID1458818Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID1466246Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jul-07, Volume: 134Synthesis and biological evaluation of novel indole-pyrimidine hybrids bearing morpholine and thiomorpholine moieties.
AID306481Growth inhibition of human M21 cells2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1498594Inhibition of tubulin (unknown origin) polymerization preincubated for 15 mins followed by GTP addition measured for 20 mins by turbidimetric analysis2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
The inhibitory effect of kokusaginine on the growth of human breast cancer cells and MDR-resistant cells is mediated by the inhibition of tubulin assembly.
AID778973Displacement of [3H]colchicine from tubulin (unknown origin) at 5 uM after 10 mins by scintillation counting analysis2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Synthesis and biological evaluation of indole-based, anti-cancer agents inspired by the vascular disrupting agent 2-(3'-hydroxy-4'-methoxyphenyl)-3-(3″,4″,5″-trimethoxybenzoyl)-6-methoxyindole (OXi8006).
AID617014Antiproliferative activity against beta3-tubulin overexpressing human HeLa cells2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Synthesis and biological activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride as potent cytotoxic antitubulin agents.
AID494828Induction of apoptosis in human MCF7 cells assessed as decrease in procaspase 7 level at 30 uM after 24 hrs by Western blot analysis2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
Synthesis and anti-cancer activity of chalcone linked imidazolones.
AID1431174Inhibition of EGFR in human A431 cells assessed as reduction in EGF induced phosphorylation preincubated for 60 mins followed by EGF addition measured after 10 mins by ELISA method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
AID580348tubulin-destabilizing activity in sea urchin embryo assessed as embryo spinning treated immediately 8 to 10 hrs after fertilization2011Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6
Application of plant allylpolyalkoxybenzenes in synthesis of antimitotic phenstatin analogues.
AID228455Inhibition of tubulin polymerization1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Synthesis and evaluation of analogues of (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene as potential cytotoxic and antimitotic agents.
AID1317587Antiproliferative activity against mouse Colon 26 cells measured after 72 hrs by MTT assay2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1278675Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID317744Displacement of [3H]colchicine from tubulin2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID1336760Inhibition of porcine brain tubulin polymerization in presence of GTP by fluorescence assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID213999Concentration inhibiting tubulin polymerization (ITP)1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor agents. 196. Substituted 2-thienyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.
AID1431175Inhibition of PDGFR-beta in human SF539 cells assessed as reduction in PDGF-BB induced phosphorylation preincubated for 60 mins followed by PDGF-BB addition measured after 10 mins by ELISA method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
AID306510Cell cycle arrest in human M21 cells assessed as accumulation at S phase at 0.015 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1348618Antiproliferative activity against human A549 cells after 72 hrs by resazurin-based fluorescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID1162818Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.
AID1231334Induction of apoptosis in human Saos2 cells assessed as phosphatidylserine externalization at 0.01 and 5 uM after 48 hrs by AnnexinV/propidium iodide staining based Tali-image based cytometry2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Antimitotic activity of structurally simplified biaryl analogs of the anticancer agents colchicine and combretastatin A4.
AID265416Antiproliferative activity against doxorubicin-resistant human A2780-dx cells2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID1771491Inhibition of tubulin polymerization in human MGC-803 cells assessed as change in shape of nucleus at 2 to 7.5 nM measured after 48 hrs by Hoechst staining based confocal microscopy analysis2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1200589Stability assessed as cis-trans isomerization equilibrium at 1.5 x 10'-2 M under natural light conditions after 7 days by LC-HRMS method2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Quantum chemistry calculation-aided structural optimization of combretastatin A-4-like tubulin polymerization inhibitors: improved stability and biological activity.
AID1570326Prodrug activation assessed as Dengue virus serotype 2 NS2B-NS3 protease expressed in Escherichia coli BL21 lambda (DE3) cells-mediated compound hydrolysis in TRIS buffer at pH 9 at 500 uM incubated for 2 hrs by HPLC-UV analysis2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.
AID1906262Antiproliferative activity against human HeLa/DDP cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
AID1324129Cytotoxicity against human RXF393 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID247967Concentration required to inhibit murine mammary carcinoma FM3A cell line proliferation2005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
AID1757275Antiproliferative activity against human HCT-8 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1403612Induction of apoptosis in human HeLa cells assessed as live cells at 100 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 96.5%)2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
AID444156Ratio of EC50 for rat A10 cells to IC50 for human MDA-MB-435 cells2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID750811Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 20 mins2013European journal of medicinal chemistry, Jun, Volume: 64Cytotoxic activities of substituted 3-(3,4,5-trimethoxybenzylidene)-1,3-dihydroindol-2-ones and studies on their mechanisms of action.
AID1308611Half life in Sprague-Dawley rat liver microsomes in presence of NADPH regenerating system by HPLC method2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID751513Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.
AID93856Inhibitory concentration against camptothecin (CPT) resistant cell line (KB-100) using tetrazolium dye reduction assay (MTT)2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID1508158Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 2 uM after 48 hrs by flow cytometric analysis (Rvb = 57.7%)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID616971Antiproliferative activity against human HAAE1 grown in presence of growth factors after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID757692Cytotoxicity against human CEM cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Synthesis and antitumor activity of novel 3,4-diaryl squaric acid analogs.
AID1832106Antiproliferative activity against human HeLa assessed as reduction in cell viability measured after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID299203Antiproliferative activity against human Molt3 cells2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity relationships.
AID387314Inhibition of bovine brain tubulin polymerization for 20 mins by turbidimetry2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.
AID1873751Induction of apoptosis in human HeLa cells assessed as necrotic cells at 10 nM incubated for 72 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 2.88 %)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID317993Displacement of [3H]colchicine from bovine tubulin at 5 uM2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors.
AID1711855Inhibition of porcine brain tubulin polymerization measured after 1 hr in presence of GTP by fluorescence assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID1266263Inhibition of tubulin polymerization in human HeLa cells assessed as increase in soluble fraction incubated for 16 hrs by cellular assay2016Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
Triazole-curcuminoids: A new class of derivatives for 'tuning' curcumin bioactivities?
AID1408384Cell cycle arrest in human K562 cells assessed as accumulation at G1 phase at 0.01 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 41.08%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID273278Antiproliferative activity against human Molt4/C8 cells2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.
AID1352573Antiproliferative activity against human H460 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Synthesis and biological evaluation of 4,6-diphenyl-2-(1H-pyrrol-1-yl)nicotinonitrile analogues of crolibulin and combretastatin A-4.
AID758694Inhibition of bovine brain tubulin assembly after 15 mins by spectrophotometric analysis2013European journal of medicinal chemistry, Jul, Volume: 652-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action.
AID1733024Antiproliferative activity against human K562 cells assessed as cell growth inhibition by MTT assay2021Bioorganic & medicinal chemistry letters, 04-15, Volume: 38Synthesis, biological evaluation, and structure-activity relationships of new tubulin polymerization inhibitors based on 5-amino-1,2,4-triazole scaffold.
AID1288164Antiproliferative activity against human A2780 cells assessed as cell viability after 48 hrs by MTT assay2016European journal of medicinal chemistry, May-23, Volume: 114Synthesis and biological evaluation of quinoline analogues of flavones as potential anticancer agents and tubulin polymerization inhibitors.
AID492264Displacement of [3H]colchicine from bovine brain tubulin at 5 uM2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Substituted 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]thiophene derivatives as potent tubulin polymerization inhibitors.
AID722280Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 5 uM incubated for 10 mins at 37 degC2013Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
Synthesis and biological evaluation of N-alkyl-N-(4-methoxyphenyl)pyridin-2-amines as a new class of tubulin polymerization inhibitors.
AID1600477Induction of apoptosis in human CCRF-CEM cells assessed as accumulation at subG1 phase at antiproliferative IC50 incubated for 24 hrs by PI staining based flow cytometric analysis (Rvb = 3.71%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1773164Induction of apoptosis in human A549 cells assessed as increase in early apoptotic cells at 500 nM measured after 24 hrs by PI/FITC analysis (Rvb = 0.955%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID276454Cytotoxicity against MDR HCT15 cells2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
Novel imidazole-based combretastatin A-4 analogues: evaluation of their in vitro antitumor activity and molecular modeling study of their binding to the colchicine site of tubulin.
AID1432894Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Development of a novel near-infrared fluorescent theranostic combretastain A-4 analogue, YK-5-252, to target triple negative breast cancer.
AID1666239Antiproliferative activity against human HT-29 cells incubated for 48 hrs by MTT assay2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.
AID1647002Induction of apoptosis in human HepG2 cells assessed as early apoptotic cells at 0.1 uM measured after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 3.8 %)2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID659048Induction of cell cycle arrest in human HeLa cells assessed as accumulation at S phase at 3 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 39.9 %)2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
AID1263253Cytotoxicity against human NCI-H23 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID685179Growth inhibition of human NCI-H23 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1233595Induction of cell cycle arrest in human M21 cells assessed as cells accumulation at subG1 phase at 10 nM after 24 hrs by flow cytometry (Rvb = 1.2%)2015European journal of medicinal chemistry, Jul-15, Volume: 100Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model.
AID1575815Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay2019MedChemComm, Aug-01, Volume: 10, Issue:8
Synthesis and biological evaluation of structurally diverse α-conformationally restricted chalcones and related analogues.
AID382333Cytotoxicity against human SKOV cells assessed as [3H]thymidine incorporation after 72 hrs by microplate scintillation counter2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin.
AID228627Inhibition of colchicine binding2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
AID455993Displacement of [3H]colchicine from bovine tubulin at 5 uM2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of tubulin polymerization.
AID685182Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1462294Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis of different heterocycles-linked chalcone conjugates as cytotoxic agents and tubulin polymerization inhibitors.
AID1882908Displacement of [3H] colchicine from tubulin (unknown origin) at 5 uM measured after 2 hrs by scintillation counting analysis relative to control2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1917031Cytotoxicity against human MGC-803 cells assessed as cell growth inhibition2022European journal of medicinal chemistry, Nov-05, Volume: 241Recent advances in combretastatin A-4 codrugs for cancer therapy.
AID1196876Cell cycle arrest in human SH-SY5Y cells assessed as accumulation at G0G1 phase at 3 times IC50 after 16 hrs by flow cytometry (Rvb = 70.2 %)2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID1612619Antiproliferative activity against human taxol-resistant HCT8/T cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID307426Cytotoxicity against human HT29 cells2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Synthesis and biological activity of naphthalene analogues of phenstatins: naphthylphenstatins.
AID384965Cytotoxic activity against human NCI-H460 cells after 72 hrs by sulforhodamine B test2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
Synthesis and biological activity of fluorinated combretastatin analogues.
AID552583Induction of cell cycle arrest in human KB cells assessed as accumulation at G2/M phase at 20 nM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 13.8%)2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis of antiproliferative flavones from calycopterin, major flavonoid of Calycopteris floribunda Lamk.
AID1597717Inhibition of bovine brain tubulin polymerization measured every 1 min for 60 mins by turbidimetric assay2019European journal of medicinal chemistry, Sep-01, Volume: 1771-Phenyl-dihydrobenzoindazoles as novel colchicine site inhibitors: Structural basis and antitumor efficacy.
AID214177Inhibition of radiolabeled [3H]colchicine binding to tubulin at a concentration of 2 uM of the compound2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.
AID1426064Inhibition of bovine brain tubulin assembly preincubated for 20 mins followed by GTP addition by turbidometric method2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis, structure-activity relationships and biological evaluation of 7-phenyl-pyrroloquinolinone 3-amide derivatives as potent antimitotic agents.
AID1508163Induction of apoptosis in human MCF7 cells assessed as necrotic cells at 2 uM after 24 hrs by Annexin-V FITC/propidium iodide staining-based FACS analysis (Rvb = 0.2%)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1628254Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 10 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 16%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID266933Inhibition of [3H]colchicine binding to tubulin at 1 uM2006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-5-aryl thiophenes as a new class of potent antitubulin agents.
AID1195294Antiproliferative activity against human SKOV3 cells overexpressing wild type beta3 tubulin after 48 hrs by sulforhodamine B assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID1600485Induction of mitotic block in human CCRF-CEM cells assessed as histone H3 Ser10 phosphorylation level at antiproliferative IC50 incubated for 48 hrs by flow cytometric analysis (Rvb = 0.97%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1059053Cytotoxicity against human AGS cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis, cytotoxic evaluation and molecular docking study of 2-alkylthio-4-(2,3,4-trimethoxyphenyl)-5-aryl-thiazoles as tubulin polymerization inhibitors.
AID1278670Inhibition of bovine brain tubulin polymerization preincubated for 15 mins by spectrophotometric analysis2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID404583Cytotoxicity against human HeLa cells after 72 hrs by XTT method2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Diarylmethyloxime and hydrazone derivatives with 5-indolyl moieties as potent inhibitors of tubulin polymerization.
AID1057115Drug metabolism in PBS at pH 7.4 assessed as product-1 level after 6.5 hrs by HPLC analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID1534365Cytotoxicity against human LO2 cells after 72 hrs by MTT assay2019Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2
Discovery of Novel Quinoline-Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity.
AID1179507Antiproliferative activity against mouse HepG2 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Synthesis, biological evaluation and molecular modeling of 1,3,4-thiadiazol-2-amide derivatives as novel antitubulin agents.
AID1379259Inhibition of bovine brain tubulin polymerization measured for 1 hr at 1 min interval by fluorescence assay relative to control2017European journal of medicinal chemistry, Oct-20, Volume: 139Novel Gomisin B analogues as potential cytotoxic agents: Design, synthesis, biological evaluation and docking studies.
AID1068598Growth inhibition of human IGROV1 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1860526Antiproliferative activity against human FaDu cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC.
AID1809295Antitumor activity against human MCF7 cells xenografted in BALB/c nude mouse assessed as decrease in tumor weight at 20 mg/kg, iv administered every 2 days for 21 days and measured every 2 days
AID685378Inhibition of ERK1/2 phosphorylation in human MCF cells at 4 uM after 24 hrs by Western blot analysis2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1891191Inhibition of tubulin polymerization (unknown origin) measured every minute for 20 mins by fluorescence based assay
AID1185193Displacement of [3H]colchicine from bovine brain tubulin assessed as rate of assembly at 5 uM after 10 mins by liquid scintillation counting2014European journal of medicinal chemistry, Sep-12, Volume: 84Novel 9'-substituted-noscapines: synthesis with Suzuki cross-coupling, structure elucidation and biological evaluation.
AID265435Cell cycle arrest in NCI-H460 cells by accumulation at S phase cell at 160 nM post 24 hrs treatment2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID269715Cell cycle arrest in SHSY5Y cells by accumulation at G1 phase after 8 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID767876Cytotoxicity against human NCI-H460 cells by SRB assay2013Journal of natural products, Sep-27, Volume: 76, Issue:9
Synthesis of a 2-aryl-3-aroyl indole salt (OXi8007) resembling combretastatin A-4 with application as a vascular disrupting agent.
AID717159Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
AID1308538Inhibition of [3H]-colchicine binding to porcine brain tubulin at 5 uM relative to control2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1421772Antiproliferative activity against mouse L929 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Conformation impacts on the bioactivities of SMART analogues.
AID379681Inhibition of topoisomerase 1 in Saccharomyces cerevisiae RS321N in glucose medium by microtiter plate assay2000Journal of natural products, Apr, Volume: 63, Issue:4
Bioactive compounds from Combretum erythrophyllum.
AID1405369Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID449213Inhibition of tubulin polymerization after 20 mins by spectrophotometry2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
AID1882893Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1119743Growth inhibition of human SKOV3 cells by sulforhodamine B assay2012MedChemComm, Jun, Volume: 3, Issue:6
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
AID1600475Therapeutic index, ratio of IC50 for HUVEC to IC50 for human HCT116 cells2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1873775Induction of mitochondrial membrane potential alteration in human HeLa cells assessed as necrotic cells at 10 nM measured after 48 hrs by JC1 staining-based flow cytometry analysis (Rvb = 0%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID613265Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetry analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and biological evaluation of 1-(4'-Indolyl and 6'-Quinolinyl) indoles as a new class of potent anticancer agents.
AID669460Growth inhibition of human MCF7 cells after 48 hrs by SRB assay2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID1408367Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1873680Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID1205512Antiproliferative activity against human RS4:11 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.
AID1125809Inhibition of bovine brain tubulin polymerization measured every 30 sec for 30 mins by spectrophotometry2014European journal of medicinal chemistry, Apr-22, Volume: 77Antimitotic and vascular disrupting agents: 2-hydroxy-3,4,5-trimethoxybenzophenones.
AID1693357Inhibition of [3H]colchicine binding to bovine tubulin at 5 uM measured after 10 mins by scintillation counting2021Bioorganic & medicinal chemistry, 01-01, Volume: 29The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
AID1737796Antiproliferative activity against human A2780 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID1689137Cytotoxicity against human 518A2 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.
AID1338085Inhibition of porcine brain tubulin polymerization measured every 60 secs for 90 mins by fluorescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of cyclic-indole derivatives as anti-tumor agents via the inhibition of tubulin polymerization.
AID1518086Induction of apoptosis in human MDA-MB-468 cells assessed as viable cells at 100 nM after 72 hrs by Annexin-FITC/propidium iodide staining based flow cytometry (Rvb = 96.8%)2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1647048Toxicity in immunocompetent BALB/c nude mouse xenografted with human A549 cells assessed as effect on heart damage or inflammation at 30 mg/kg, iv administered after 29 consecutive days measured hematoxylin-eosin staining based fluorescence microscopy2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1667120Antiproliferative activity against human KYSE-150 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and biological evaluation of novel pyrazolo[3,4-b]pyridines as cis-restricted combretastatin A-4 analogues.
AID657880Growth inhibition of human NCI-H460 cells after 48 hrs by sulforhodamine B assay2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID348405Inhibition of tubulin polymerization2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization.
AID1352871Antimitotic activity against Paracentrotus lividus embryo assessed as cleavage alteration measured at 2.5 hrs post fertilization by light microscopy2018European journal of medicinal chemistry, Feb-25, Volume: 146Regioselective synthesis of 3,4-diaryl-5-unsubstituted isoxazoles, analogues of natural cytostatic combretastatin A4.
AID1195288Induction of microtubule depolymerization in rat A10 cells after 18 hrs by indirect immunofluorescence assay2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID1317590Antiproliferative activity against human MCF10A cells measured after 72 hrs by MTT assay2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1234870Inhibition of calf brain tubulin polymerization after 20 mins by spectrophotometric analysis2015European journal of medicinal chemistry, Jul-15, Volume: 100Exploring the size adaptability of the B ring binding zone of the colchicine site of tubulin with para-nitrogen substituted isocombretastatins.
AID265441Cell cycle arrest in NCI-H460 cells by accumulation at S phase cell at 160 nM post 24 hrs treatment and 48 hrs recovery2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID1711847Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 50 nM measured after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 85.3 %)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID1263246Cytotoxicity against human K562 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1689087Toxicity in BALB/c nude mouse transfected with human HeLa cells assessed as body weight changes at 30 mg/kg/day, iv for 21 days2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1351660Inhibition of tubulin polymerization in human A431 cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID769836Induction of microtubule depolymerization in rat A10 cells after 18 hrs by indirect immunofluorescence assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.
AID1154744Growth inhibition of human HeLa cells overexpressing beta-3 after 96 hrs incubation by sulforhodamine B technique2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential.
AID1064378Growth inhibition of human DU145 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID691662Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as effect on ALT level at 50 mg/kg, ip qd after 21 days (Rvb = 28 +/- 0.4 IU/L)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1917030Cytotoxicity against human HeLa cells assessed as cell growth inhibition2022European journal of medicinal chemistry, Nov-05, Volume: 241Recent advances in combretastatin A-4 codrugs for cancer therapy.
AID1183720Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 20 nM by propidium iodide staining-based flow cytometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID1435072Cell cycle arrest in human HT29-D4 cells assessed as accumulation at S phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID569521Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs using propidium iodide staining by flow cytometry relative to control2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents.
AID1698824Antimitotic activity against sea urchin embryo assessed as embryo spinning measured 2.5 to 6 hrs post-fertilization observed after 15 min to 20 hrs of treatment by light microscopy analysis2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Computational modeling and target synthesis of monomethoxy-substituted o-diphenylisoxazoles with unexpectedly high antimitotic microtubule destabilizing activity.
AID1400378Antiproliferative activity against CYP1A1 deficient human MDA-MB-231 cells after 72 hrs by SRB assay2018Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
4-(3-Alkyl-2-oxoimidazolidin-1-yl)-N-phenylbenzenesulfonamides as new antimitotic prodrugs activated by cytochrome P450 1A1 in breast cancer cells.
AID1458820Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents.
AID265444Cell cycle arrest in NCI-H460 cells by accumulation at G2/M phase cell at 160 nM post 24 hrs treatment2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID1706481Inhibition of porcine brain tubulin polymerization measured for 20 mins by spectrometric assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Development of triazolothiadiazine derivatives as highly potent tubulin polymerization inhibitors: Structure-activity relationship, in vitro and in vivo study.
AID1288158Cell cycle arrest in human MCF7/MX cells assessed as accumulation at G2/M phase at 3 uM after 72 hrs by propidium iodide staining based flow cytometry (Rvb = 5.68%)2016European journal of medicinal chemistry, May-23, Volume: 114Synthesis and biological evaluation of quinoline analogues of flavones as potential anticancer agents and tubulin polymerization inhibitors.
AID1873750Induction of apoptosis in human HeLa cells assessed as late apoptotic cells at 10 nM incubated for 72 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 4.70%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID502745Growth inhibition of human RXF393 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID1773136Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1851424Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells at G1 phase at 10 uM by flow cytometry analysis (Rvb = 73.3%)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Synthesis and antitumor activity of a series of novel N-aryl-5-(2,2,2-trifluoroethoxy)-1,5-dihydro-2H-pyrrol-2-ones derivatives.
AID1070875Cytotoxicity against human HeLa cells after 72 hrs by MTS assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
The bat flower: a source of microtubule-destabilizing and -stabilizing compounds with synergistic antiproliferative actions.
AID317733Cytotoxicity against mock-infected human MT4 cells by MTT assay2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID404585Cytotoxicity against human A549 cells after 72 hrs by XTT method2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Diarylmethyloxime and hydrazone derivatives with 5-indolyl moieties as potent inhibitors of tubulin polymerization.
AID1405397Antimigratory activity against human SKOV3 cells assessed as number of migrated cells at 25 nM after 24 hrs by crystal violet staining based transwell migration assay (Rvb = 49.3 to 50.7 No_unit)2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID630733Inhibition of tubulin polymerization at 10 uM after 60 mins by spectrophotometry2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
1,1-Diarylalkenes as anticancer agents: dual inhibitors of tubulin polymerization and phosphodiesterase 4.
AID729788Inhibition of tubulin (unknown origin) assembly after 20 mins by turbidimetric analysis2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Identification of diaryl 5-amino-1,2,4-oxadiazoles as tubulin inhibitors: the special case of 3-(2-fluorophenyl)-5-(4-methoxyphenyl)amino-1,2,4-oxadiazole.
AID1068593Growth inhibition of human SKOV3 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID266931Antiproliferative activity against mouse L1210 cell line2006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-5-aryl thiophenes as a new class of potent antitubulin agents.
AID1778193Antiproliferative activity against human HEK293 cells assessed as cell growth inhibition after 48 hrs by MTT assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines.
AID1064408Growth inhibition of human SNB19 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1075758Displacement of [3H]colchine from tubulin (unknown origin) at 5 uM after 10 mins2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of 4-(N-cycloamino)phenylquinazolines as a novel class of tubulin-polymerization inhibitors targeting the colchicine site.
AID1595689Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.
AID84445In vitro cytotoxic activity against human HT-29 cell line of colorectal carcinoma2004Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents.
AID1875871Induction of microtubule fragmentation in human 518A2 cells assessed as appearance of area with transverse arcs at 25 nM measured after 24 hrs by immunofluorescence assay
AID1698823Antimitotic activity against sea urchin embryo assessed as cleavage arrest measured 2.5 to 6 hrs post-fertilization by light microscopy analysis2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Computational modeling and target synthesis of monomethoxy-substituted o-diphenylisoxazoles with unexpectedly high antimitotic microtubule destabilizing activity.
AID1119740Displacement of [3H]-Colchicine from tubulin (unknown origin) at 1 uM relative to control2012MedChemComm, Jun, Volume: 3, Issue:6
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
AID1288161Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 3 uM after 72 hrs by propidium iodide staining based flow cytometry (Rvb = 6.18%)2016European journal of medicinal chemistry, May-23, Volume: 114Synthesis and biological evaluation of quinoline analogues of flavones as potential anticancer agents and tubulin polymerization inhibitors.
AID1514443Inhibition of tubulin (unknown origin) polymerization at 10 uM relative to control
AID42665Ability to inhibit Tubulin polymerization in Bovine brain1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization.
AID1057120Chemical stability of the compound in PBS at pH 7.4 assessed as compound remaining after 4 hrs by HPLC analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID1336757Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 100 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 12.1%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID590609Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 1 uM after 48 hrs by flow cytometric analysis2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Design, synthesis, and biological evaluation of novel γ-carboline ketones as anticancer agents.
AID1196870Inhibition of tubulin (unknown origin) polymerization by fluorescence assay2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID717164Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
AID1851426Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells at S phase at 10 uM by flow cytometry analysis (Rvb = 21.32%)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Synthesis and antitumor activity of a series of novel N-aryl-5-(2,2,2-trifluoroethoxy)-1,5-dihydro-2H-pyrrol-2-ones derivatives.
AID1612614Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID658262Cytotoxicity against human K562 cells after 72 hrs using resazurin dye by microtiter plate fluorimeter analysis2012European journal of medicinal chemistry, Jun, Volume: 52Conformationnally restricted naphthalene derivatives type isocombretastatin A-4 and isoerianin analogues: synthesis, cytotoxicity and antitubulin activity.
AID1308555Cytotoxicity against human A2780/TAX cells assessed as growth inhibition after 48 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID607530Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 3 times IC50 value after 16 hrs using propidium iodide staining by FACS analysis2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues.
AID1234872Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation after 72 hrs by XTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Exploring the size adaptability of the B ring binding zone of the colchicine site of tubulin with para-nitrogen substituted isocombretastatins.
AID214170Concentration inhibiting [3H]colchicine binding to tubulin, at a concentration of 5 uM1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor agents. 196. Substituted 2-thienyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.
AID1403591Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
AID1324126Cytotoxicity against human IGROV1 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1424777Growth inhibition of human MCF7 cells after 96 hrs by trypan blue exclusion assay2018European journal of medicinal chemistry, May-25, Volume: 152New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors.
AID1689136Cytotoxicity against wild type human HCT-116 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.
AID1392070Antiproliferative activity against human MDA-MB-231 cells by SRB assay2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.
AID1196867Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 48 hrs by MTT assay2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID1324115Cytotoxicity against human SK-MEL-28 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID314016Antiproliferative activity against human 786-0 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID1737797Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID1651876Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 1 uM incubated for 10 mins by scintillation counting relative to control2020Journal of natural products, 04-24, Volume: 83, Issue:4
Bioreductively Activatable Prodrug Conjugates of Combretastatin A-1 and Combretastatin A-4 as Anticancer Agents Targeted toward Tumor-Associated Hypoxia.
AID1187062Antiproliferative activity against human HeLa cells after 24 to 48 hrs by CKK8 assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Discovery and molecular modeling of novel 1-indolyl acetate--5-nitroimidazole targeting tubulin polymerization as antiproliferative agents.
AID383961Cytotoxicity against human SNB75 cells2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
2-(6-aryl-3(Z)-hexen-1,5-diynyl)anilines as a new class of potent antitubulin agents.
AID1534525Antiproliferative activity against human K562 cells after 72 hrs by MTS assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation.
AID657907Inhibition of purified tubulin assembly after 20 mins2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID1689131Induction of microtubule cytoskeleton disruption in human EA.hy926 cells at 25 nM measured after 24 hrs by DAPI staining based fluorescence microscopic analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.
AID1700954Antiproliferation activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
AID1240947Displacement of [3H]-colchicine from tubulin (unknown origin) at 1 uM after 10 mins2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines as tubulin polymerization inhibitors.
AID273365Antiproliferative activity against human MKN45 cell line by methylene blue dye assay2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.
AID1698449Inhibition of tubulin polymerization in human A549 cells assessed as increase in soluble fraction of tubulin at 1 uM measured after 48 hrs by western blot analysis2020Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22
Ultrasound assisted synthesis of tetrazole based pyrazolines and isoxazolines as potent anticancer agents via inhibition of tubulin polymerization.
AID1608954Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.
AID1459293Binding affinity to colchicine-binding site of beta tubulin in human MCF7 cells assessed as inhibition of formation of protein-N,N'-Ethylene-bis(iodoacetamide) adduct at 10 uM after 2 hrs by Western blot method2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID106518In vitro cytotoxicity evaluated in mouse heart endotheliaoma cell (MHEC5-T) after incubation of the cells for 1 hr2003Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4.
AID1518077Induction of cell cycle arrest in human MDA-MB-468 cells assessed as accumulation of cells at G2/M phase at IC50 concentration by propidium iodide staining-based flow cytometric analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1689093Induction of cell cycle arrest in human HeLa cells assessed as accumulation at S phase at 0.5 uM measured after 24 hrs by propidium iodide/RNAse staining based flow cytometry (Rvb = 27.8%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1196881Metabolic stability in human liver microsomes assessed as peak area after 60 mins by LC-UV analysis in presence of NADPH and GSH2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
AID721878Cytotoxicity against human HCT116 assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID273277Antiproliferative activity against mouse FM3A cells2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.
AID1760491Cytotoxicity against African green monkey Vero cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020).
AID340148Growth inhibition of human MKN45 cells after 72 hrs by methylene blue dye assay2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.
AID1327861Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay
AID1890443Induction of apoptosis in human MDA-MB-231 cells assessed as viable cells at 10 uM incubated for 24 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 93.6 %)2022Bioorganic & medicinal chemistry, 04-15, Volume: 60Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones.
AID290178Antiproliferative activity against human DND1 cells2007Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
Novel pyridinyl and pyrimidinylcarbazole sulfonamides as antiproliferative agents.
AID1351633Induction of apoptosis in human SKOV3 cells assessed as increase in histone-associated DNA fragments in mononucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID152252Cytotoxic activity against P-388 cell line2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
A new family of quinoline and quinoxaline analogues of combretastatins.
AID317729Antiviral activity against HIV1RF infected in human CEM-SS cells2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID1338589Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of novel alkylsulfanyl-1,2,4-triazoles as cis-restricted combretastatin A-4 analogues.
AID1917312Cytotoxicity against mouse HT-22 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID1237707Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID1689085Antitumor activity against human HeLa cells xenografted in BALB/c mouse assessed as inhibition of tumor volume at 30 mg/kg/day, iv administered for 21 days by caliper analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1057193Inhibition of TERT mRNA expression in human HT-29 cells after 48 hrs by RT-PCR analysis relative to control2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity.
AID1709299Ratio of EC50 for induction of microtubule depolymerization in rat A10 cells to IC50 for antiproliferative activity against human MDA-MB-435 cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1711846Cell cycle arrest in human MCF7 cells assessed as accumulation at sub-G1 phase at 50 nM measured after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 2.4 %)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID1729879Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth after 72 hrs by XTT assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Methylsulfanylpyridine based diheteroaryl isocombretastatin analogs as potent anti-proliferative agents.
AID622507Cytotoxicity against human OVCAR3 cells after 48 hrs by sulforhodamine B assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID685196Growth inhibition of human MALME-3M cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID761828Inhibition of tubulin (unknown origin) polymerization after 20 mins2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity.
AID1387441Inhibition of bovine tubulin polymerization at 1 uM measured every 30 secs for 2 hrs by turbidity method2018Journal of natural products, 09-28, Volume: 81, Issue:9
Synthesis and in Vitro Bioactivity of Polyunsaturated Fatty Acid Conjugates of Combretastatin A-4.
AID214179Inhibition of radiolabeled colchicine binding to tubulin1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
AID492258Antiproliferative activity against mouse FM3A cells after 2 days by coulter counting2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Substituted 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]thiophene derivatives as potent tubulin polymerization inhibitors.
AID156162Concentration which produces 50% inhibition of growth of prostate tumor cell line PC-32001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Combretoxazolones: synthesis, cytotoxicity and antitumor activity.
AID1773144Cell cycle arrest in human A549 cells assessed as S phase at 500 nM measured after 24 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 14.78%)2021European journal of medicinal chemistry, Nov-15, Volume: 224Discovery of novel trimethoxyphenylbenzo[d]oxazoles as dual tubulin/PDE4 inhibitors capable of inducing apoptosis at G2/M phase arrest in glioma and lung cancer cells.
AID1183706Cytotoxicity against human MCF7 cells after 96 hrs by Giemsa staining-based light microscopy2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID449231Growth inhibition of HUVEC2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.
AID1760492Cytotoxicity against human L02 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020).
AID46122In vitro cytotoxic activity tested against human CNS (U251) cell line2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.
AID510857Inhibition of sheep brain tubulin microtubule assembly by turbidimetry assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Regioselective hydrostannation of diarylalkynes directed by a labile ortho bromine atom: an easy access to stereodefined triarylolefins, hybrids of combretastatin A-4 and isocombretastatin A-4.
AID293339Cell cycle arrest in HMEC1 cells assessed as accumulation at G1 phase at 25 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID228456Inhibition of tubulin (10 uM) polymerization, after a 20 min incubation at 30 degrees Centigrade2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
One-pot synthesis of benzo[b]furan and indole inhibitors of tubulin polymerization.
AID1064421Growth inhibition of human NCI-H23 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1736443Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID662348Antiproliferative activity in human MCF7 cells assessed as cell viability after 72 hrs by MTT assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID1195290Ratio of EC50 for microtubule depolymerization in rat A10 cells to IC50 for human MDA-MB-435 cells2015Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
AID605710Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4.
AID1593625Antiproliferative activity against TCCD-induced ER positive human MCF7 cells expressing CYP1A1 assessed as reduction in cell viability after 96 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells.
AID317730Antiviral activity against HIV13B infected in human MT4 cells2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID1906237Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 3 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 18.8%)
AID595053Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis, biological evaluation, and molecular docking studies of resveratrol derivatives possessing chalcone moiety as potential antitubulin agents.
AID1612610Antiproliferative activity against human K562 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1336754Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 50 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 12.1%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1906267Aqueous solubility of compound at pH 7.0 phosphate buffer incubated overnight by HPLC analysis analysis
AID622410Cytotoxicity against human A549 cells after 48 hrs by sulforhodamine B assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1064389Growth inhibition of human SKOV3 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1711839Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID277281Cytotoxicity against KB-3-1 cell line2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Highly potent triazole-based tubulin polymerization inhibitors.
AID1873749Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 10 nM incubated for 72 hrs by annexin V FITC and propidium iodide staining based flow cytometry analysis (Rvb = 2.36%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID546574Inhibition of bovine tubulin polymerization assessed as fold reduction Vmax of polymerization at 10 uM by spectrophotometry relative to untreated control2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Synthesis and evaluation of azetidinone analogues of combretastatin A-4 as tubulin targeting agents.
AID685168Cytotoxicity against human PC3 cells after 48 hrs assessed as inhibition of cell growth at 10 uM after 48 hrs by SRB assay relative to control2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID613264Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis and biological evaluation of 1-(4'-Indolyl and 6'-Quinolinyl) indoles as a new class of potent anticancer agents.
AID670884Antimitotic activity in human HeLa cells assessed as change in dipolar spindle formation in metaphase at 1 nM after 6 hrs by DAPI staining-based immunofluorescence analysis2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
AID474644Induction of microtubule network disruption in human HeLa cells at 0.02 uM after 24 hrs by immunofluorescence assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID145414Compound was evaluated against Human cell line ovarian OVCAR-31999Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
AID1555134Cytotoxicity against human SKOV3 cells assessed as growth inhibition measured after 48 hrs by SRB assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.
AID1647026Antitumor activity against mouse H22 cells expressing TDO xenografted in ICR mouse assessed as tumor growth inhibition at 30 mg/kg, iv administered once daily for 21 consecutive days and measured every 2 days for 21 days by electronic caliper method relat2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1600480Induction of cell cycle arrest in human CCRF-CEM cells assessed as accumulation at G0/G1 phase at 5 times antiproliferative IC50 incubated for 24 hrs by PI staining based flow cytometric analysis (Rvb = 40.89%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1327860Cytotoxicity against human SGC7901 cells assessed as reduction in cell viability after 24 hrs by MTT assay
AID437548Anticancer activity against human SW1990 cells after 72 hrs2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines).
AID642534Inhibition of bovine brain tubulin polymerization measured every 30 sec for 30 mins by turbidimetric assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. Part 2. The impact of bridging groups at position C-2.
AID384969Cell cycle arrest in human NCI-H460 cells assessed as G2/M phase accumulation after 24 hrs by flow cytometry2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
Synthesis and biological activity of fluorinated combretastatin analogues.
AID1153047Displacement of [3H]colchicine from bovine brain tubulin at 1 uM after 10 mins by liquid scintillation counting2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis, biological evaluation and molecular docking studies of trans-indole-3-acrylamide derivatives, a new class of tubulin polymerization inhibitors.
AID1730580Disruption of microtubule polymerization in human M21 cells at 10 nM measured after 24 hrs by DAPI staining based immunofluorescence microscopic analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID1778220Inhibition of tubulin polymerization (unknown origin) measured afer 30 mins every 1 min for 20 mins by spectrophotometric method2021European journal of medicinal chemistry, Aug-05, Volume: 220Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines.
AID515467Cytotoxicity against human cisplatin-resistant 1411HP cells after 96 hrs by SRB assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
4-(3-Halo/amino-4,5-dimethoxyphenyl)-5-aryloxazoles and -N-methylimidazoles that are cytotoxic against combretastatin A resistant tumor cells and vascular disrupting in a cisplatin resistant germ cell tumor model.
AID106520In vitro cytotoxicity evaluated in mouse heart endotheliaoma cell (MHEC5-T) after incubation of the cells for 5 days2003Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4.
AID616980Antiproliferative activity against human SKOV3 after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID717144Displacement of [3H]colchicine from tubulin in bovine brain at 5 uM DEAE-cellulose filter method2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Synthesis and biological evaluation of 2-substituted-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents.
AID1635336Relative ratio of IC50 for human HeLa cells expressing wild type beta3 tubulin to IC50 for human HeLa cells2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID1392074Antiproliferative activity against human SKOV3 cells by SRB assay2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.
AID662357Induction of apoptosis in human HuTu 80 cells assessed as caspase-3 cleavage at 30 nM after 16 hrs by Western blot analysis2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID1351658Inhibition of tubulin polymerization in human SKOV3 cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID8658Concentration which produces 50% inhibition of growth of human lung carcinoma cell line A5492001Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
Combretoxazolones: synthesis, cytotoxicity and antitumor activity.
AID494829Induction of apoptosis in human MCF7 cells assessed as decrease in PARP cleavage at 30 uM after 24 hrs by Western blot analysis2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
Synthesis and anti-cancer activity of chalcone linked imidazolones.
AID1165183Selectivity index, ratio of IC50 for HEK293 cells to IC50 for human MCF7 cells2014European journal of medicinal chemistry, Nov-24, Volume: 87Design and synthesis of pironetin analogue/combretastatin A-4 hybrids containing a 1,2,3-triazole ring and evaluation of their cytotoxic activity.
AID1736459Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 4 uM incubated for 2 hrs by scintillation counting method relative to control2020European journal of medicinal chemistry, Mar-15, Volume: 190Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site.
AID1308558Resistance index, ratio of IC50 for human HCT8/VCT cells to IC50 for human HCT8 cells2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo.
AID1742931Antiproliferative activity against human K562 cells assessed as inhibition of cell growth at 0.1 uM incubated for 72 hrs by MTT assay relative to control2020European journal of medicinal chemistry, Dec-01, Volume: 207Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors.
AID1336748Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1351638Induction of apoptosis in human MDA-MB-231 cells assessed as increase in histone-associated DNA fragments in oligonucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1862609Antiproliferative activity against human K562 cells after 72 hrs by CellTiter Glo assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.
AID642110Induction of mitotic arrest in human HeLa cells assessed as accumulation at G2/M phase at 2 to 20 nM after 24 hrs by flow cytometry analysis relative to control2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1700956Antiproliferation activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
AID1263283Cytotoxicity against human CAKI-1 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1409116Antiproliferative activity against human HeLa cells after 48 hrs by sulforhodamine B assay2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.
AID1600468Cytotoxicity against p53 deficient human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1711840Antiproliferative activity against human HOP-62 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID1689078Induction of apoptosis in human HeLa cells assessed as upregulation of Bax protein expression at 0.5 uM measured after 24 hrs by western blot analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1771519Induction of apoptosis in human MGC-803 cells assessed as late apoptotic cells at 2 nM measured after 48 hrs by Annexin V-APC/PI double staining based flow cytometry assay (Rvb = 3.62 %)2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID330406Inhibition of calf tubulin polymerization2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID452435Displacement of [3H]colchicine from tubulin assessed as bound colchicine at 0.05 to 10 mM incubated in dark for 2 hrs by scintillation spectroscopy2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: synthesis and biological evaluation of antivascular activity.
AID657911Antibacterial activity against Neisseria gonorrhoeae assessed per disc2012Journal of natural products, Mar-23, Volume: 75, Issue:3
Antineoplastic agents. 548. Synthesis of iodo- and diiodocombstatin phosphate prodrugs.
AID293344Cell cycle arrest in HMEC1 cells assessed as accumulation at G2/M phase at 25 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID214039Inhibition of bovine brain tubulin polymerization (ITP).1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Antitumor agents. 181. Synthesis and biological evaluation of 6,7,2',3',4'-substituted-1,2,3,4-tetrahydro-2-phenyl-4-quinolones as a new class of antimitotic antitumor agents.
AID355281Inhibition of collagen-induced platelet aggregation in human platelet-rich plasma1997Journal of natural products, Nov, Volume: 60, Issue:11
Isolation, synthesis, and antiplatelet aggregation activity of resveratrol 3-O-beta-D-glucopyranoside and related compounds.
AID771213Cytotoxicity against human BxPC3 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID1068623Growth inhibition of human NCI-H460 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID607294Displacement of [3H]colchicine from bovine brain tubulin at 5 uM2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID1406346Growth inhibition of human HepG2 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation.
AID1463416Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Constructing novel dihydrofuran and dihydroisoxazole analogues of isocombretastatin-4 as tubulin polymerization inhibitors through [3+2] reactions.
AID281361Metabolic stability in human liver microsomes after 60 mins2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID443467Cytotoxicity against human HeLa cells by MTT assay2009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
Synthesis and antitumor-evaluation of cyclopropyl-containing combretastatin analogs.
AID154379The compound was evaluated for its cytotoxic potency against P388 cell line2000Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22
Design, synthesis and cytotoxic activities of naphthyl analogues of combretastatin A-4.
AID1154741Inhibition of bovine brain tubulin assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometry2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential.
AID1757893Antiproliferative activity against human OVCAR-8 cells2021Bioorganic & medicinal chemistry letters, 06-01, Volume: 41Novel pyrazolo[4,3-d]pyrimidine microtubule targeting agents (MTAs): Synthesis, structure-activity relationship, in vitro and in vivo evaluation as antitumor agents.
AID1832133Induction of apoptosis in human HeLa cells assessed as necrotic cells at 5 nM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 0.4%)2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID502731Growth inhibition of human SK-MEL-2 cells after 48 hrs by SRB assay2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Synthesis and in vitro antitumor activity of new 4,5-dihydropyrazole derivatives.
AID90854Inhibitory concentration against human NPC cancer cell line using tetrazolium dye reduction assay (MTT)2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID642536Displacement of [3H]cholchicine from bovine brain tubulin at 5 uM after 2 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. Part 2. The impact of bridging groups at position C-2.
AID1189965Toxicity in C57BL/6 mouse assessed as interphase microtubule de-stabilizing activity by measuring influx of rhodamine in to spleen at 1 mg/kg, iv co-administered with rhodamine B by fluorimetry2015Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2
Synthesis and biological evaluation of furanoallocolchicinoids.
AID293348Cell cycle arrest in HMEC1 cells assessed as accumulation at S phase at 12.5 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID1427222Cytotoxicity against human OVK18 cells assessed as reduction in cell viability after 72 hrs by WST8 assay2017ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
Combretastatin A4-β-Galactosyl Conjugates for Ovarian Cancer Prodrug Monotherapy.
AID471946Growth inhibition of human SF268 cells after 48 hrs by sulforhodamine B assay2009Journal of natural products, Sep, Volume: 72, Issue:9
Antineoplastic agents. 579. Synthesis and cancer cell growth evaluation of E-stilstatin 3: a resveratrol structural modification.
AID1917304Antiproliferative activity against human NCI-H1437 cells measured after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.
AID636397Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Design, synthesis, biological evaluation and molecular modeling of 1,3,4-oxadiazoline analogs of combretastatin-A4 as novel antitubulin agents.
AID630732Inhibition of tubulin polymerization at 5 uM after 60 mins by spectrophotometry2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
1,1-Diarylalkenes as anticancer agents: dual inhibitors of tubulin polymerization and phosphodiesterase 4.
AID1161494Induction of mitotic arrest in human K562 cells assessed as mitotic indices at 100 uM by light microscopy2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Antiproliferative 4-(1,2,4-oxadiazol-5-yl)piperidine-1-carboxamides, a new tubulin inhibitor chemotype.
AID1420991Inhibition of bovine brain tubulin polymerization after 30 mins by UV-based assay
AID1057114Drug metabolism in PBS at pH 7.4 assessed as product-2 level after 4 hrs by HPLC analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID1779198Inhibition of tubulin polymerization (unknown origin) assessed as reduction in tubulin assembly preincubated for 15 mins followed by GTP addition by spectrophotometric method2021European journal of medicinal chemistry, Oct-05, Volume: 221Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia.
AID479719Antiproliferative activity against human K562 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
Synthesis and antitumor activity of 1,5-disubstituted 1,2,4-triazoles as cis-restricted combretastatin analogues.
AID1405394Antimigratory activity against human SKOV3 cells assessed as wound closure at 80 nM after 24 hrs by microscopy based scratch wound assay (Rvb = 79.5 +/- 2.8%)2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID642051Inhibition of tubulin polymerization after 15 mins preincubation measured after 20 mins by spectrophotometry2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID281347Cytotoxicity against human MiaPaCa2 cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1325842Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 2000 nM after 48 hrs by propidium iodide-staining based FACS analysis2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Scaffold-Hopping of Aurones: 2-Arylideneimidazo[1,2-
AID307422Inhibition of tubulin polymerization at 20 uM2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Synthesis and biological activity of naphthalene analogues of phenstatins: naphthylphenstatins.
AID1351589Cytotoxicity against human A431 cells after 48 hrs by MTT assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1353632Antiproliferative activity against human A549 cells after 2 days by MTT assay2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID363248Growth inhibition of human NCI-H460 after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Design, synthesis and biological evaluation of dihydronaphthalene and benzosuberene analogs of the combretastatins as inhibitors of tubulin polymerization in cancer chemotherapy.
AID1064427Growth inhibition of human RPMI8226 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1336750Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID93840Compound was tested for cell arrest at Go/G1 phase at 100 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID1070871Cytotoxicity against human SKOV3 cells expressing MDR1 after 72 hrs by MTS assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
The bat flower: a source of microtubule-destabilizing and -stabilizing compounds with synergistic antiproliferative actions.
AID317988Antiproliferative activity against mouse L1210 cells2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors.
AID751018Induction of microtubule depolymerization in human PC3 cells at 200 nM after 24 hrs by DAPI staining-based immunofluorescence microscopic analysis2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Dual-functional abeo-taxane derivatives destabilizing microtubule equilibrium and inhibiting NF-κB activation.
AID1686597Growth inhibition of human SK-OV-3 cells2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Potent Antitumor Activities and Structure Basis of the Chiral β-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin.
AID1570334Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by cell titer blue assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.
AID1647016Reduction in TDO protein expression in human HepG2 cells measured after 24 hrs by Western blot analysis2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1068600Growth inhibition of human UACC257 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID619866Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 100 nM after 48 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 60.22+/-3.1%)2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, biochemical and molecular modelling studies of antiproliferative azetidinones causing microtubule disruption and mitotic catastrophe.
AID730203Selectivity ratio of IC50 for quesicent HUVECs to IC50 for activated HUVECs2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Synthesis and structure-activity relationships of N-methyl-5,6,7-trimethoxylindoles as novel antimitotic and vascular disrupting agents.
AID1068611Growth inhibition of human SF539 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID622611Inhibition of bovine brain tubulin polymerization at 37 degC after 0.5 hrs by turbidimetry analysis2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID1600491Inhibition of porcine brain tubulin polymerization assessed as Vmax measured every 60 secs by turbidometric assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID765489Inhibition of tubulin assembly (unknown origin) preincubated for 15 mins followed by GTP addition measured after 20 mins by turbidimetric analysis2013European journal of medicinal chemistry, Sep, Volume: 67N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines: a novel class of antitumor agents targeting the colchicine site on tubulin.
AID1757285Resistant index, ratio of IC50 for VCR resistant human K562 cells to IC50 for human K562 cells2021European journal of medicinal chemistry, Apr-15, Volume: 216Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.
AID1263248Cytotoxicity against human RPMI8226 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1628240Antiproliferative activity against human HuH7 cells incubated for 24 hrs by sulforhodamine B assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID552582Induction of cell cycle arrest in human KB cells assessed as accumulation at S phase at 20 nM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 18.4%)2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis of antiproliferative flavones from calycopterin, major flavonoid of Calycopteris floribunda Lamk.
AID1324114Cytotoxicity against human SK-MEL-2 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID293336Inhibition of tubulin polymerization2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID1600478Induction of apoptosis in human CCRF-CEM cells assessed as accumulation at subG1 phase at 5 times antiproliferative IC50 incubated for 24 hrs by PI staining based flow cytometric analysis (Rvb = 3.71%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID642095Growth inhibition of HUVEC cells after 48 hrs by MTT assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID319823Cytotoxicity against human K562 cells2008Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
Synthesis and antitumor activity of benzils related to combretastatin A-4.
AID1608962Inhibition of bovine brain tubulin assembly using GTP as substrate incubated for 20 mins by spectrophotometric method2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.
AID1276117Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID761830Cytotoxicity against human PC3 cells after 48 hrs by sulforhodamine B assay2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity.
AID1157575Cytotoxicity against human OVCAR8 cells assessed as inhibition of cell proliferation by SRB assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.
AID1851618Induction of cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of cells at S phase at 10 uM (Rvb = 21.17 %)2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives.
AID569519Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 5 uM after 24 hrs using propidium iodide staining by flow cytometry relative to control2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents.
AID1405372Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID494825Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 30 uM after 24 hrs by FACS analysis2010Bioorganic & medicinal chemistry letters, Aug-15, Volume: 20, Issue:16
Synthesis and anti-cancer activity of chalcone linked imidazolones.
AID1119749Vascular disrupting activity in HUVEC assessed as disruption of capillary-like network of tubules at 0.01 to 1 uM after 2 hrs by matrigel assay2012MedChemComm, Jun, Volume: 3, Issue:6
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
AID1294470Growth inhibition of human NCI-H522 cells after 48 hrs by sulforhodamine B assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents.
AID761817Cytotoxicity against human H1299 cells assessed as growth inhibition after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Correlation of hydrogen-bonding propensity and anticancer profile of tetrazole-tethered combretastatin analogues.
AID1064386Growth inhibition of human CAKI-1 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1717480Cell cycle arrest in human HT-1080 cells assessed as accumulation at sub-G1 phase at 0.025 uM measured after 12 hrs by propidium iodide staining based flow cytometry (Rvb = 0.31%)
AID1126642Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorimetric analysis2014European journal of medicinal chemistry, May-06, Volume: 78Discovery of azaisoerianin derivatives as potential antitumors agents.
AID1324098Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID214014Inhibition of tubulin polymerization1994Journal of medicinal chemistry, Apr-15, Volume: 37, Issue:8
Antitumor agents. 150. 2',3',4',5',5,6,7-substituted 2-phenyl-4-quinolones and related compounds: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.
AID1717460Inhibition of porcine tubulin polymerization at 2 uM measured at 1 min interval for 90 mins by fluorescence assay
AID1550347Cell cycle arrest in human SGC7901 cells assessed as increase in cell population at G2/M phase at 2 fold IC50 concentration measured after 24 hrs by propidium iodide staining based FACScan flow cytometry2019European journal of medicinal chemistry, Jun-01, Volume: 171Synthesis and bioevaluation of diarylpyrazoles as antiproliferative agents.
AID376525Displacement of [3H]colchicine from bovine tubulin at inhibitor to colchicine ratio of 1:12000Journal of natural products, Jul, Volume: 63, Issue:7
Antineoplastic agents 440. Asymmetric synthesis and evaluation of the combretastatin A-1 SAR probes (1S,2S)- and (1R,2R)-1, 2-dihydroxy- 1-(2',3'-dihydroxy-4'-methoxyphenyl)-2-(3' ',4' ',5' '-trimethoxyphenyl)-ethane.
AID1906220Induction of cell cycle arrest in human HeLa cells assessed as >4N cells at 6 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis relative to control
AID595051Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis, biological evaluation, and molecular docking studies of resveratrol derivatives possessing chalcone moiety as potential antitubulin agents.
AID1778190Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines.
AID1400380Selectivity ratio of IC50 for human HaCaT cells to IC50 for CYP1A1 expressing human MCF7 cells2018Bioorganic & medicinal chemistry, 10-01, Volume: 26, Issue:18
4-(3-Alkyl-2-oxoimidazolidin-1-yl)-N-phenylbenzenesulfonamides as new antimitotic prodrugs activated by cytochrome P450 1A1 in breast cancer cells.
AID1068631Growth inhibition of human RPMI8226 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1126002Cytotoxicity against human A549 cells after 72 hrs by resazurin based fluorescence assay2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
AID1153046Displacement of [3H]colchicine from bovine brain tubulin at 5 uM after 10 mins by liquid scintillation counting2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis, biological evaluation and molecular docking studies of trans-indole-3-acrylamide derivatives, a new class of tubulin polymerization inhibitors.
AID261212Cell cycle arrest in A431 cells by accumulation at G2/M phase2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines.
AID214340Percent inhibitory activity (2 uM) against colchicine binding to tubulin in mitosis in MCF-7 breast cancer cells2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Antineoplastic agents. 487. Synthesis and biological evaluation of the antineoplastic agent 3,4-methylenedioxy-5,4'-dimethoxy-3'-amino-Z-stilbene and derived amino acid amides.
AID1408368Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1593624Antiproliferative activity against ER positive human MCF7 cells expressing low level of CYP assessed as reduction in cell viability measured after 96 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells.
AID1324092Cytotoxicity against human SR cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1422791Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay
AID214690Inhibitory concentration required against MAP-rich tubulin polymerization2004Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents.
AID299207Antiproliferative activity against human PC3 cells2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity relationships.
AID1518327Disruption of microtubule network in human HCT116 cells assessed as microtubule condensation at 50 nM incubated for 18 hrs by FITC/DAPI staining-based confocal microscopic analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.
AID1865671Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay2021RSC medicinal chemistry, Aug-18, Volume: 12, Issue:8
Design, synthesis and biological evaluation of combretastatin A-4 sulfamate derivatives as potential anti-cancer agents.
AID1317592Cell cycle arrest in human HepG2 cells assessed as accumulation in G2/M phase at growth inhibitory IC50 measured after 8 hrs by propidium iodide-staining based FACS analysis (Rvb = 28%)2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID314004Antiproliferative activity against human MOLT4 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID729940Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and biochemical activities of antiproliferative amino acid and phosphate derivatives of microtubule-disrupting β-lactam combretastatins.
AID1263281Cytotoxicity against human A498 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1809274Antiproliferative activity against human MCF-10A cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
AID1906230Induction of apoptosis in human HeLa cells assessed as viable cells at 1.5 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 75.5%)
AID1233621Displacement of [3H]colchicine from bovine brain tubulin at 5 uM2015European journal of medicinal chemistry, Jun-24, Volume: 99Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin polymerization inhibitors.
AID1310190Growth inhibition of primary chicken fibroblasts after 48 hrs by MTT assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1411797Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay2018MedChemComm, Feb-01, Volume: 9, Issue:2
Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.
AID1600484Induction of cell cycle arrest in human CCRF-CEM cells assessed as accumulation at G2/M phase at 5 times antiproliferative IC50 incubated for 24 hrs by PI staining based flow cytometric analysis (Rvb = 12.12%)2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1403615Induction of apoptosis in human HeLa cells assessed as necrotic cells at 100 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.9%)2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents.
AID643527Cytotoxicity against human A549 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Synthesis and evaluation of 1,5-disubstituted tetrazoles as rigid analogues of combretastatin A-4 with potent antiproliferative and antitumor activity.
AID1689076Induction of intracellular reactive oxygen species generation in human HeLa cells at 0.5 uM measured after 24 hrs by DCFH-DA staining based flow cytometry (Rvb = 6.47%)2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID78625Concentration required to inhibit proliferation of multidrug resistant Human colon carcinoma HCT-15 cell line2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.
AID1351623Induction of apoptosis in human MCF7 cells after 24 hrs by FITC Annexin V/propidium iodide staining-based FACScan flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1351612Inhibition of tubulin polymerization in human MDA-MB-231 cells assessed as micronuclei formation at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1647045Toxicity in immunocompetent BALB/c nude mouse xenografted with human A549 cells assessed as effect on lung damage or inflammation at 30 mg/kg, iv administered once daily for 29 consecutive days measured after 29 days by hematoxylin-eosin staining based fl2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1411611Substrate activity at human OCT1 expressed in HEK293 cells assessed as compound uptake by HPLC-UV method2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID1508482Cytotoxicity in human HL60 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, antiproliferative, anti-tubulin activity, and docking study of new 1,2,4-triazoles as potential combretastatin analogues.
AID1906196Induction of cell cycle arrest in human HeLa cells assessed as < 2N cells at 6 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 9.32%)
AID1600470Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay2019Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19
Synthesis and biological evaluation of cis-restrained carbocyclic combretastatin A-4 analogs: Influence of the ring size and saturation on cytotoxic properties.
AID1586011Inhibition of pig brain tubulin polymerization at 10 uM by spectrophotometric analysis relative to control
AID1183705Inhibition of tubulin (unknown origin) polymerization incubated 15 mins prior to GTP addition by spectrophotometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID642530Growth inhibition of human MKN45 cells after 72 hrs by methylene blue assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. Part 2. The impact of bridging groups at position C-2.
AID552575Induction of cell cycle arrest in human KB cells assessed as accumulation at G2/M phase at 20 nM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 19.6%)2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis of antiproliferative flavones from calycopterin, major flavonoid of Calycopteris floribunda Lamk.
AID342518Ratio of IC50 of drug to IC50 of colchicine for calf brain tubulin polymerization2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Synthesis and biological evaluation of new disubstituted analogues of 6-methoxy-3-(3',4',5'-trimethoxybenzoyl)-1H-indole (BPR0L075), as potential antivascular agents.
AID1351615Inhibition of tubulin polymerization in human HaCaT cells assessed as micronuclei formation at 1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1851622Induction of apoptosis in human MDA-MB-231 cells assessed as dead cells at 10 uM by Annexin V-FITC/propidium iodide staining based flow cytometric analysis (Rvb = 0.68 %)2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Design, synthesis, and antitumor study of a series of novel 1-Oxa-4-azaspironenone derivatives.
AID1353630Antiproliferative activity against human MCF7 cells after 2 days by MTT assay2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID1647030Toxicity in ICR mouse xenografted with mouse H22 cells assessed as effect on liver damage or inflammation at 30 mg/kg, iv administered once daily for 21 consecutive days measured after 21 days by hematoxylin-eosin staining based fluorescence microscopy2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1183654Growth inhibition of human Jurkat cells after 72 hrs by MTT assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID658920Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G0/G1 phase at 10 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 43.9 %)2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
AID1278674Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.
AID642113Induction apoptosis in human HeLa cells at 20 nM after 24 hrs by Annexin V-based flow cytometry analysis2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID657577Inhibition of bovine tubulin polymerization after 20 mins by spectrophotometry2012Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10
Design, synthesis and biological evaluation of novel chalcone derivatives as antitubulin agents.
AID1586360Antiproliferative activity against human HeLa cells by MTT assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4.
AID1285318Cytotoxicity against human DU145 cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.
AID1738832Inhibition of bovine brain tubulin polymerisation preincubated with compound followed by GTP addition and measured after 20 mins by turbidimetry based spectrophotometric method2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors.
AID1064392Growth inhibition of human OVCAR4 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1351628Induction of apoptosis in human A431 cells assessed as increase in histone-associated DNA fragments in mononucleosomes at 0.1 uM after 24 hrs by ELISA2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1518322Disruption of microtubule network in human SW620 cells assessed as microtubule condensation at 50 nM incubated for 18 hrs by FITC/DAPI staining-based confocal microscopic analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.
AID474634Cell cycle arrest in human HeLa cells assessed as accumulation of cells in G0/1 phase at 2.2 uM after 24 hrs using propidium iodide by flow cytometry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1288163Antiproliferative activity against human MCF7/MX cells assessed as cell viability after 48 hrs by MTT assay2016European journal of medicinal chemistry, May-23, Volume: 114Synthesis and biological evaluation of quinoline analogues of flavones as potential anticancer agents and tubulin polymerization inhibitors.
AID1402690Inhibition of microtubules in human HeLa cells assessed as induction of disorganized spindle fibers formation at 5 uM after 24 hrs by DAPI staining-based confocal microscopic analysis
AID1693356Inhibition of bovine tubulin polymerization assessed as reduction in extent of assembly preincubated for 15 mins followed by addition of reaction mixture measured after 20 mins by turbidimetric assay2021Bioorganic & medicinal chemistry, 01-01, Volume: 29The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
AID751511Resistance ratio of IC50 for human SKOV3 cells expressing MDR1 to IC50 for human SKOV3 cells2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.
AID1518073Inhibition of pig brain tubulin polymerization in presence of GTP by spectrophotometric analysis2019European journal of medicinal chemistry, Dec-15, Volume: 184Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.
AID1689101Toxicity in BALB/c nude mouse transfected with human HeLa cells assessed as lung damage at 30 mg/kg/day, iv for 21 days by H&E staining based immunohistochemistry2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1064377Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID93848Compound was tested for cell arrest at sub-G1 phase at 50 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID1164801Antiproliferative activity against human KB cells after 72 hrs by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Synthesis and biological evaluation of novel 3,4-diaryl-1,2,5-selenadiazol analogues of combretastatin A-4.
AID1263244Cytotoxicity against human CCRF-CEM cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID771214Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay2013European journal of medicinal chemistry, Oct, Volume: 68Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.
AID669466Cell cycle arrest in human SKOV3 cells assessed as accumulation at sub-G1 phase at 5 nM by FACS analysis2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID1263285Cytotoxicity against human MCF7 cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID46877Inhibitory concentration against camptothecin (CPT) resistant cell line using tetrazolium dye reduction assay (MTT)2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID1324122Cytotoxicity against human OVCAR5 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID669458Growth inhibition of human SKOV3 cells after 48 hrs by SRB assay2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
AID607527Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues.
AID93847Compound was tested for cell arrest at sub-G1 phase at 25 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID1732760Induction of cell death in human RL cells assessed as cell gating level at 1 to 10 nM measured upto 48 hrs by PI staining based flow cytometry analysis (Rvb = 80 to 85 %)2021European journal of medicinal chemistry, Apr-05, Volume: 215Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies.
AID314021Antiproliferative activity against human DU145 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID1200587Stability assessed as cis-trans isomerization equilibrium by mesuring remaining compound level at 1.5 x 10'-2 M exposed to UV-visible light irradiation after 1.5 hrs by LC-HRMS method2015Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5
Quantum chemistry calculation-aided structural optimization of combretastatin A-4-like tubulin polymerization inhibitors: improved stability and biological activity.
AID280072Antiproliferative activity against drug sensitive Messa cell line by Alamar Blue assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
AID314009Antiproliferative activity against human HCT116 cells2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Design, synthesis, and in vitro antitumor activity of new 1,4-diarylimidazole-2-ones and their 2-thione analogues.
AID1183715Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID685375Inhibition of tubulin polymerization after 30 mins to 1 hr by spectrophotometry2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1508151Induction of intrinsic apoptosis in human MCF7 cells assessed as effect on mitochondrial membrane depolarization at 2 uM after 5 hrs by DiOC6 staining-based FACS analysis relative to control2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1832145Metabolic stability in human liver microsomes assessed as parent compound remaining after 30 mins2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID214001Inhibition of glutamate-dependent tubulin polymerization at 30 degrees C(0.25 mM MgCl2)1992Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6
Synthesis of alkoxy-substituted diaryl compounds and correlation of ring separation with inhibition of tubulin polymerization: differential enhancement of inhibitory effects under suboptimal polymerization reaction conditions.
AID1317624Antiangiogenic activity against human EAhy926 assessed as inhibition of capillary tube formation at 0.11 uM after 72 hrs by matrigel assay2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID1730566Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 48 hrs by sulforhodamine B assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID452434Inhibition of tubulin assembly by Woods method2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: synthesis and biological evaluation of antivascular activity.
AID685202Growth inhibition of human UACC257 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID767272Inhibition of [3H] radiolabelled colchicine binding to tubulin beta (unknown origin) at 1 uM by DEAE-cellulose filter method2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Exploring natural product chemistry and biology with multicomponent reactions. 5. Discovery of a novel tubulin-targeting scaffold derived from the rigidin family of marine alkaloids.
AID1612616Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1693360Inhibition of beta3 Tubulin (unknown origin) expressed in human HeLa cell line assessed as inhibition of cell proliferation measured after 48 hrs by SRB method2021Bioorganic & medicinal chemistry, 01-01, Volume: 29The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.
AID310088Inhibition of tubulin polymerization at 3 uM2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Conformationally restricted macrocyclic analogues of combretastatins.
AID1906263Antiproliferative activity against human SiHa/DDP cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
AID1628401Growth inhibition of human MCF7 cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Design, Synthesis, and Biological Evaluation of 1-Methyl-1,4-dihydroindeno[1,2-c]pyrazole Analogues as Potential Anticancer Agents Targeting Tubulin Colchicine Binding Site.
AID1832143Metabolic stability in human liver microsomes assessed as parent compound remaining measured immediately after compound addition2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID1612622Drug resistance index, ratio of IC50 for taxol-resistant human A549/TR cells to IC50 for human A549 cells2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID128971Vascular shutdown expressed as vessel density decrease in percent of the control at the dose of 100 mg/kg2003Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4.
AID1612618Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site.
AID1055626Cytotoxicity against human NCI-H460 cells after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Synthesis of structurally diverse benzosuberene analogues and their biological evaluation as anti-cancer agents.
AID1057127Cytotoxicity against human MCF7 cells after 3 days2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design and synthesis of silicon-containing tubulin polymerization inhibitors: replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
AID1731992Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214Novel diaryl-2H-azirines: Antitumor hybrids for dual-targeting tubulin and DNA.
AID1240941Antiproliferative activity against human A549 cells assessed as cell growth inhibition by SRB assay2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Optimization of N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines as tubulin polymerization inhibitors.
AID420602Inhibition of tubulin polymerization2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Design and synthesis of 2-(3-benzo[b]thienyl)-6,7-methylenedioxyquinolin-4-one analogues as potent antitumor agents that inhibit tubulin assembly.
AID1832108Antiproliferative activity against human MCF7 assessed as reduction in cell viability measured after 48 hrs by MTT assay2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID642052Growth inhibition of human MCF7 cells after 96 hrs2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1711838Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID1336752Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 50 nM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 78.5%)2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1887830Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR.
AID1351661Inhibition of tubulin polymerization in human HeLa cells assessed as perturbation in cytoskeleton structure at 1 uM after 24 hrs by Hoechst 33258/FITC staining-based flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID246826Effective dose against murine P388 leukemia cell line2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41.
AID1185192Inhibition of bovine brain tubulin assessed as rate of assembly preincubated for 15 mins by turbidimetry2014European journal of medicinal chemistry, Sep-12, Volume: 84Novel 9'-substituted-noscapines: synthesis with Suzuki cross-coupling, structure elucidation and biological evaluation.
AID1555138Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 5 uM measured after 10 mins by beckman scintillation counting method relative to control2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.
AID691735Toxicity in ICR mouse assessed as body weight loss at 50 mg/kg, ip administered on day 1 measured for 10 days relative to vehicle-treated control2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1338079Antiproliferative activity against human HeLa cells measured after 48 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Design, synthesis, and biological evaluation of cyclic-indole derivatives as anti-tumor agents via the inhibition of tubulin polymerization.
AID1191395Cytotoxicity against human H1299 cells after 72 hrs by CellTitre-Blue assay2015European journal of medicinal chemistry, Jan-27, Volume: 90Rapid synthesis of 4-arylchromenes from ortho-substituted alkynols: A versatile access to restricted isocombretastatin A-4 analogues as antitumor agents.
AID341687Displacement of [3H]colchicine from tubulin at 50 uM2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Asymmetric synthesis of 2,3-dihydro-2-arylquinazolin-4-ones: methodology and application to a potent fluorescent tubulin inhibitor with anticancer activity.
AID1689138Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.
AID1732758Induction of cell cycle arrest in human RL cells assessed as increase in accumulation in subG0/G1 phase at 10 nM incubated for 48 hrs by PI staining based flow cytometry analysis (Rvb = 8 %)2021European journal of medicinal chemistry, Apr-05, Volume: 215Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies.
AID1310189Growth inhibition of p53 null human HCT116 cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID412968Inhibition of tubulin polymerization after 30 mins2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Synthesis and structure-activity relationships of 2-amino-1-aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents.
AID442981Vascular disrupting activity in HUVEC assessed as appearance of blebbing morphology of rounded cells at 0.1 uM after 1 hr by FITC-onjugated DAPI staining-based immunofluorescence assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Vascular disrupting activity of tubulin-binding 1,5-diaryl-1H-imidazoles.
AID1646997Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID384966Cytotoxic activity against human HT29 cells after 72 hrs by sulforhodamine B test2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
Synthesis and biological activity of fluorinated combretastatin analogues.
AID629595Antiproliferative activity against mouse FM3A cells after 2 days by coulter counter analysis2011European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
AID1628238Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by sulforhodamine B assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID442970Cytotoxicity against HUVEC after 1 hr by crystal violet staining2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Vascular disrupting activity of tubulin-binding 1,5-diaryl-1H-imidazoles.
AID444162Antiproliferative activity against human SKOV3 cells expressing adenoviral MDR1 after 48 hrs by SRB assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Design, synthesis, and biological evaluations of 2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoline analogs of combretastatin-A4.
AID1700957Cytotoxicity against human L02 cells assessed as assessed as cell growth inhibition measured after 72 hrs by MTT assay
AID685198Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1737794Antiproliferative activity against human Huh-7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID1854153Cytotoxicity against human A2780 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Cascade synthetic strategies opening access to medicinal-relevant aliphatic 3- and 4-membered N-heterocyclic scaffolds.
AID1906249Induction of apoptosis in human HeLa cells assessed as necrotic cells at 3 nM measured after 24 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis (Rvb = 0.45%)
AID1324125Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings.
AID1327134Antiproliferative activity against human SGC7901 cells measured after 72 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 1224,5-Diaryl-3H-1,2-dithiole-3-thiones and related compounds as combretastatin A-4/oltipraz hybrids: Synthesis, molecular modelling and evaluation as antiproliferative agents and inhibitors of tubulin.
AID214367In vitro tubulin polymerization-inhibitory activity.1998Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15
Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug resistant cells.
AID758697Increase in mitotic index in human CA46 cells at 100 uM by light microscopic analysis (Rvb = 3%)2013European journal of medicinal chemistry, Jul, Volume: 652-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action.
AID442972Growth inhibition of human HCT15 cells after 3 days by crystal violet staining2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Vascular disrupting activity of tubulin-binding 1,5-diaryl-1H-imidazoles.
AID685163Cytotoxicity against human COLO205 cells after 48 hrs assessed as inhibition of cell growth at 10 uM after 48 hrs by SRB assay relative to control2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID452617Inhibition of tubulin assembly by spectrophotometry2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID607284Antiproliferative activity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Convergent synthesis and biological evaluation of 2-amino-4-(3',4',5'-trimethoxyphenyl)-5-aryl thiazoles as microtubule targeting agents.
AID1506491Cytotoxicity against human A375 cells after 48 hrs by MTT assay2017MedChemComm, Jan-01, Volume: 8, Issue:1
Design, synthesis, anticancer activity and docking studies of theophylline containing 1,2,3-triazoles with variant amide derivatives.
AID1706477Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth after 48 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Development of triazolothiadiazine derivatives as highly potent tubulin polymerization inhibitors: Structure-activity relationship, in vitro and in vivo study.
AID55793Cell growth inhibition of prostate DU-145 cells, expressed as 50% reduction in the net protein increase2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Antineoplastic agents. 465. Structural modification of resveratrol: sodium resverastatin phosphate.
AID1657525Cytotoxicity against HEK293 cells after 68 hrs by MTT assay2020Journal of natural products, 05-22, Volume: 83, Issue:5
Synthesis and Cytotoxicity Studies of Stilbene Long-Chain Fatty Acid Conjugates.
AID1351626Induction of apoptosis in human SKOV3 cells after 24 hrs by FITC Annexin V/propidium iodide staining-based FACScan flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID622417Cytotoxicity against human SF295 cells after 48 hrs by sulforhodamine B assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Synthesis and biological evaluation of phenstatin metabolites.
AID281504Displacement of [3H]colchine from tubulin at 5 uM2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Arylthioindoles, potent inhibitors of tubulin polymerization.
AID1771501Induction of cell cycle arrest in human MGC-803 cells assessed as accumulation at S phase at 2 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb =31.51 %)2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1237708Displacement of [3H]-colchicine from tubulin (unknown origin) at 5 uM after 10 mins relative to control2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID616976Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID691641Toxicity in nude BALB/c mouse xenografted with human HT-29 cells assessed as body weight change at 30 mg/kg, ip qd after 21 days (Rvb = 2.7 g)2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Synthesis and biological evaluation of 1-benzylidene-3,4-dihydronaphthalen-2-one as a new class of microtubule-targeting agents.
AID1729299Antiproliferative activity against human A549/PTX cells assessed as reduction in cell viability measured after 48 hrs by CCK8 assay
AID310756Antiproliferative activity against human MCF7 cells2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
3-(2'-Bromopropionylamino)-benzamides as novel S-phase arrest agents.
AID1064403Growth inhibition of human LOXIMVI cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1730139Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 5 uM by DEAE-cellulose filter method relative to control2021European journal of medicinal chemistry, Feb-15, Volume: 212Insight on [1,3]thiazolo[4,5-e]isoindoles as tubulin polymerization inhibitors.
AID1732754Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Apr-05, Volume: 215Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies.
AID1352872Antimitotic activity against Paracentrotus lividus embryo assessed as cleavage arrest measured at 5.5 hrs post fertilization by light microscopy2018European journal of medicinal chemistry, Feb-25, Volume: 146Regioselective synthesis of 3,4-diaryl-5-unsubstituted isoxazoles, analogues of natural cytostatic combretastatin A4.
AID1399373Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by sulforhodamine B assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and preclinical evaluation of 5-methyl-N
AID1570325Cytotoxicity against human HeLa cells harboring Dengue virus serotype 2 NS2B-NS3 protease assessed as reduction in cell viability after 72 hrs by cell titer blue assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.
AID93845Compound was tested for cell arrest at S phase at 50 nM concentration in KB human cancer cells2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity and crystallographic analysis of benzophenone derivatives-the potential anticancer agents.
AID1647054Inhibition of tubulin polymerization in human HepG2 cells assessed as depolymerization of interphase microtubule by measuring disorderly dispersed microtubules in cytoplasm at 0.05 uM measured after 24 hrs by DAPI staining based laser scanning confocal mi2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1064397Growth inhibition of human UACC62 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID461785Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue dye assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors.
AID616972Antiproliferative activity against human HAAE1 grown in absence of growth factors after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID1310239Antivascular activity in human EAhy926 cells assessed as change in cell morphology from stretched to rounded form at 100 nM after 16 hrs by matrigel based tube formation assay2016European journal of medicinal chemistry, Aug-08, Volume: 118Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.
AID1711864Induction of mitochondrial membrane potential loss in human MCF7 cells assessed as cell population with intact mitochondrial membrane potential at 50 nM measured after 48 hrs by JC-1 staining based flow cytometry (Rvb = 1 %)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID265412Antiproliferative activity against human MeWo cells2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID9207The compound was evaluated for its cytotoxic potency against A-549 cell line2000Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22
Design, synthesis and cytotoxic activities of naphthyl analogues of combretastatin A-4.
AID1205542Cytotoxicity against mouse BNL 1ME A.7R.1 cells2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin.
AID306513Cell cycle arrest in human M21 cells assessed as accumulation at G1 phase at 0.050 uM after 24 hrs2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
AID1906194Induction of cell cycle arrest in human HeLa cells assessed as < 2N cells at 1.5 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 9.32%)
AID442544Cytotoxicity against human HeLa cells after 72 hrs by XTT assay2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Exploring the effect of 2,3,4-trimethoxy-phenyl moiety as a component of indolephenstatins.
AID1351622Induction of apoptosis in human HaCaT cells after 24 hrs by FITC Annexin V/propidium iodide staining-based FACScan flow cytometric analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID451275Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Synthesis and biological evaluation of 3,4-diaryl-5-aminoisoxazole derivatives.
AID1068589Growth inhibition of human RXF393 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1336762Inhibition of alpha-tubulin polymerization in human A549 cells assessed as increase in soluble tubulin fraction at 1 uM after 48 hrs by Western blot method2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers.
AID1327862Cytotoxicity against human HT1080 cells assessed as reduction in cell viability after 24 hrs by MTT assay
AID1689139Induction of F-actin cytoskeleton disruption in human EA.hy926 cells at 50 nM assessed as formation of actin stress fibers measured after 3 hrs by DAPI staining based fluorescence microscopic analysis2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones.
AID674211Antiproliferative activity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Discovery and optimization of a series of 2-aryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazoles as novel anticancer agents.
AID383960Cytotoxicity against human HCT15 cells2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
2-(6-aryl-3(Z)-hexen-1,5-diynyl)anilines as a new class of potent antitubulin agents.
AID721880Cytotoxicity against human HT-29 cells assessed as growth inhibition after 48 hrs by MTT assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID751574Induction of interphase microtubule depolymerization in rat A10 cells after 18 to 24 hrs by indirect immunofluorescence assay2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.
AID92128Cytotoxic effect in human tumor cell lines, tested by the National Cancer Institute1997Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
Antitumor agents. 174. 2',3',4',5,6,7-Substituted 2-phenyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.
AID1508160Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells at 2 uM after 24 hrs by Annexin-V FITC/propidium iodide staining-based FACS analysis (Rvb = 5.4%)2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel pyrazolochalcones as potential modulators of PI3K/Akt/mTOR pathway and inducers of apoptosis in breast cancer cells.
AID1875856Hydrolytic stability of compound in DMSO-d6/D2O measured after 7 days by 1H-NMR analysis
AID1068602Growth inhibition of human SK-MEL-28 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1703289Inhibition of pig brain tubulin polymerization measured by light scattering based spectrophotometer method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities.
AID1635314Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID1351588Cell cycle arrest in human MCF7 cells assessed as accumulation of cells at G2/M phase at 0.1 to 1 uM after 24 hrs by propidium iodide staining-based FACS analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1906258Antimigratory activity against human HeLa cells at 1.5 nM measured after 24 hrs by scratch wound healing based fluorescence inverted microscopic analysis
AID1068586Growth inhibition of human SN12C cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1437254Inhibition of porcine tubulin assembly measured for 30 mins by UV/visible spectrophotometric method2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Tubulin-binding dibenz[c,e]oxepines: Part 2. Structural variation and biological evaluation as tumour vasculature disrupting agents.
AID383962Cytotoxicity against human UACC62 cells2008Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
2-(6-aryl-3(Z)-hexen-1,5-diynyl)anilines as a new class of potent antitubulin agents.
AID1647057Induction of apoptotic cell death in human HepG2 cells assessed as increase in orange fluorescence at 0.1 uM measured after 24 hrs by acridine orange/ethidium bromide staining based fluorescence microscopy2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1237723Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 48 hrs by SRB assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer.
AID1635270Inhibition of tubulin assembly in bovine brain homogenate assessed as reduction in turbidity increase preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric analysis2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID269716Cell cycle arrest in SHSY5Y cells by accumulation at G1 phase after 12 hrs2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
AID1411606Drug uptake in mock transfected HEK293 cells by HPLC-UV assay2017MedChemComm, Jul-01, Volume: 8, Issue:7
Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles
AID662345Antiproliferative activity in human SW480 cells assessed as cell viability after 72 hrs by MTT assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Synthesis and biological evaluation of 1,4-diaryl-2-azetidinones as specific anticancer agents: activation of adenosine monophosphate activated protein kinase and induction of apoptosis.
AID1405367Antiproliferative activity against human SKOV3 cells after 72 hrs by CCK8 assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Design, synthesis and biological evaluation of a novel tubulin inhibitor 7a3 targeting the colchicine binding site.
AID1706478Cytotoxicity against HEK293 cells assessed as reduction in cell growth after 48 hrs by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208Development of triazolothiadiazine derivatives as highly potent tubulin polymerization inhibitors: Structure-activity relationship, in vitro and in vivo study.
AID721873Cytotoxicity against human MESSA/DX5 cells assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
AID1183656Growth inhibition of human SEM cells after 72 hrs by MTT assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis, antimitotic and antivascular activity of 1-(3',4',5'-trimethoxybenzoyl)-3-arylamino-5-amino-1,2,4-triazoles.
AID1729302Inhibition of pig brain tubulin polymerization by spectrophotometric method
AID1729878Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by XTT assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Methylsulfanylpyridine based diheteroaryl isocombretastatin analogs as potent anti-proliferative agents.
AID1851425Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells at G2 phase at 10 uM by flow cytometry analysis (Rvb = 5.38%)2022Bioorganic & medicinal chemistry letters, 10-01, Volume: 73Synthesis and antitumor activity of a series of novel N-aryl-5-(2,2,2-trifluoroethoxy)-1,5-dihydro-2H-pyrrol-2-ones derivatives.
AID1408398Antivascular activity against HUVEC assessed as reduction in wound closure after 24 hrs by phase contrast microscopic method2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities.
AID1689089Toxicity in BALB/c nude mouse transfected with human HeLa cells assessed as liver damage at 30 mg/kg/day, iv for 21 days by H&E staining based immunohistochemistry2020European journal of medicinal chemistry, Mar-01, Volume: 189Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase.
AID1424778Inhibition of [3H]colchicine binding to tubulin (unknown origin) at 5 uM after 10 mins relative to control2018European journal of medicinal chemistry, May-25, Volume: 152New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors.
AID1570333Cytotoxicity against human HuH7 cells assessed as reduction in cell viability measured after 72 hrs by cell titer blue assay2019ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.
AID1179506Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
Synthesis, biological evaluation and molecular modeling of 1,3,4-thiadiazol-2-amide derivatives as novel antitubulin agents.
AID450673Cytotoxicity against human HL60 cells after 72 hrs by XTT assay2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Isocombretastatins A: 1,1-diarylethenes as potent inhibitors of tubulin polymerization and cytotoxic compounds.
AID1730575Cell cycle arrest in human M21 cells assessed as accumulation at S phase at 11 nM measured after 24 hrs by DAPI staining based flow cytometry (Rvb = 16.1%)2021European journal of medicinal chemistry, Mar-05, Volume: 213Phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonates and phenyl 4-(2-oxopyrrolidin-1-yl)benzenesulfonamides as new antimicrotubule agents targeting the colchicine-binding site.
AID666752Cytotoxicity against mouse B16 cells assessed as cell viability after 48 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54In vitro and in vivo biological evaluation of new 4,5-disubstituted 1,2,3-triazoles as cis-constrained analogs of combretastatin A4.
AID1068615Growth inhibition of human SW620 cells after 48 hrs by sulforhodamine B assay2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID1317626Cell cycle arrest in human HepG2 cells assessed as decrease in S phase at growth inhibitory IC50 measured after 24 hrs by propidium iodide-staining based FACS analysis2016European journal of medicinal chemistry, Sep-14, Volume: 120Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity.
AID310760Antiproliferative activity against human DND1 cells2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
3-(2'-Bromopropionylamino)-benzamides as novel S-phase arrest agents.
AID450672Inhibition of calf brain tubulin polymerization after 20 mins by turbidimetric method2009Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17
Isocombretastatins A: 1,1-diarylethenes as potent inhibitors of tubulin polymerization and cytotoxic compounds.
AID1847782Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 12-15, Volume: 52From natural products to HDAC inhibitors: An overview of drug discovery and design strategy.
AID626631Antitumor activity against human HT1080 cells xenografted in chicken chorioallantoic membrane assessed as inhibition of tumor growth at 1 to 3 ug, iv measured on day 17 by CAM assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships.
AID751510Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by SRB assay2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.
AID265411Antiproliferative activity against human HCT116 cells2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Novel combretastatin analogues endowed with antitumor activity.
AID1353633Antiproliferative activity against human HL60 cells after 2 days by MTT assay2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID1392076Resistance index, ratio of IC50 for human SKOV3-MDR1-M6/6 cells to IC50 for human SKOV3 cells2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.
AID474629Cytotoxicity against human MIAPaCa2 cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
AID1738826Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors.
AID1064398Growth inhibition of human SK-MEL-5 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1906325Inhibition of calf brain tubulin polymerization upto 50 uM measured after 40 mins by spectrophotometric analysis
AID1737817Aqueous solubility of the compound in phosphate buffer at pH 7.4 measured after 10 mins by HPLC analysis2020European journal of medicinal chemistry, Jul-01, Volume: 197Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy.
AID330412Cytotoxicity against human DU145 cells after 48 hrs by SRB assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Combretastatin dinitrogen-substituted stilbene analogues as tubulin-binding and vascular-disrupting agents.
AID611190Induction of apoptosis in human MCF7 cells assessed as double-strand DNA breaks at 2 uM after 24 hrs measured as phosphorylation at ser-139 on H2AX protein by immunostaining relative to control2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Synthesis and biological evaluation of 4β-acrylamidopodophyllotoxin congeners as DNA damaging agents.
AID1263282Cytotoxicity against human ACHN cells by SRB assay2015MedChemComm, May-01, Volume: 6, Issue:3
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin.
AID1518329Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Dec-15, Volume: 184Discovery of 3-(((9H-purin-6-yl)amino)methyl)-4,6-dimethylpyridin-2(1H)-one derivatives as novel tubulin polymerization inhibitors for treatment of cancer.
AID1064400Growth inhibition of human SK-MEL-28 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1711858Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells at 50 nM measured after 48 hrs by annexinV-FITC/propidium iodide staining based flow cytometry (Rvb = 95 %)2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis and biological evaluation of arylcinnamide linked combretastatin-A4 hybrids as tubulin polymerization inhibitors and apoptosis inducing agents.
AID404190Inhibition of bovine brain tubulin polymerization for 20 mins2008Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10
Design, synthesis, and biological evaluation of thiophene analogues of chalcones.
AID1064394Growth inhibition of human OVCAR3 cells after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2
Synthesis and antiproliferative activity of conformationally restricted 1,2,3-triazole analogues of combretastatins in the sea urchin embryo model and against human cancer cell lines.
AID1351602Cell cycle arrest in human A431 cells assessed as accumulation of cells at G2/M phase at 0.1 to 1 uM after 24 hrs by propidium iodide staining-based FACS analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents.
AID1353634Antiproliferative activity against HMEC1 cells after 2 days by MTT assay2018European journal of medicinal chemistry, Mar-10, Volume: 147Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.
AID293338Cell cycle arrest in HMEC1 cells assessed as accumulation at G1 phase at 12.5 nM after 24 hrs by flow cytometry assay relative to control2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
AID281353Enhanced mitotic arrest in human ECV304 cells assessed as accumulation at G2/M phase at 1 uM after 24 hrs relative to control2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.
AID1647008Induction of mitochondrial membrane potential disruption in human HepG2 cells assessed as increase in green-emitting fluorescence at 0.1 uM measured after 24 hrs by JC1 staining based fluorescence microscopy2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1635271Displacement of [3H]colchicine from tubulin in bovine brain homogenate at 1 uM incubated for 10 mins by DEAE-cellulose filter assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.
AID659051Induction of microtubule depolymerization in HUVEC after 30 mins by DAPI staining method2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
AID1508551Inhibition of beta tubulin polymerisation in human HepG2 cells incubated for 2 hrs using TMB substrate by ELISA relative to untreated control2017European journal of medicinal chemistry, Dec-01, Volume: 141Synthesis, antiproliferative, anti-tubulin activity, and docking study of new 1,2,4-triazoles as potential combretastatin analogues.
AID1068640Antimitotic activity in sea urchin fertilized egg assessed as cleavage alteration treated at 8 to 20 mins post-fertilization measured at 2.5 to 5.5 hrs post-fertilization2014European journal of medicinal chemistry, Feb-12, Volume: 733-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
AID685193Growth inhibition of human SNB75 cells after 48 hrs by SRB assay2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1125811Displacement of [3H]colchicine from tubulin (unknown origin) at 5 uM after 2 hrs by scintillation counting analysis2014European journal of medicinal chemistry, Apr-22, Volume: 77Antimitotic and vascular disrupting agents: 2-hydroxy-3,4,5-trimethoxybenzophenones.
AID1731561Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents.
AID106314The compound was evaluated for its cytotoxic potency against MEL-28 cell line2000Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22
Design, synthesis and cytotoxic activities of naphthyl analogues of combretastatin A-4.
AID1832131Induction of apoptosis in human HeLa cells assessed as early apoptotic cells at 5 nM incubated for 48 hrs by Annexin V and propidium iodide Staining based assay (Rvb = 0.2%)2021European journal of medicinal chemistry, Nov-05, Volume: 223Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
AID1498596Displacement of [3H]colchicine from tubulin (unknown origin) at 5 uM after 10 mins relative to control2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
The inhibitory effect of kokusaginine on the growth of human breast cancer cells and MDR-resistant cells is mediated by the inhibition of tubulin assembly.
AID1873772Induction of mitochondrial membrane potential alteration in human HeLa cells assessed as viable cells at 10 nM measured after 48 hrs by JC1 staining-based flow cytometry analysis (Rvb = 90.9%)2022European journal of medicinal chemistry, Aug-05, Volume: 238Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent.
AID355284Inhibition of adenosine diphosphate-induced platelet aggregation in human platelet-rich plasma1997Journal of natural products, Nov, Volume: 60, Issue:11
Isolation, synthesis, and antiplatelet aggregation activity of resveratrol 3-O-beta-D-glucopyranoside and related compounds.
AID1731563Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay2021European journal of medicinal chemistry, Mar-15, Volume: 214A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents.
AID1187063Antiproliferative activity against human U251 cells after 24 to 48 hrs by CKK8 assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Discovery and molecular modeling of novel 1-indolyl acetate--5-nitroimidazole targeting tubulin polymerization as antiproliferative agents.
AID1462295Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
Synthesis of different heterocycles-linked chalcone conjugates as cytotoxic agents and tubulin polymerization inhibitors.
AID674212Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Discovery and optimization of a series of 2-aryl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazoles as novel anticancer agents.
AID607525Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues.
AID552574Induction of cell cycle arrest in human KB cells assessed as accumulation at S phase at 20 nM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb = 6.9%)2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis of antiproliferative flavones from calycopterin, major flavonoid of Calycopteris floribunda Lamk.
AID670887Antimitotic activity in human HeLa cells assessed as disruption of interphase microtubule network at 10 nM after 6 hrs by DAPI staining-based immunofluorescence analysis2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
AID1771457Antiproliferative activity against human MGC-803 cells assessed as cell growth inhibition after 72 hrs by SRB assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
AID1191394Inhibition of sheep brain tubulin polymerization by DAPI staining-based fluorescence assay2015European journal of medicinal chemistry, Jan-27, Volume: 90Rapid synthesis of 4-arylchromenes from ortho-substituted alkynols: A versatile access to restricted isocombretastatin A-4 analogues as antitumor agents.
AID1906200Induction of cell cycle arrest in human HeLa cells assessed as 2N cells at 1.5 nM measured after 24 hrs by propidium iodide staining based flow cytometric analysis analysis ( Rvb = 41.7%)
AID1628253Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 5 nM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 16%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Novel Combretastatin-2-aminoimidazole Analogues as Potent Tubulin Assembly Inhibitors: Exploration of Unique Pharmacophoric Impact of Bridging Skeleton and Aryl Moiety.
AID442969Vascular disrupting activity in HUVEC assessed as change in cell morphology with detachment form substrate after 1 hr by crystal violet staining-based inverted light microscopy2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Vascular disrupting activity of tubulin-binding 1,5-diaryl-1H-imidazoles.
AID590529Inhibition of tubulin polymerization in human MCF7 cells by fluorometric analysis2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Design, synthesis, and biological evaluation of novel γ-carboline ketones as anticancer agents.
AID1435064Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 03-01, Volume: 25, Issue:5
Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.
AID616968Antiproliferative activity against HUVEC grown in presence of growth factors after 48 hrs by spectrophotometry2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
AID452620Antiproliferative activity against human A549 cells after 5 days by MTT assay2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
AID1183707Displacement of [3H]colchicine from tubulin (unknown origin) at 5 uM after 10 mins2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
AID642111Induction apoptosis in human HeLa cells at 100 nM after 24 hrs by Annexin V-based flow cytometry analysis2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.
AID1608955Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.
AID1646999Cell cycle arrest in human HepG2 cells assessed as accumulation at G2 phase at 0.1 uM measured after 24 hrs by RNase A/propidium iodide staining based flow cytometry (Rvb = 16.23 %)2020European journal of medicinal chemistry, Feb-01, Volume: 187Microtubule inhibitors containing immunostimulatory agents promote cancer immunochemotherapy by inhibiting tubulin polymerization and tryptophan-2,3-dioxygenase.
AID1728936Induction of apoptosis in human MDA-MB-231 cells assessed as early apoptotic cells at 1 uM measured after 24 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.49%)2021European journal of medicinal chemistry, Mar-05, Volume: 213Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.
AID1422797Inhibition of porcine brain tubulin polymerization after 30 mins by spectrophotometric method
AID512064Cytotoxicity against human HL60 cells after 72 hrs by MTT assay2010Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17
Identification of CKD-516: a potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
AID685166Cytotoxicity against human MCF7 cells after 48 hrs assessed as inhibition of cell growth at 10 uM after 48 hrs by SRB assay relative to control2012European journal of medicinal chemistry, Oct, Volume: 56Synthesis and biological evaluation of combretastatin-amidobenzothiazole conjugates as potential anticancer agents.
AID1799503Tubulin Polymerization from Article 10.1016/j.chembiol.2005.06.016: \\Structure-based discovery of a boronic acid bioisostere of combretastatin A-4.\\2005Chemistry & biology, Sep, Volume: 12, Issue:9
Structure-based discovery of a boronic acid bioisostere of combretastatin A-4.
AID1799504Cell Proliferation Assay from Article 10.1016/j.chembiol.2005.06.016: \\Structure-based discovery of a boronic acid bioisostere of combretastatin A-4.\\2005Chemistry & biology, Sep, Volume: 12, Issue:9
Structure-based discovery of a boronic acid bioisostere of combretastatin A-4.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346187Human tubulin beta 3 class III (Tubulins)2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (962)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (0.31)18.7374
1990's42 (4.37)18.2507
2000's269 (27.96)29.6817
2010's507 (52.70)24.3611
2020's141 (14.66)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.66

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index20.66 (24.57)
Research Supply Index6.21 (2.92)
Research Growth Index5.23 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.66)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials21 (3.57%)5.53%
Trials0 (0.00%)5.53%
Reviews53 (9.01%)6.00%
Reviews8 (1.61%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other514 (87.41%)84.16%
Other489 (98.39%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (18)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase II, Dose Ranging, Multi-Center Study to Evaluate the Safety and Efficacy of Combretastatin A4 Phosphate for Treating Subfoveal Choroidal Neovascularization in Subjects With Pathologic Myopia [NCT01423149]Phase 223 participants (Actual)Interventional2005-03-31Completed
A Phase Ib and Randomised Phase II Trial of Pazopanib With or Without Fosbretabulin in Advanced Recurrent Ovarian Cancer [NCT02055690]Phase 1/Phase 221 participants (Actual)Interventional2014-09-30Terminated(stopped due to Safety)
A Randomized Open-Labeled Phase II Study of Combretastatin A-4 Phosphate in Combination With Paclitaxel and Carboplatin to Evaluate the Safety and Efficacy in Subjects With Advanced Imageable Malignancies [NCT00113438]Phase 213 participants (Actual)Interventional2005-03-31Completed
OXiGENE OXC402-201: A Phase 2, Randomized, Double-Masked, Placebo-Controlled Study of the Safety, Pharmacokinetics, and Biological Effects of Intravenous Fosbretabulin in Asian Subjects With Polypoidal Choroidal Vasculopathy (PCV) [NCT01023295]Phase 220 participants (Actual)Interventional2009-07-31Completed
A Phase II/III Study to Evaluate the Safety and Efficacy of Combretastatin A-4 Phosphate in Combination With Paclitaxel and Carboplatin in Comparison With Paclitaxel and Carboplatin Against Anaplastic Thyroid Carcinoma [FACT] [NCT00507429]Phase 2/Phase 380 participants (Actual)Interventional2007-08-31Terminated(stopped due to Low rate of subject accrual)
A Phase II Study to Assess the Safety and Efficacy of the Combination of Carboplatin, Paclitaxel, and Bevacizumab ± Combretastatin A4 Phosphate (CA4P) Followed by Bevacizumab ± CA4P in Subjects With Chemotherapy Naïve Stage IIIB/IV Non-Squamous Cell Histo [NCT00653939]Phase 263 participants (Actual)Interventional2008-03-31Completed
FOCUS: A Multicenter, Multinational, Double-Blind, 2-Arm, Randomized, Phase 2/3, Study of Physician's Choice Chemotherapy ([PCC] Weekly Paclitaxel or Pegylated Liposomal Doxorubicin [PLD]) Plus Bevacizumab and CA4P Versus PCC Plus Bevacizumab and Placebo [NCT02641639]Phase 2/Phase 391 participants (Actual)Interventional2016-06-30Terminated(stopped due to Interim analysis failed to show efficacy benefit)
A Phase I Pharmacokinetic Study of Single Dose Intravenous CA4P in Patients With Advanced Cancer [NCT00003768]Phase 125 participants (Actual)Interventional1998-09-30Completed
Phase II Trial of Combined Modality Combretastatin A-4 Phosphate (CA4P)-Based Therapy for Patients With Newly Diagnosed Anaplastic Thyroid Cancer [Induction Chemotherapy With Doxorubicin/Cisplatin; Combined Modality Therapy With CA4P and Radiation; Follow [NCT00077103]Phase 1/Phase 24 participants (Actual)Interventional2003-11-30Terminated(stopped due to slow accrual)
OXC4P1-105: A Phase I Study of the Safety, Tolerability, and Antitumor Activity of Escalating Doses of Combretastatin A4 Phosphate Given in Combination With Bevacizumab to Subjects With Advanced Solid Tumors [NCT00395434]Phase 120 participants (Anticipated)Interventional2006-09-30Completed
Phase II Trial Of Combretastatin A-4 Phosphate (CA4P) In Advanced Anaplastic Carcinoma Of The Thyroid [NCT00060242]Phase 226 participants (Actual)Interventional2003-02-28Completed
Rollover for Study OX4218s, A P2 Study to Investigate Safety and Activity of Fosbretabulin Tromethamine in the Treatment of Well-Differentiated, Low-to-Intermediate-Grade Unresectable, Recurrent or Metastatic PNET or GI-NET With Elevated Biomarkers [NCT02279602]Phase 27 participants (Actual)Interventional2014-12-31Completed
A Ph 2 Study to Investigate the Safety and Activity of Fosbretabulin Tromethamine (CA4P) in the Treatment of Well-Differentiated, Low-to-Intermediate-Grade Unresectable, Recurrent or Metastatic PNET or GI-NET Neuroendocrine Tumors/Carcinoid With Elevated [NCT02132468]Phase 218 participants (Actual)Interventional2014-09-30Completed
A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of Fosbretabulin Tromethamine (CA4P) in Combination With Paclitaxel and Carboplatin in Anaplastic Thyroid Carcinoma (FACT2) [NCT01701349]Phase 30 participants (Actual)Interventional2015-03-31Withdrawn(stopped due to Expected inability to recruit study participants in a reasonable amount of time.)
A Phase 1 Study of Fosbretabulin in Combination With Everolimus in Neuroendocrine Tumors (Grades 1-3) That Have Progressed After at Least One Prior Regimen for Metastatic Disease [NCT03014297]Phase 117 participants (Actual)Interventional2017-03-06Terminated(stopped due to Part I completed. Part 2 will not be done due to sponsor decision.)
A Randomized Phase II Evaluation of Single-Agent Bevacizumab (NSC #704865) and Combination Bevacizumab With Fosbretabulin Tromethamine (CA4P) (NSC #752293) in the Treatment of Recurrent or Persistent Epithelial Ovarian, Fallopian Tube or Primary Peritonea [NCT01305213]Phase 2107 participants (Actual)Interventional2011-03-21Completed
An Open Label, Pilot (Phase I/II), Dose-Escalation Safety and Tolerability Study of Combretastatin A4 Phosphate in Patients With Neovascular Age-Related Macular Degeneration. [NCT01570790]Phase 1/Phase 28 participants (Actual)Interventional2003-05-31Completed
A Phase I Trial of Combretastatin A4 Phosphate in Patients With Solid Tumours Given by Weekly Intravenous Infusion [NCT00003698]Phase 135 participants (Anticipated)Interventional1998-07-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00507429 (2) [back to overview]Overall Survival
NCT00507429 (2) [back to overview]To Determine Percentage of 1 Year Survival
NCT00653939 (6) [back to overview]Overall Survival (OS) Using a Multivariate Cox Regression Model in the Intent-to-Treat Population
NCT00653939 (6) [back to overview]Progression Free Survival (PFS) in the Intent-to-Treat Population
NCT00653939 (6) [back to overview]Best Overall Tumor Response Rate (RR) in the Intent-to-Treat Population
NCT00653939 (6) [back to overview]Chemistry NCI-CTCAE Toxicity Grade of 3 or 4 (Safety Population)
NCT00653939 (6) [back to overview]Coagulation NCI-CTCAE Grade 3 or 4 (Safety Population)
NCT00653939 (6) [back to overview]Hematology NCI-CTCAE Grade 3 or 4 (Safety Population)
NCT01305213 (6) [back to overview]Measurable Disease by Response Evaluation Criteria in Solid Tumors (RECIST) Criteria and Progression Free Survival (PFS)
NCT01305213 (6) [back to overview]Overall Survival (OS)
NCT01305213 (6) [back to overview]Progression-free Survival (PFS)
NCT01305213 (6) [back to overview]Response by CA-125
NCT01305213 (6) [back to overview]Tumor Response
NCT01305213 (6) [back to overview]Incidence of Adverse Events (Grade 3 or Higher) as Assessed by Common Terminology Criteria for Adverse Events (CTCAE) v 4.0

Overall Survival

(NCT00507429)
Timeframe: From randomization to date last known alive

Interventionmonths (Median)
Arm 1, Active: CA4P + Carboplatin + Paclitaxel5.2
Arm 2, Comparator: Carboplatin + Paclitaxel4.0

[back to top]

To Determine Percentage of 1 Year Survival

(NCT00507429)
Timeframe: from randomization through end of study visit

Interventionpercentage of participants (Number)
Arm 1, Active: CA4P + Carboplatin + Paclitaxel26
Arm 2, Control: Carboplatin + Paclitaxel9

[back to top]

Overall Survival (OS) Using a Multivariate Cox Regression Model in the Intent-to-Treat Population

(NCT00653939)
Timeframe: Until death or lost to follow-up, up to 12 months since randomization

InterventionMonths (Median)
Arm 1: Chemotherapy+Bevacizumab16.2
Arm 2: Active Comparator+Fosbretabulin13.6

[back to top]

Progression Free Survival (PFS) in the Intent-to-Treat Population

Progression was defined using Response Evaluation Criteria in Solid Tumors (RECIST) Version 1.0. Based on 20% increase of the longest diameter of target lesions or appearance of one or more new non-target lesions or/and progression of non-target lesions since the treatment started. (NCT00653939)
Timeframe: Six 21-day cycles

Interventionmonths (Median)
Arm 1: Chemotherapy+Bevacizumab9.3
Arm 2: Active Comparator+Fosbretabulin8.6

[back to top]

Best Overall Tumor Response Rate (RR) in the Intent-to-Treat Population

Based on Response Evaluation Criteria in Solid Tumors (RECIST) Version 1.0 for target lesions (assessed by MRI or CT scan): Complete Response (CR) is defined as the disappearance of all target lesions, Partial Response (PR) is defined as at least a 30% decrease in the sum of the longest diameter of target lesions, Progressive Disease is defined as at least 20% increase in the sum of the longest diameter of target lesions, Stable Disease (SD) is defined as neither shrinkage to qualify for a PR or increase to qualify for a PD. (NCT00653939)
Timeframe: Six 21-day cycles

,
Interventionparticipants (Number)
Complete ResponsePartial ResponseStable DiseaseProgressive DiseaseUnknown
Arm 1: Chemotherapy+Bevacizumab0111334
Arm 2: Active Comparator+Fosbretabulin018815

[back to top]

Chemistry NCI-CTCAE Toxicity Grade of 3 or 4 (Safety Population)

(NCT00653939)
Timeframe: Days 1 (pretreatment) per 21-day Cycle (6 Cycles)

,
Interventionparticipants (Number)
ALT - Grade 3ALT - Grade 4AST - Grade 3AST - Grade 4ALP - Grade 3ALP - Grade 4Total Bilirubin - Grade 3Total Bilirubin - Grade 4Glucose - Grade 3Glucose - Grade 4Creatinine - Grade 3Creatinine - Grade 4Calcium - Grade 3Calcium - Grade 4Magnesium - Grade 3Magnesium - Grade 4Phosphorus - Grade 3Phosphorus - Grade 4Potassium - Grade 3Potassium - Grade 4Sodium - Grade 3Sodium - Grade 4
Arm 1: Chemotherapy+Bevacizumab1000000001013122005150
Arm 2: Active Comparator+Fosbretabulin1010000000010111100020

[back to top]

Coagulation NCI-CTCAE Grade 3 or 4 (Safety Population)

(NCT00653939)
Timeframe: Day 1 (pretreatment) per 21-day Cycle (6 Cycles)

,
Interventionparticipants (Number)
INR - Grade 3INR - Grade 4PTT - Grade 3PTT - Grade 4
Arm 1: Chemotherapy+Bevacizumab2030
Arm 2: Active Comparator+Fosbretabulin3050

[back to top]

Hematology NCI-CTCAE Grade 3 or 4 (Safety Population)

(NCT00653939)
Timeframe: Days 1 (pretreatment), 7, 14, and 21 per 21-day Cycle (6 Cycles)

,
Interventionparticipants (Number)
Hemoglobin - Grade 3Hemoglobin - Grade 4White Blood Cell - Grade 3White Blood Cell - Grade 4Absolute Neutrophils - Grade 3Absolute Neutrophils - Grade 4Platelets - Grade 3Platelets - Grade 4
Arm 1: Chemotherapy+Bevacizumab7414242036
Arm 2: Active Comparator+Fosbretabulin0112152053

[back to top]

Measurable Disease by Response Evaluation Criteria in Solid Tumors (RECIST) Criteria and Progression Free Survival (PFS)

Differences between measurable versus non-measurable disease status on PFS and OS will be examined with plots of survival curves, estimates of quartiles and hazard ratios. (NCT01305213)
Timeframe: Up to 5 years

Interventionmonths (Median)
Non Measurable Disease Patients3.99
Measurable Disease Patients6.80

[back to top]

Overall Survival (OS)

Differences between measurable versus non-measurable disease status on PFS and OS will be examined with plots of survival curves, estimates of quartiles and hazard ratios. (NCT01305213)
Timeframe: Up to 5 years

Interventionmonths (Median)
Non Measurble Disease22.0
Measurable Disease Patients21.2

[back to top]

Progression-free Survival (PFS)

The time from randomization until disease progression, death, or date of last contact. Endpoints are progression or death. Patients who are not observed with an endpoint are censored. (NCT01305213)
Timeframe: For those patients whose disease can be evaluated by physical examination, progression was assessed prior to each 21 day cycle. CT scan or MRI if used to follow lesion for measurable disease every other cycle, up to 5 years

Interventionmonths (Median)
Arm I Bevacizumab4.83
Arm II Bevacizumab + Fosbretabulin7.23

[back to top]

Response by CA-125

The effects of treatment on the proportion responding by CA125 will be examined. (NCT01305213)
Timeframe: Up to 5 years

InterventionPercentage of Participants (Number)
Arm I Bevacizumab23.7
Arm II Bevacizumab + Fosbretabulin33.3

[back to top]

Tumor Response

Complete and Partial Tumor Response by RECIST 1.0 (NCT01305213)
Timeframe: for those patients whose disease can be evaluated by physical examination, response wa assessed prior to each 21 day cycle. CT scan or MRI if used to follow lesion for measurable disease every other cycle, up to 5 years

Interventionpercentage of participants (Number)
Arm I Bevacizumab28.2
Arm II Bevacizumab + Fosbretabulin35.7

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Incidence of Adverse Events (Grade 3 or Higher) as Assessed by Common Terminology Criteria for Adverse Events (CTCAE) v 4.0

Toxicities will be characterized by their frequency and severity. Differences in the level of toxicities by treatment regimen will be assessed by classifying them as severe or not severe and examining the relative proportion of severe toxicities. (NCT01305213)
Timeframe: Up to 5 years

,
InterventionParticipants (Count of Participants)
ThrombocytopeniaNeutropeniaOther InvestigationsOther Blood/LymphaticsCardiacNauseaVomitingOther GastrointestinalGeneral and Administration SiteInfections/InfestationsMetabolism/NutritionMusculoskeletal/Connective tissueNeoplasms Benign/MalignantPeripheral sensory NeuropathyNervous systemRenal/UrinaryRespiratory/Thoracic/MediastinalVascular Disorders
Arm I Bevacizumab0310120523821010210
Arm II Bevacizumab + Fosbretabulin11411328331120122119

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SubstanceRelationship StrengthStudiesTrialsClassesRoles
adenine
[no description available]		2.1106-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
carbamates
[no description available]		2.1710amino-acid anion
methane
Methane: The simplest saturated hydrocarbon. It is a colorless, flammable gas, slightly soluble in water. It is one of the chief constituents of natural gas and is formed in the decomposition of organic matter. (Grant & Hackh's Chemical Dictionary, 5th ed). methane : A one-carbon compound in which the carbon is attached by single bonds to four hydrogen atoms. It is a colourless, odourless, non-toxic but flammable gas (b.p. -161degreeC).		2.8330alkane;
gas molecular entity;
mononuclear parent hydride;
one-carbon compound		bacterial metabolite;
fossil fuel;
greenhouse gas
coumarin
2H-chromen-2-one: coumarin derivative		2.0310coumarinsfluorescent dye;
human metabolite;
plant metabolite
guaiacol
Guaiacol: An agent thought to have disinfectant properties and used as an expectorant. (From Martindale, The Extra Pharmacopoeia, 30th ed, p747). methylcatechol : Any member of the class of catechols carrying one or more methyl substituents.. guaiacol : A monomethoxybenzene that consists of phenol with a methoxy substituent at the ortho position.		2.9740guaiacolsdisinfectant;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
expectorant;
plant metabolite
lactic acid
Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group.		2.54202-hydroxy monocarboxylic acidalgal metabolite;
Daphnia magna metabolite
glycolic acid
glycolic acid: RN given refers to parent cpd. glycolic acid : A 2-hydroxy monocarboxylic acid that is acetic acid where the methyl group has been hydroxylated.		2.41102-hydroxy monocarboxylic acid;
primary alcohol		keratolytic drug;
metabolite
hydrogen
Hydrogen: The first chemical element in the periodic table with atomic symbol H, and atomic number 1. Protium (atomic weight 1) is by far the most common hydrogen isotope. Hydrogen also exists as the stable isotope DEUTERIUM (atomic weight 2) and the radioactive isotope TRITIUM (atomic weight 3). Hydrogen forms into a diatomic molecule at room temperature and appears as a highly flammable colorless and odorless gas.. dihydrogen : An elemental molecule consisting of two hydrogens joined by a single bond.		2.0510elemental hydrogen;
elemental molecule;
gas molecular entity		antioxidant;
electron donor;
food packaging gas;
fuel;
human metabolite
imidazole
imidazole: RN given refers to parent cpd. 1H-imidazole : An imidazole tautomer which has the migrating hydrogen at position 1.		2.4620imidazole
indole
[no description available]		3.6120indole;
polycyclic heteroarene		Escherichia coli metabolite
thioctic acid
Thioctic Acid: An octanoic acid bridged with two sulfurs so that it is sometimes also called a pentanoic acid in some naming schemes. It is biosynthesized by cleavage of LINOLEIC ACID and is a coenzyme of oxoglutarate dehydrogenase (KETOGLUTARATE DEHYDROGENASE COMPLEX). It is used in DIETARY SUPPLEMENTS.		2.2110dithiolanes;
heterocyclic fatty acid;
thia fatty acid		fundamental metabolite;
geroprotector
naphthalene
[no description available]		210naphthalenes;
ortho-fused bicyclic arene		apoptosis inhibitor;
carcinogenic agent;
environmental contaminant;
mouse metabolite;
plant metabolite;
volatile oil component
nickel
Nickel: A trace element with the atomic symbol Ni, atomic number 28, and atomic weight 58.69. It is a cofactor of the enzyme UREASE.. nickel ion : A nickel atom having a net electric charge.. nickel atom : Chemical element (nickel group element atom) with atomic number 28.		2.1110metal allergen;
nickel group element atom		epitope;
micronutrient
niacin
Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group.		2.1710pyridine alkaloid;
pyridinemonocarboxylic acid;
vitamin B3		antidote;
antilipemic drug;
EC 3.5.1.19 (nicotinamidase) inhibitor;
Escherichia coli metabolite;
human urinary metabolite;
metabolite;
mouse metabolite;
plant metabolite;
vasodilator agent
pyrazole
1H-pyrazole : The 1H-tautomer of pyrazole.		2.1310pyrazole
pyruvic acid
Pyruvic Acid: An intermediate compound in the metabolism of carbohydrates, proteins, and fats. In thiamine deficiency, its oxidation is retarded and it accumulates in the tissues, especially in nervous structures. (From Stedman, 26th ed). pyruvic acid : A 2-oxo monocarboxylic acid that is the 2-keto derivative of propionic acid. It is a metabolite obtained during glycolysis.		2.05102-oxo monocarboxylic acidcofactor;
fundamental metabolite
uric acid
Uric Acid: An oxidation product, via XANTHINE OXIDASE, of oxypurines such as XANTHINE and HYPOXANTHINE. It is the final oxidation product of purine catabolism in humans and primates, whereas in most other mammals URATE OXIDASE further oxidizes it to ALLANTOIN.. uric acid : An oxopurine that is the final oxidation product of purine metabolism.. 6-hydroxy-1H-purine-2,8(7H,9H)-dione : A tautomer of uric acid having oxo groups at C-2 and C-8 and a hydroxy group at C-6.. 7,9-dihydro-1H-purine-2,6,8(3H)-trione : An oxopurine in which the purine ring is substituted by oxo groups at positions 2, 6, and 8.		2.0710uric acidEscherichia coli metabolite;
human metabolite;
mouse metabolite
urea
pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.		2.7830isourea;
monocarboxylic acid amide;
one-carbon compound		Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
azobenzene
azobenzene: photosensor molecule known to undergo reversible isomerization from trans to cis on illumination with photons of appropriate wavelength; RN given refers to cpd without isomeric designation; structure. (E)-azobenzene : The (E)-isomer of azobenzene.. (Z)-azobenzene : The (Z)-isomer of azobenzene.. azobenzene : A molecule whose structure comprises two phenyl rings linked by a N=N double bond; the parent compound of the azobenzene class of compounds.		3.3510azobenzenes
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		2.1510aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
ellipticine
ellipticine : A organic heterotetracyclic compound that is pyrido[4,3-b]carbazole carrying two methyl substituents at positions 5 and 11.		3.5110indole alkaloid;
organic heterotetracyclic compound;
organonitrogen heterocyclic compound;
polycyclic heteroarene		antineoplastic agent;
plant metabolite
ethylenediamine
ethylenediamine: RN given refers to parent cpd; edamine is the recommended contraction for the ethylenediamine radical. ethylenediamine : An alkane-alpha,omega-diamine in which the alkane is ethane.		2.1110alkane-alpha,omega-diamineGABA agonist
flucytosine
Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections.		210aminopyrimidine;
nucleoside analogue;
organofluorine compound;
pyrimidine antifungal drug;
pyrimidone		prodrug
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		4.1140nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
glutaral
Glutaral: One of the protein CROSS-LINKING REAGENTS that is used as a disinfectant for sterilization of heat-sensitive equipment and as a laboratory reagent, especially as a fixative.. glutaraldehyde : A dialdehyde comprised of pentane with aldehyde functions at C-1 and C-5.		2.1310dialdehydecross-linking reagent;
disinfectant;
fixative
hypericin
[no description available]		2.0810
nocodazole
[no description available]		2.0210aromatic ketone;
benzimidazoles;
carbamate ester;
thiophenes		antimitotic;
antineoplastic agent;
microtubule-destabilising agent;
tubulin modulator
metronidazole
Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death.		210C-nitro compound;
imidazoles;
primary alcohol		antiamoebic agent;
antibacterial drug;
antimicrobial agent;
antiparasitic agent;
antitrichomonal drug;
environmental contaminant;
prodrug;
radiosensitizing agent;
xenobiotic
mitoxantrone
Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.		2.0610dihydroxyanthraquinoneanalgesic;
antineoplastic agent
oxonic acid
Oxonic Acid: Antagonist of urate oxidase.		2.07101,3,5-triazines;
monocarboxylic acid
pd 98059
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one: inhibits MAP kinase kinase (MEK) activity, p42 MAPK and p44 MAPK; structure in first source. 2-(2-amino-3-methoxyphenyl)chromen-4-one : A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'.		2.0710aromatic amine;
monomethoxyflavone		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector
sb 202190
4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)imidazole: structure given in first source; inhibits p38 MAP kinase		2.0410imidazoles;
organofluorine compound;
phenols;
pyridines		apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
vorinostat
Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).		3.110dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
temozolomide
[no description available]		2.0610imidazotetrazine;
monocarboxylic acid amide;
triazene derivative		alkylating agent;
antineoplastic agent;
prodrug
thalidomide
Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.		3.1910phthalimides;
piperidones
diethylnitrosamine
Diethylnitrosamine: A nitrosamine derivative with alkylating, carcinogenic, and mutagenic properties.. N-nitrosodiethylamine : A nitrosamine that is N-ethylethanamine substituted by a nitroso group at the N-atom.		2.2510nitrosaminecarcinogenic agent;
hepatotoxic agent;
mutagen
carbon tetrachloride
Carbon Tetrachloride: A solvent for oils, fats, lacquers, varnishes, rubber waxes, and resins, and a starting material in the manufacturing of organic compounds. Poisoning by inhalation, ingestion or skin absorption is possible and may be fatal. (Merck Index, 11th ed). tetrachloromethane : A chlorocarbon that is methane in which all the hydrogens have been replaced by chloro groups.		2.1510chlorocarbon;
chloromethanes		hepatotoxic agent;
refrigerant
serine
Serine: A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids.. serine : An alpha-amino acid that is alanine substituted at position 3 by a hydroxy group.		4.7250L-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid;
serine zwitterion;
serine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
vincristine
[no description available]		2.6120acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
2,3,4,6-tetrachlorophenol
2,3,4,6-tetrachlorophenol: RN given refers to parent cpd; see also record for tetrachlorophenol with locants for chloro groups not specified. 2,3,4,6-tetrachlorophenol : A tetrachlorophenol in which the chlorines are located at positions 2, 3, 4, and 6.		2.0510tetrachlorophenolxenobiotic metabolite
bromodeoxyuridine
Bromodeoxyuridine: A nucleoside that substitutes for thymidine in DNA and thus acts as an antimetabolite. It causes breaks in chromosomes and has been proposed as an antiviral and antineoplastic agent. It has been given orphan drug status for use in the treatment of primary brain tumors.		2.9510pyrimidine 2'-deoxyribonucleosideantimetabolite;
antineoplastic agent
galactose
galactopyranose : The pyranose form of galactose.		4.2131D-galactose;
galactopyranose		Escherichia coli metabolite;
mouse metabolite
phenylephrine
Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.. phenylephrine : A member of the class of the class of phenylethanolamines that is (1R)-2-(methylamino)-1-phenylethan-1-ol carrying an additional hydroxy substituent at position 3 on the phenyl ring.		2.0710phenols;
phenylethanolamines;
secondary amino compound		alpha-adrenergic agonist;
cardiotonic drug;
mydriatic agent;
nasal decongestant;
protective agent;
sympathomimetic agent;
vasoconstrictor agent
phenylalanine
Phenylalanine: An essential aromatic amino acid that is a precursor of MELANIN; DOPAMINE; noradrenalin (NOREPINEPHRINE), and THYROXINE.. L-phenylalanine : The L-enantiomer of phenylalanine.. phenylalanine : An aromatic amino acid that is alanine in which one of the methyl hydrogens is substituted by a phenyl group.		2.4920amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
phenylalanine;
proteinogenic amino acid		algal metabolite;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
Escherichia coli metabolite;
human xenobiotic metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
colchicine
(S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.		6.97380alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
ficusin
Ficusin: A naturally occurring furocoumarin, found in PSORALEA. After photoactivation with UV radiation, it binds DNA via single and double-stranded cross-linking.. psoralen : The simplest member of the class of psoralens that is 7H-furo[3,2-g]chromene having a keto group at position 7. It has been found in plants like Psoralea corylifolia and Ficus salicifolia.		2.110psoralensplant metabolite
dimethylformamide
Dimethylformamide: A formamide in which the amino hydrogens are replaced by methyl groups.. N,N-dimethylformamide : A member of the class of formamides that is formamide in which the amino hydrogens are replaced by methyl groups.		2.0510formamides;
volatile organic compound		geroprotector;
hepatotoxic agent;
polar aprotic solvent
arginine
Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.		3.711arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
ethylene
Plastipore: high density polyethylene sponge biocompatible material; used as posts in dental bridges		2.0410alkene;
gas molecular entity		plant hormone;
refrigerant
acetylene
[no description available]		2.0310alkyne;
gas molecular entity;
terminal acetylenic compound
perflutren
Definity: a fluorocarbon-filled ultrasonic contrast agent; Definity is tradename. octafluoropropane : A fluorocarbon that is propane in which all of the hydrogens have been replaced by fluorines.		2.0310fluoroalkane;
fluorocarbon
carbazole
carbazole: structure in first source		2.0510carbazole
quinoxalines
quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.		2.0210mancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene
quinoline
[no description available]		2.0210azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinolines
diphenyl
diphenyl: RN given refers to unlabeled cpd; structure		2.1510aromatic fungicide;
benzenes;
biphenyls		antifungal agrochemical;
antimicrobial food preservative
xanthenes
Xanthenes: Compounds with three aromatic rings in linear arrangement with an OXYGEN in the center ring.		4.0250xanthene
benzothiophene
[no description available]		2.07101-benzothiophenes;
benzothiophene
4-butyrolactone
4-Butyrolactone: One of the FURANS with a carbonyl thereby forming a cyclic lactone. It is an endogenous compound made from gamma-aminobutyrate and is the precursor of gamma-hydroxybutyrate. It is also used as a pharmacological agent and solvent.. tetrahydrofuranone : Any oxolane having an oxo- substituent at any position on the tetrahydrofuran ring.. gamma-butyrolactone : A butan-4-olide that is tetrahydrofuran substituted by an oxo group at position 2.		2.4520butan-4-olidemetabolite;
neurotoxin
acrylonitrile
[no description available]		1.9910aliphatic nitrile;
volatile organic compound		antifungal agent;
carcinogenic agent;
fungal metabolite;
mutagen;
polar aprotic solvent
3-hydroxybutanal
[no description available]		2.4110
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		2.9740pyrrole;
secondary amine
furan
furan : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing four carbons and one oxygen, with formula C4H4O. It is a toxic, flammable, low-boiling (31degreeC) colourless liquid.		2.0310furans;
mancude organic heteromonocyclic parent;
monocyclic heteroarene		carcinogenic agent;
hepatotoxic agent;
Maillard reaction product
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		3.3260mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
dichlone
dichlone: structure		2.2110
benzil
benzil: structure. benzil : An alpha-diketone that is ethane-1,2-dione substituted by phenyl groups at positions 1 and 2 respectively.		2.0410alpha-diketone;
aromatic ketone
tripropionin
tripropionin : A triglyceride obtained by formal acylation of the three hydroxy groups of glycerol by propionic acid.		2.1510propanoate ester;
triglyceride		flavouring agent
perylene
Perylene: A 20-carbon dibenz(de,kl)anthracene that can be viewed as a naphthalene fused to a phenalene or as dinaphthalene. It is used as fluorescent lipid probe in the cytochemistry of membranes and is a polycyclic hydrocarbon pollutant in soil and water. Derivatives may be carcinogenic.. perylene : An ortho- and peri-fused polycyclic arene comprising of five benzene rings that is anthracene in which the d,e and k,l sides are fused to benzene rings.		2.520ortho- and peri-fused polycyclic arene;
perylenes
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		3.1910azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
indazoles
Indazoles: A group of heterocyclic aromatic organic compounds consisting of the fusion of BENZENE and PYRAZOLES.		4.821indazole
benzofuran
benzofuran: RN & structure given in first source. 1-benzofuran : A benzofuran consisting of fused benzene and furan rings. It is the parent compound of the class of 1-benzofurans.		2.07101-benzofurans;
benzofuran
cyclopentane
Cyclopentanes: A group of alicyclic hydrocarbons with the general formula R-C5H9.. cyclopentanes : Cyclopentane and its derivatives formed by substitution.		2.5120cycloalkane;
cyclopentanes;
volatile organic compound		non-polar solvent
isoxazoles
Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.		3.3360isoxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
oxazoles
Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.		2.99401,3-oxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
thiazoles
[no description available]		4.54701,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
1,2,4-triazole
1,2,4-triazole: RN given refers to 1H-1,2,4-triazole		2.21101,2,4-triazole
pyridazine
pyridazine: structure given in first source		2.0810diazine;
pyridazines
pyrimidine
pyrimidine : The parent compound of the pyrimidines; a diazine having the two nitrogens at the 1- and 3-positions.		2.0410diazine;
pyrimidines		Daphnia magna metabolite
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		4.0520diazine;
pyrazines		Daphnia magna metabolite
rhein
[no description available]		2.6920dihydroxyanthraquinone
podophyllotoxin
Podophyllum: A genus of poisonous American herbs, family BERBERIDACEAE. The roots yield PODOPHYLLOTOXIN and other pharmacologically important agents. The plant was formerly used as a cholagogue and cathartic. It is different from the European mandrake, MANDRAGORA.		4.5170furonaphthodioxole;
lignan;
organic heterotetracyclic compound		antimitotic;
antineoplastic agent;
keratolytic drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
azomycin
azomycin: RN given refers to parent cpd with specified locant; structure		2.5320C-nitro compound;
imidazoles		antitubercular agent
tropolone
Tropolone: A seven-membered aromatic ring compound. It is structurally related to a number of naturally occurring antifungal compounds (ANTIFUNGAL AGENTS).. tropolone : A cyclic ketone that is cyclohepta-2,4,6-trien-1-one substituted by a hydroxy group at position 2. It is a toxin produced by the agricultural pathogen Burkholderia plantarii.		1.9710alpha-hydroxy ketone;
cyclic ketone;
enol		bacterial metabolite;
fungicide;
toxin
2-pyrrolecarboxylic acid
2-pyrrolecarboxylic acid: hypocalcemic action; structure. pyrrole-2-carboxylic acid : A pyrrolecarboxylic acid that is 1H-pyrrole carrying a carboxy substituent at position 2.		2.0310pyrrolecarboxylic acidplant metabolite
cyclopentenone
2-cyclopenten-1-one : An enone that is cyclopentanone having a C=C double bond at position 2.		2.4110alicyclic ketone;
enone		Hsp70 inducer
deoxycytidine
[no description available]		2.110pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
phenylglyoxal
[no description available]		2.0410phenylacetaldehydes
potassium hydroxide
potassium hydroxide: RN given refers to cpd with MF of K-OH		2.0510alkali metal hydroxide
arsenic trioxide
Arsenic Trioxide: An inorganic compound with the chemical formula As2O3 that is used for the treatment of ACUTE PROMYELOCYTIC LEUKEMIA in patients who have relapsed from, or are resistant to, conventional drug therapy.		3.1310
2,5-dihydrofuran
2,5-dihydrofuran: structure in first source		2.1510
sulfur hexafluoride
Sulfur Hexafluoride: Sulfur hexafluoride. An inert gas used mainly as a test gas in respiratory physiology. Other uses include its injection in vitreoretinal surgery to restore the vitreous chamber and as a tracer in monitoring the dispersion and deposition of air pollutants.. sulfur hexafluoride : A sulfur coordination entity consisting of six fluorine atoms attached to a central sulfur atom. It is the most potent greenhouse gas currently known, with a global warming potential of 23,900 times that of CO2 over a 100 year period (SF6 has an estimated lifetime in the atmosphere of between 800 and 3,000 years).		2.1710sulfur coordination entitygreenhouse gas;
NMR chemical shift reference compound;
ultrasound contrast agent
fluorescein-5-isothiocyanate
Fluorescein-5-isothiocyanate: Fluorescent probe capable of being conjugated to tissue and proteins. It is used as a label in fluorescent antibody staining procedures as well as protein- and amino acid-binding techniques.. fluorescein 5-isothiocyanate : The 5-isomer of fluorescein isothiocyanate. Acts as a fluorescent probe capable of being conjugated to tissue and proteins; used as a label in fluorescent antibody staining procedures as well as protein- and amino acid-binding techniques.		2.4520fluorescein isothiocyanate
lutetium
Lutetium: An element of the rare earth family of metals. It has the atomic symbol Lu, atomic number 71, and atomic weight 175.		2.1510d-block element atom;
lanthanoid atom
palladium
Palladium: A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.. palladium : Chemical element (nickel group element atom) with atomic number 46.		2.9840metal allergen;
nickel group element atom;
platinum group metal atom
platinum
Platinum: A heavy, soft, whitish metal, resembling tin, with atomic number 78, atomic weight 195.084, symbol Pt. It is used in manufacturing equipment for laboratory and industrial use. It occurs as a black powder (platinum black) and as a spongy substance (spongy platinum) and may have been known in Pliny's time as alutiae.		2.5220elemental platinum;
nickel group element atom;
platinum group metal atom
ruthenium
Ruthenium: A hard, brittle, grayish-white rare earth metal with an atomic symbol Ru, atomic number 44, and atomic weight 101.07. It is used as a catalyst and hardener for PLATINUM and PALLADIUM.		2.6320iron group element atom;
platinum group metal atom
cerium
Cerium: An element of the rare earth family of metals. It has the atomic symbol Ce, atomic number 58, and atomic weight 140.12. Cerium is a malleable metal used in industrial applications.		2.3110f-block element atom;
lanthanoid atom
erbium
Erbium: Erbium. An element of the rare earth family of metals. It has the atomic symbol Er, atomic number 68, and atomic weight 167.26.		2.0710f-block element atom;
lanthanoid atom
gadolinium
Gadolinium: An element of the rare earth family of metals. It has the atomic symbol Gd, atomic number 64, and atomic weight 157.25. Its oxide is used in the control rods of some nuclear reactors.		2.0310f-block element atom;
lanthanoid atom
gold
Gold: A yellow metallic element with the atomic symbol Au, atomic number 79, and atomic weight 197. It is used in jewelry, goldplating of other metals, as currency, and in dental restoration. Many of its clinical applications, such as ANTIRHEUMATIC AGENTS, are in the form of its salts.		2.1310copper group element atom;
elemental gold
ytterbium
Ytterbium: An element of the rare earth family of metals. It has the atomic symbol Yb, atomic number 70, and atomic weight 173. Ytterbium has been used in lasers and as a portable x-ray source.		2.0710f-block element atom;
lanthanoid atom
yttrium
Yttrium: An element of the rare earth family of metals. It has the atomic symbol Y, atomic number 39, and atomic weight 88.91. In conjunction with other rare earths, yttrium is used as a phosphor in television receivers and is a component of the yttrium-aluminum garnet (YAG) lasers.		2.0710d-block element atom;
rare earth metal atom;
scandium group element atom
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		4.5970delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
bromine
Bromine: A halogen with the atomic symbol Br, atomic number 35, and atomic weight 79.904. It is a volatile reddish-brown liquid that gives off suffocating vapors, is corrosive to the skin, and may cause severe gastroenteritis if ingested.		2.0510diatomic bromine
fluorine
Fluorine: A nonmetallic, diatomic gas that is a trace element and member of the halogen family. It is used in dentistry as fluoride (FLUORIDES) to prevent dental caries.		2.4720diatomic fluorine;
gas molecular entity		NMR chemical shift reference compound
fluorides
[no description available]		2.0710halide anion;
monoatomic fluorine
daunorubicin
Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola.		2.4120aminoglycoside antibiotic;
anthracycline;
p-quinones;
tetracenequinones		antineoplastic agent;
bacterial metabolite
alkenes
[no description available]		3.1650
glutamic acid
Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.		3.2340glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
azides
Azides: Organic or inorganic compounds that contain the -N3 group.. azide : Any nitrogen molecular entity containing the group -N3.		210pseudohalide anionmitochondrial respiratory-chain inhibitor
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		9.32223taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
etoposide
[no description available]		3.8830beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound		antineoplastic agent;
DNA synthesis inhibitor
diltiazem
Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension.		2.11105-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetateantihypertensive agent;
calcium channel blocker;
vasodilator agent
ng-nitroarginine methyl ester
NG-Nitroarginine Methyl Ester: A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.		2.4220alpha-amino acid ester;
L-arginine derivative;
methyl ester;
N-nitro compound		EC 1.14.13.39 (nitric oxide synthase) inhibitor
indacrinone
indacrinone: polyvalent saluretic; RN given refers to parent cpd without isomeric designation; structure		2.0310
2-methoxy-5-(2',3',4'-trimethoxyphenyl)tropone
2-methoxy-5-(2',3',4'-trimethoxyphenyl)tropone: structure given in first source		1.9710
pimonidazole
pimonidazole: structure given in first source		2.1110
flavone acetic acid
flavone acetic acid: structure given in first source		2.4420
gemcitabine
gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.		3.6820organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic
irinotecan
[no description available]		2.0210carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
vanadates
Vanadates: Oxyvanadium ions in various states of oxidation. They act primarily as ion transport inhibitors due to their inhibition of Na(+)-, K(+)-, and Ca(+)-ATPase transport systems. They also have insulin-like action, positive inotropic action on cardiac ventricular muscle, and other metabolic effects.. vanadate(3-) : A vanadium oxoanion that is a trianion with formula VO4 in which the vanadium is in the +5 oxidation state and is attached to four oxygen atoms.		2.0710trivalent inorganic anion;
vanadium oxoanion		EC 3.1.3.1 (alkaline phosphatase) inhibitor;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
EC 3.1.3.41 (4-nitrophenylphosphatase) inhibitor;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor
carbogen
carbogen: mixture of 95% O2 & 5% CO2		2.0310
glucose, (beta-d)-isomer
beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.		2.0710D-glucopyranoseepitope;
mouse metabolite
thiazolyl blue
thiazolyl blue: RN & II refers to bromide. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide : The bromide salt of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium.		2.7530organic bromide saltcolorimetric reagent;
dye
plerixafor
plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma.		2.2110azacycloalkane;
azamacrocycle;
benzenes;
crown amine;
secondary amino compound;
tertiary amino compound		anti-HIV agent;
antineoplastic agent;
C-X-C chemokine receptor type 4 antagonist;
immunological adjuvant
goralatide
goralatide: from fetal calf bone marrow; exerts a high inhibitory activity on the proliferation of hematopoietic pluripotent stem cells. goralatide : A tetrapeptide that is Ser-Asp-Lys-Pro in which the N-terminal amino group carries an acetyl group. It is selective inhibitor of primitive haematopoietic cell proliferation and exhibits anti-inflammatory, anti-fibrotic, and pro-angiogenic properties.		2.0610oligopeptide;
tetrapeptide		anti-inflammatory agent;
pro-angiogenic agent
2-methoxyestradiol
2-methoxy-17beta-estradiol : A 17beta-hydroxy steroid, being 17beta-estradiol methoxylated at C-2.		2.713017beta-hydroxy steroid;
3-hydroxy steroid		angiogenesis modulating agent;
antimitotic;
antineoplastic agent;
human metabolite;
metabolite;
mouse metabolite
1,7-phenanthroline
[no description available]		2.0310phenanthroline
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		3.18501,2,3-triazole
1h-tetrazole
tetrazole : An azaarene that is a five-membered ring composed of 4 nitrogen and 1 carbon atom.. 2H-tetrazole : A tetrazole tautomer where the proton is located on the 2 position.		2.0710one-carbon compound;
tetrazole
fluorodeoxyglucose f18
Fluorodeoxyglucose F18: The compound is given by intravenous injection to do POSITRON-EMISSION TOMOGRAPHY for the assessment of cerebral and myocardial glucose metabolism in various physiological or pathological states including stroke and myocardial ischemia. It is also employed for the detection of malignant tumors including those of the brain, liver, and thyroid gland. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1162)		2102-deoxy-2-((18)F)fluoro-D-glucose;
2-deoxy-2-fluoro-aldehydo-D-glucose
cryptopleurine
cryptopleurine: plant bark alkaloid shown to inhibit protein synthesis; RN given refers to (R)-isomer; structure. cryptopleurine : An organic heteropentacyclic compound that is (14aR)-11,12,13,14,14a,15-hexahydro-9H-dibenzo[f,h]pyrido[1,2-b]isoquinoline substituted at positions 2, 3 and 6 by methoxy groups.		2.0310alkaloid antibiotic;
alkaloid;
aromatic ether;
organic heteropentacyclic compound		antineoplastic agent;
antiviral agent;
protein synthesis inhibitor
sennidin a
dihydroxydianthrone: aglycone of senna glycosides		2.110
6,7-dichloroquinoline-5,8-dione
6,7-dichloro-5,8-quinolinedione: structure in first source		2.2110
Koenimbine
koenimbin: has antineoplastic activity; isolated from curry leaf, Murraya koenigii; structure in first source		3.5110carbazoles
combretastatin
combretastatin: cytotoxic principle from South African tree COMBRETUM caffrum; structure given in first source; acts at COLCHICINE site of TUBULIN		5.89170
thiophene a
thiophene A: RN not in Chemline 4/87; RN from Chem Abstracts Index Guide 1986; structure given in first source		210
arginyl-glycyl-aspartic acid
arginyl-glycyl-aspartic acid: amino acid sequence of basic unit of widespread cellular recognition system		3.1550oligopeptide
ecteinascidin 743
[no description available]		3.110acetate ester;
azaspiro compound;
bridged compound;
hemiaminal;
isoquinoline alkaloid;
lactone;
organic heteropolycyclic compound;
organic sulfide;
oxaspiro compound;
polyphenol;
tertiary amino compound		alkylating agent;
angiogenesis modulating agent;
anti-inflammatory agent;
antineoplastic agent;
marine metabolite
anecortave acetate
anecortave acetate: derived from cortisone (11 OH replaced by 9-11 double bond)		2.0310organic molecular entity
1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid: structure given in first source. DOTA : An azamacrocyle in which four nitrogen atoms at positions 1, 4, 7 and 10 of a twelve-membered ring are each substituted with a carboxymethyl group.		2.2510azamacrocyclechelator;
copper chelator
gadolinium 1,4,7,10-tetraazacyclododecane-n,n',n'',n'''-tetraacetate
gadolinium 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetate: RN refers to Na salt		2.110
carbene
carbene: electrically neutral species H2C: and its derivatives, in which the carbon is covalently bonded to two univalent groups of any kind or a divalent group and bears two nonbonding electrons; carbene is the name of the parent hydride :CH2 ; hence, the name dichlorocarbene for :CCl2. However, names for acyclic and cyclic hydrocarbons containing one or more divalent carbon atoms are derived from the name of the corresponding all-4-hydrocarbon using the suffix -ylidene; methylene carbene also available. carbene : The electrically neutral species H2C(2.) and its derivatives, in which the carbon is covalently bonded to two univalent groups of any kind or a divalent group and bears two nonbonding electrons, which may be spin-paired (singlet state) or spin-non-paired (triplet state).		2.5220carbene;
methanediyl
cyclopropene
cyclopropene: structure. cyclopropene : A cycloalkene that consists of cyclopropane having a double bond in the ring. The parent of the class of cyclopropenes.		2.0810cycloalkene;
cyclopropenes
imatinib mesylate
imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.		3.110methanesulfonate saltanticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
vadimezan
vadimezan : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a 5,6-dimethyl-9-oxoxanthen-4-yl group.		8.18170monocarboxylic acid;
xanthones		antineoplastic agent
azatoxin
azatoxin: structure given in first source; a topoisomerase II inhibitor		2.1710
1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene
1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene: inhibits tubulin polymerization; RN & structure given in first source		2.420
methotrexate
[no description available]		2.0810dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
combretastatin b-1
combretastatin B-1: structure in first source		3.3510
beta-lactams
2-azetidinone: structure in first source. azetidin-2-one : An unsubstituted beta-lactam compound.. beta-lactam : A lactam in which the amide bond is contained within a four-membered ring, which includes the amide nitrogen and the carbonyl carbon.		3.3460beta-lactam antibiotic allergen;
beta-lactam
proline
Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.		2.0310amino acid zwitterion;
glutamine family amino acid;
L-alpha-amino acid;
proline;
proteinogenic amino acid		algal metabolite;
compatible osmolytes;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
amphethinile
amphethinile: structure given in first source		1.9710
docetaxel anhydrous
Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.		2.0110secondary alpha-hydroxy ketone;
tetracyclic diterpenoid		antimalarial;
antineoplastic agent;
photosensitizing agent
singlet oxygen
Singlet Oxygen: An excited state of molecular oxygen generated photochemically or chemically. Singlet oxygen reacts with a variety of biological molecules such as NUCLEIC ACIDS; PROTEINS; and LIPIDS; causing oxidative damages.		2.610chalcogen;
monoatomic oxygen;
nonmetal atom		macronutrient
protohypericin
protohypericin: structure in first source		2.1110
sb 203580
[no description available]		2.0410imidazoles;
monofluorobenzenes;
pyridines;
sulfoxide		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent
sorafenib
[no description available]		2.2110(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
batabulin
batabulin: disrupts microtubule polymerization by binding certain beta-tubulin isotypes; effective against some multidrug-resistant tumors; structure in first source		3.2310
demecolcine
Demecolcine: An alkaloid isolated from Colchicum autumnale L. and used as an antineoplastic.. (-)-demecolcine : A secondary amino compound that is (S)-colchicine in which the N-acetyl group is replaced by an N-methyl group. Isolable from the autumn crocus, Colchicum autumnale, it is less toxic than colchicine and is used as an antineoplastic.		3.7120alkaloid;
secondary amino compound		antineoplastic agent;
microtubule-destabilising agent
benzofurans
Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.		2.520
o-(chloroacetylcarbamoyl)fumagillol
O-(Chloroacetylcarbamoyl)fumagillol: Semisynthetic analog of fumagillin (a cyclohexane-sesquiterpene antibiotic isolated from ASPERGILLUS FUMIGATUS) that inhibits angiogenesis.. O-(chloroacetylcarbamoyl)fumagillol : A carbamate ester that is fumagillol in which the hydroxy group has been converted to the corresponding N-(chloroacetyl)carbamate derivative.		210carbamate ester;
organochlorine compound;
semisynthetic derivative;
sesquiterpenoid;
spiro-epoxide		angiogenesis inhibitor;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
methionine aminopeptidase 2 inhibitor;
retinoic acid receptor alpha antagonist
bortezomib
[no description available]		4.0520amino acid amide;
L-phenylalanine derivative;
pyrazines		antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
carboplatin
[no description available]		7.2464
nitroarginine
Nitroarginine: An inhibitor of nitric oxide synthetase which has been shown to prevent glutamate toxicity. Nitroarginine has been experimentally tested for its ability to prevent ammonia toxicity and ammonia-induced alterations in brain energy and ammonia metabolites. (Neurochem Res 1995:200(4):451-6). N(gamma)-nitro-L-arginine : An L-arginine derivative that is L-arginine in which the terminal nitrogen of the guanidyl group is replaced by a nitro group.		2.4320guanidines;
L-arginine derivative;
N-nitro compound;
non-proteinogenic L-alpha-amino acid
lignans
Lignans: A class of dibenzylbutane derivatives which occurs in higher plants and in fluids (bile, serum, urine, etc.) in man and other animals. These compounds, which have a potential anti-cancer role, can be synthesized in vitro by human fecal flora. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)		2.0210
doxorubicin hydrochloride
[no description available]		2.7620anthracycline
betadex
beta-Cyclodextrins: Cyclic GLUCANS consisting of seven (7) glucopyranose units linked by 1,4-glycosidic bonds.		2.110cyclodextrin
tretinoin
Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.		3.1310retinoic acid;
vitamin A		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule
resveratrol
trans-resveratrol : A resveratrol in which the double bond has E configuration.		2.0710resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
y 27632
Y 27632: RN given for di-HCl salt; inhibits Rho-associated protein kinase; inhibits calcium sensitization to affect smooth muscle relaxation; structure in first source. Y-27632 : A monocarboxylic acid amide that is trans-[(1R)-1-aminoethyl]cyclohexanecarboxamide in which one of the nitrogens of the aminocarbony group is substituted by a pyridine nucleus. It has been shown to exhibit inhibitory activity against Rho-associated protein kinase (ROCK) enzyme.		2.5420aromatic amide
imidazolidines
[no description available]		2.7730azacycloalkane;
imidazolidines;
saturated organic heteromonocyclic parent
chalcone
trans-chalcone : The trans-isomer of chalcone.		4.2650chalconeEC 3.2.1.1 (alpha-amylase) inhibitor
piplartine
piplartine: Antineoplastic Agent, Phytogenic; alkaloid from Piper; structure in first source		2.1310cinnamamides;
dicarboximide
squalene
Addavax: an oil-water nanoemulsion and adjuvant containing squalene, Tween 80, and sorbitane trioleate		2.110triterpenehuman metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
stilbenes
Stilbenes: Organic compounds that contain 1,2-diphenylethylene as a functional group.. trans-stilbene : The trans-isomer of stilbene.		19.1254521stilbene
pyrophosphate
Diphosphates: Inorganic salts of phosphoric acid that contain two phosphate groups.		6.9481diphosphate ion
sesquiterpenes
[no description available]		210
mercaptopurine
Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis.		2.0510aryl thiol;
purines;
thiocarbonyl compound		anticoronaviral agent;
antimetabolite;
antineoplastic agent
curcumin
Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.. curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.		2.9830aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol		anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger
potassium oxonate
potassium oxonate: used to induce hyperuricemia in mice		2.0710organic molecular entity
ferric ferrocyanide
ferric ferrocyanide: antidote to thallium poisoning; RN given refers to Fe(+3)[3:4] salt; structure		2.2110
tamoxifen
[no description available]		2.110stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
oreoselone
oreoselone: Coumarins from the aerial part of Halocnemum strobilaceum; structure in first source		2.110
monastrol
monastrol: stops mitosis by fostering formation of monopolar spindles; structure in first source. (S)-monastrol : An ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate that has S configuration.. monastrol : A racemate comprising equimolar amounts of R- and S-monastrol.. ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate : A member of the class of thioureas that is 3,4-dihydropyrimidine-2(1)-thione substituted by a 3-hydroxyphenyl group at position 4, an ethoxycarbonyl group at position 5, and a methyl group at position 6.		2.0510enoate ester;
ethyl ester;
phenols;
racemate;
thioureas		antileishmanial agent;
antimitotic;
antineoplastic agent;
EC 3.5.1.5 (urease) inhibitor
u 0126
U 0126: protein kinase kinase inhibitor; structure in first source		2.0510aryl sulfide;
dinitrile;
enamine;
substituted aniline		antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent
lithium
Lithium: An element in the alkali metals family. It has the atomic symbol Li, atomic number 3, and atomic weight [6.938; 6.997]. Salts of lithium are used in treating BIPOLAR DISORDER.		3.1910alkali metal atom
e 7010
E 7010: inhibits tubulin polymerization; structure given in first source		3.5420sulfonamide
dasatinib
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).		2.53201,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
zd 6474
CH 331: structure in first source		3.1910aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine		antineoplastic agent;
tyrosine kinase inhibitor
sanorg 34006
idraparinux: a synthetic analogue of the pentasaccharide sequence in heparins		2.0110
ginsenosides
ginsenoside : Triterpenoid saponins with a dammarane-like skeleton originally isolated from ginseng (Panax) species. Use of the term has been extended to include semi-synthetic derivatives.		2.3110
mtt formazan
MTT formazan: a blue MEM-insoluble mitochondrial byproduct; used to determine viability of cells with active mitochondrial dehydrogenase enzymes		2.0310
naphthoquinones
Naphthoquinones: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.		2.2110
11-cis-retinal
Rhodopsin: A purplish-red, light-sensitive pigment found in RETINAL ROD CELLS of most vertebrates. It is a complex consisting of a molecule of ROD OPSIN and a molecule of 11-cis retinal (RETINALDEHYDE). Rhodopsin exhibits peak absorption wavelength at about 500 nm.. 11-cis-retinal : A retinal having 2E,4Z,6E,8E-double bond geometry.		2.0110retinalchromophore;
human metabolite;
mouse metabolite
hymecromone
Hymecromone: A coumarin derivative possessing properties as a spasmolytic, choleretic and light-protective agent. It is also used in ANALYTICAL CHEMISTRY TECHNIQUES for the determination of NITRIC ACID.		2.1110hydroxycoumarinantineoplastic agent;
hyaluronic acid synthesis inhibitor
trans-2,3',4,5'-tetrahydroxystilbene
trans-2,3',4,5'-tetrahydroxystilbene: hydroxystilbene oxyresveratrol		2.0710stilbenoid
pterostilbene
[no description available]		2.0710diether;
methoxybenzenes;
stilbenol		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
hypoglycemic agent;
neuroprotective agent;
neurotransmitter;
plant metabolite;
radical scavenger
curacin a
curacin A: RN refers to curacin A (the Z,E,E-isomer), the major lipid component of a strain of the marine cyanobacterium Lyngbya majuscula; structure given in first source		2.0210thiazoles
fondaparinux
Fondaparinux: Synthetic pentasaccharide that mediates the interaction of HEPARIN with ANTITHROMBINS and inhibits FACTOR Xa; it is used for prevention of VENOUS THROMBOEMBOLISM after surgery.. fondaparinux : A synthetic pentasaccharide which, apart from the O-methyl group at the reducing end of the molecule, consists of monomeric sugar units which are identical to a sequence of five monomeric sugar units that can be isolated after either chemical or enzymatic cleavage of the polymeric glycosaminoglycans heparin and heparan sulfate.		2.0110amino sugar;
oligosaccharide sulfate;
pentasaccharide derivative		anticoagulant
sirolimus
Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.		2.5720antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
semaxinib
semaxanib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is replaced by a 3,5-dimethylpyrrol-2-yl group.		2.4320olefinic compound;
oxindoles;
pyrroles		angiogenesis modulating agent;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist
hemiasterlin
hemiasterlin: structure in first source		2.0410
indanocine
indanocine: a microtubule-binding indanone with antiproliferative activity; structure in first source		2.0210
arsenic
Arsenic: A shiny gray element with atomic symbol As, atomic number 33, and atomic weight 75. It occurs throughout the universe, mostly in the form of metallic arsenides. Most forms are toxic. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), arsenic and certain arsenic compounds have been listed as known carcinogens. (From Merck Index, 11th ed)		3.1310metalloid atom;
pnictogen		micronutrient
enalapril
Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).		2.3110dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug
nsc 600032
combretastatin A-1: from Combretum caffrum; structure given in first source		4.3960
fumarates
Fumarates: Compounds based on fumaric acid.. fumarate(2-) : A C4-dicarboxylate that is the E-isomer of but-2-enedioate(2-)		2.0510butenedioate;
C4-dicarboxylate		human metabolite;
metabolite;
Saccharomyces cerevisiae metabolite
silicon
Silicon: A trace element that constitutes about 27.6% of the earth's crust in the form of SILICON DIOXIDE. It does not occur free in nature. Silicon has the atomic symbol Si, atomic number 14, and atomic weight [28.084; 28.086].		2.4620carbon group element atom;
metalloid atom;
nonmetal atom
phosphorus
Phosphorus: A non-metal element that has the atomic symbol P, atomic number 15, and atomic weight 31. It is an essential element that takes part in a broad variety of biochemical reactions.		210monoatomic phosphorus;
nonmetal atom;
pnictogen		macronutrient
boron
Boron: A trace element with the atomic symbol B, atomic number 5, and atomic weight [10.806; 10.821]. Boron-10, an isotope of boron, is used as a neutron absorber in BORON NEUTRON CAPTURE THERAPY.		2.2110boron group element atom;
metalloid atom;
nonmetal atom		micronutrient
ximelagatran
ximelagatran: prodrug (via hydroxylation) of melagatran & a direct thrombin inhibitor; liver toxicity concerns so AZD0837 being developed to replace this. ximelagatran : A member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage.		2.0110amidoxime;
azetidines;
carboxamide;
ethyl ester;
hydroxylamines;
secondary amino compound;
secondary carboxamide;
tertiary carboxamide		anticoagulant;
EC 3.4.21.5 (thrombin) inhibitor;
prodrug;
serine protease inhibitor
carbocyanines
Carbocyanines: Compounds that contain three methine groups. They are frequently used as cationic dyes used for differential staining of biological materials.		2.1110cyanine dye;
organic iodide salt		fluorochrome
selenium
Selenium: An element with the atomic symbol Se, atomic number 34, and atomic weight 78.97. It is an essential micronutrient for mammals and other animals but is toxic in large amounts. Selenium protects intracellular structures against oxidative damage. It is an essential component of GLUTATHIONE PEROXIDASE.		2.5220chalcogen;
nonmetal atom		micronutrient
bafilomycin a1
bafilomycin A1: from Streptomyces griseus; structure given in first source. bafilomycin A1 : The most used of the bafilomycins, a family of toxic macrolide antibiotics derived from Streptomyces griseus.		2.110cyclic hemiketal;
macrolide antibiotic;
oxanes		apoptosis inducer;
autophagy inhibitor;
bacterial metabolite;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
EC 3.6.3.14 (H(+)-transporting two-sector ATPase) inhibitor;
ferroptosis inhibitor;
fungicide;
potassium ionophore;
toxin
manumycin
manumycin: an NSAID; RN given for (1S-(1alpha,3(2E,4E,6S*),5alpha,5(1E,3E,5E),6alpha))-isomer; a farnesyl protein transferase inhibitor; from Streptomyces parvulus; MF C31-H38-N2-O7; structure given in first source. manumycin A : A polyketide with formula C31H38N2O7 initially isolated from Streptomyces parvulus as a result of a random screening program for farnesyl transferase (FTase) inhibitors. It is a natural product that exhibits anticancer and antibiotic properties.		2.9510enamide;
epoxide;
organic heterobicyclic compound;
polyketide;
secondary carboxamide;
tertiary alcohol		antiatherosclerotic agent;
antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
marine metabolite
pironetin
pironetin: a microbial secondary metabolite having the activity of shortening plant height from Streptomyces sp.; structure in first source		2.1110aliphatic alcohol
mulberroside a
mulberroside A: structure in first source		2.0710glycoside;
stilbenoid
tanespimycin
CP 127374: analog of herbimycin A		3.1101,4-benzoquinones;
ansamycin;
carbamate ester;
organic heterobicyclic compound;
secondary amino compound		antineoplastic agent;
apoptosis inducer;
Hsp90 inhibitor
gadolinium dtpa
Gadolinium DTPA: A complex of gadolinium with a chelating agent, diethylenetriamine penta-acetic acid (DTPA see PENTETIC ACID), that is given to enhance the image in cranial and spinal MRIs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p706)		3.4170gadolinium coordination entityMRI contrast agent
soblidotin
soblidotin: a dolastatin 10 derivative; RN refers to (2S-(1(1R*(R*),2S*),2R*(1S*,2S*)))-isomer; structure given in first source. soblidotin : A tetrapeptide derivative of dolastatin 10. It is an inhibitor of tubulin polymerization which exhibits potent antitumor activity.		4.3330tetrapeptideantineoplastic agent;
apoptosis inducer;
microtubule-destabilising agent
ac 7700
AC 7700: a vascular disrupting agent; structure in first source		4.7250
oxi 4503
Oxi 4503: diphosphate prodrug of cambretastatin A1		6.9481
hti-286
HTI-286: a synthetic analog of the tripeptide hemiasterlin; structure in first source		2.0410
formazans
Formazans: Colored azo compounds formed by the reduction of tetrazolium salts. Employing this reaction, oxidoreductase activity can be determined quantitatively in tissue sections by allowing the enzymes to act on their specific substrates in the presence of tetrazolium salts.		2.0310
ave-8063
AVE-8063: has both antivascular and antineoplastic activities; structure in first source		2.1110
efatutazone
efatutazone: a high-affinity PPARgamma agonist with antineoplastic activity		3.2510
reparixin
reparixin: inhibits CXCR1 to prevent polymorphonuclear cell recruitment		2.3110monoterpenoid
mocetinostat
mocetinostat: undergoing phase II clinical trials for treatment of cancer. mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).		2.4420aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline		antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent
lamellarin d
lamellarin D: a benzo-isoquinoline-coumarin		2.0510
zd 6126
[no description available]		6.7370
dolastatin 15
dolastatin 15: from Dolabella auricularia; seven subunit depsipeptide		2.0810
npi 2358
NPI 2358: antineoplastic; structure in first source. plinabulin : A member of the class of 2,5-diketopiperazines that is piperazine-2,5-dione substituted by benzylidene and (5-tert-butyl-1H-imidazol-4-yl)methylidene groups at positions 3 and 6, respectively. It is a vascular disrupting agent and a microtubule destabalising agent which was in clinical trials (now discontinued) for the treatment of non-small cell lung cancer.		3.54202,5-diketopiperazines;
benzenes;
imidazoles;
olefinic compound		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
microtubule-destabilising agent
pazopanib
pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer.		9.5511aminopyrimidine;
indazoles;
sulfonamide		angiogenesis modulating agent;
antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist
(1,2-bis(1,2-benzisoselenazolone-3(2h)-ketone))ethane
(1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone))ethane: has antineoplastic activity; structure in first source		2.4110
cis-3,4',5-trimethoxy-3'-aminostilbene
cis-3,4',5-trimethoxy-3'-aminostilbene: structure in first source		2.0410
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		2.4720
abt-737
[no description available]		2.110aromatic amine;
aryl sulfide;
biphenyls;
C-nitro compound;
monochlorobenzenes;
N-arylpiperazine;
N-sulfonylcarboxamide;
secondary amino compound;
tertiary amino compound		anti-allergic agent;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor
peloruside a
peloruside A: Antibiotics, Antineoplastic from the sponge Mycale; structure in first source. peloruside A : A macrolide that is a novel secondary metabolite isolated from a New Zealand marine sponge, Mycale hentscheli.		2.0810
er-086526
eribulin: a halichondrin B derivative that suppresses microtubule growth and acts as an antimitotic agent; structure in first source. eribulin : A fully synthetic macrocyclic ketone analogue of marine sponge natural products. Inhibits growth phase of microtubules via tubulin-based antimitotic mechanism, which leads to G2/M cell-cycle block, disruption of mitotic spindles, and, ultimately, apoptotic cell death after prolonged mitotic blockage		3.2310cyclic ketal;
cyclic ketone;
macrocycle;
polycyclic ether;
polyether;
primary amino compound		antineoplastic agent;
microtubule-destabilising agent
verubulin
verubulin: antineoplastic; a small-molecule inhibitor of microtubule formation that is not a substrate for multidrug resistance pumps; structure in first source		2.1710
ginsenoside rd
ginsenoside Rd: RN refers to (3beta,12beta)-isomer. ginsenoside Rd : A ginsenoside found in Panax ginseng and Panax japonicus var. major that is (20S)-ginsenoside Rg3 in which the hydroxy group at position 20 has been converted to its beta-D-glucopyranoside.		2.3110beta-D-glucoside;
ginsenoside;
tetracyclic triterpenoid		anti-inflammatory drug;
apoptosis inducer;
immunosuppressive agent;
neuroprotective agent;
plant metabolite;
vulnerary
combretastatin a-2
combretastatin A-2: isolated from Combretum caffrum; RN from first source; structure given in first source		2.3820
imidazolone
imidazolone: a reaction product of arginine with 3-deoxyglucosone which markedly accumulates in uremic serum; structure in first source		2.0610organonitrogen heterocyclic compound
indocyanine green
Indocyanine Green: A tricarbocyanine dye that is used diagnostically in liver function tests and to determine blood volume and cardiac output.		2.1101,1-diunsubstituted alkanesulfonate;
benzoindole;
cyanine dye
o-methylmurrayamine a
O-methylmurrayamine A: structure in first source		3.5110
cytochrome c-t
Cytochromes c: Cytochromes of the c type that are found in eukaryotic MITOCHONDRIA. They serve as redox intermediates that accept electrons from MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX III and transfer them to MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX IV.		2.0310
glucagon
Glucagon: A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511). glucagon : A 29-amino acid peptide hormone consisting of His, Ser, Gln, Gly, Thr, Phe, Thr, Ser, Asp, Tyr, Ser, Lys, Tyr, Leu, Asp, Ser, Arg, Arg, Ala, Gln, Asp, Phe, Val, Gln, Trp, Leu, Met, Asn and Thr residues joined in sequence.		3.711peptide hormone
complestatin
complestatin: compound extracted from Streptomyces lavendulae mycelia; on acid hydrolysis yields D-4-hydroxyphenylglycine & D-3,5-dichloro-4-hydroxyphenylglycine & acidic chromophore; inhibits gp120-CD4 binding. isocomplestatin : A heterodetic cyclic peptide which is a atropisomer of complestatin. It is isolated from the culture broth of Streptomyces and has anti-HIV-1 activity.. chloropeptin II : A heterodetic cyclic peptide consisting of N-acylated trytophan, 3,5-dichloro-4-hydroxyphenylglycine, 4-hydroxyphenylglycine, 3,5-dichloro-4-hydroxyphenylglycyl, tyrosine and 4-hydroxyphenylglycine residues joined in sequence and in which the side-chain of the central 4-hydroxyphenylglycine residue is attached to the side-chain of the tryptophan via a C3-C6 bond and to the side-chain of the tyrosine via an ether bond from C5. It is isolated from the culture broth of Streptomyces and has anti-HIV-1 activity.		2.0510cyclic ether;
heterodetic cyclic peptide;
indoles;
organic heterobicyclic compound;
organochlorine compound;
peptide antibiotic;
polyphenol		anti-HIV-1 agent;
antimicrobial agent;
HIV-1 integrase inhibitor;
metabolite
hoe 33342
bisbenzimide ethoxide trihydrochloride: benzimidazole fluorescent dye		2.730
crolibulin
crolibulin: a vascular disrupting agent with antineoplastic activity; structure in first source		2.1710neoflavonoid
chiniofon
Hydroxyquinolines: The 8-hydroxy derivatives inhibit various enzymes and their halogenated derivatives, though neurotoxic, are used as topical anti-infective agents, among other uses.		2.0610
cardiovascular agents
Cardiovascular Agents: Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume.		2.110
neurotensin
neurotensin, Tyr(11)-: RN given refers to parent cpd & (D)-isomer; RN for cpd without isomeric designation not avail 5/91		2.0510peptide hormonehuman metabolite;
mitogen;
neurotransmitter;
vulnerary
cabozantinib
cabozantinib: a multikinase inhibitor. cabozantinib : A dicarboxylic acid diamide that is N-phenyl-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide in which the hydrogen at position 4 on the phenyl ring is substituted by a (6,7-dimethoxyquinolin-4-yl)oxy group. A multi-tyrosine kinase inhibitor, used (as its malate salt) for the treatment of progressive, metastatic, medullary thyroid cancer.		3.1910aromatic ether;
dicarboxylic acid diamide;
organofluorine compound;
quinolines		antineoplastic agent;
tyrosine kinase inhibitor
piperidines
Piperidines: A family of hexahydropyridines.		3.1910
bryostatin 1
bryostatin 1: a protein kinase C activator; macrocyclic lactone from marine Bryozoan Bugula neritina; RN given refers to (1S*-(1R*,3R*,5Z,7S*,8E,11R*,12R*(2E,4E),13E,15R*,17S*(S*),21S*,23S*,25R*))-isomer; structure given in first source; activates protein kinase c. bryostatin 1 : A member of the class of bryostatins that is (17E)-2-oxooxacyclohexacos-17-ene which is substituted by hydroxy groups at positions 4, 10, and 20; an acetoxy group at position 8; methyl groups at positions 9, 9, 18, and 19; 2-methoxy-2-oxoethylidene groups at positions 14 and 24; an (E,E)-octa-2,4-dienoyloxy group at position 21; and with oxygen bridges linking positions 6 to 10, 12 to 16, and 20 to 24. It is one of the most abundant member of the class of bryostatins.		3.1410
exenatide
Exenatide: A synthetic form of exendin-4, a 39-amino acid peptide isolated from the venom of the Gila monster lizard (Heloderma suspectum). Exenatide increases CYCLIC AMP levels in pancreatic acinar cells and acts as a GLUCAGON-LIKE PEPTIDE-1 RECEPTOR (GLP-1) agonist and incretin mimetic, enhancing insulin secretion in response to increased glucose levels; it also suppresses inappropriate glucagon secretion and slows gastric emptying. It is used an anti-diabetic and anti-obesity agent.		3.711
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		3.3260benzenes;
hydroxycoumarin;
methyl ketone
almagate
pegaptanib: a 28-base ribonucleic acid aptamer covalently linked to two branched 20-kD polyethylene glycol moieties to block the activity of extracellular VEGF, specifically the 165-amino-acid isoform (VEGF165); for treatment of neovascular age-related macular degeneration		4.0410
2-ethylphenyl 4-(3-ethylureido)benzenesulfonate
2-ethylphenyl 4-(3-ethylureido)benzenesulfonate: has antineoplastic activity; structure in first source		2.0710
nitrophenols
Nitrophenols: PHENOLS carrying nitro group substituents.		2.110
steganacin
steganacin: bisbenzocyclooctadiene lactone extract from Steganotaenia araliacea; structure		2.0210
chondroitin sulfates
Chondroitin Sulfates: Derivatives of chondroitin which have a sulfate moiety esterified to the galactosamine moiety of chondroitin. Chondroitin sulfate A, or chondroitin 4-sulfate, and chondroitin sulfate C, or chondroitin 6-sulfate, have the sulfate esterified in the 4- and 6-positions, respectively. Chondroitin sulfate B (beta heparin; DERMATAN SULFATE) is a misnomer and this compound is not a true chondroitin sulfate.		2.1310
guanosine diphosphate
Guanosine Diphosphate: A guanine nucleotide containing two phosphate groups esterified to the sugar moiety.		3.1110guanosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate		Escherichia coli metabolite;
mouse metabolite;
uncoupling protein inhibitor
guanosine triphosphate
Guanosine Triphosphate: Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety.		3.4920guanosine 5'-phosphate;
purine ribonucleoside 5'-triphosphate		Escherichia coli metabolite;
mouse metabolite;
uncoupling protein inhibitor
folic acid
folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin.		3.0240folic acids;
N-acyl-amino acid		human metabolite;
mouse metabolite;
nutrient
3-methyladenine
N3-methyladenine: structure in first source		2.110
dacarbazine
(E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration.		2.0610dacarbazine
tirapazamine
Tirapazamine: A triazine derivative that introduces breaks into DNA strands in hypoxic cells, sensitizing tumor cells to the cytotoxic activity of other drugs and radiation.. tirapazamine : A member of the class of benzotriazines that is 1,2,4-benzotriazine carrying an amino substituent at position 3 and two oxido substituents at positions 1 and 4.		2.2110aromatic amine;
benzotriazines;
N-oxide		antibacterial agent;
antineoplastic agent;
apoptosis inducer
lometrexol
lometrexol: RN & structure given in first source;		3.110
dimethyl sulfoxide
Dimethyl Sulfoxide: A highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during CRYOPRESERVATION. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation.. dimethyl sulfoxide : A 2-carbon sulfoxide in which the sulfur atom has two methyl substituents.		2.0110sulfoxide;
volatile organic compound		alkylating agent;
antidote;
Escherichia coli metabolite;
geroprotector;
MRI contrast agent;
non-narcotic analgesic;
polar aprotic solvent;
radical scavenger
zopolrestat
zopolrestat: structure given in first source		3.2510
amsacrine
Amsacrine: An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent.. amsacrine : A sulfonamide that is N-phenylmethanesulfonamide substituted by a methoxy group at position 3 and an acridin-9-ylamino group at position 4. It exhibits antineoplastic activity.		2.1710acridines;
aromatic ether;
sulfonamide		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
verapamil
Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.		2.5820aromatic ether;
nitrile;
polyether;
tertiary amino compound
carbonyl cyanide m-chlorophenyl hydrazone
Carbonyl Cyanide m-Chlorophenyl Hydrazone: A proton ionophore. It is commonly used as an uncoupling agent and inhibitor of photosynthesis because of its effects on mitochondrial and chloroplast membranes.. CCCP : A member of the class of monochlorobenzenes that is benzene substituted by 2-(1,3-dinitrilopropan-2-ylidene)hydrazinyl and chloro groups at positions 1 and 3, respectively. It is a mitochondrial depolarizing agent that induces reactive oxygen species mediated cell death.		2.0810hydrazone;
monochlorobenzenes;
nitrile		antibacterial agent;
geroprotector;
ionophore
chlorambucil
Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia.		2.1310aromatic amine;
monocarboxylic acid;
nitrogen mustard;
organochlorine compound;
tertiary amino compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		2.1110aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
ciprofloxacin
Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.		2.1310aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic
clotrimazole
[no description available]		3.5110conazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes		antiinfective agent;
environmental contaminant;
xenobiotic
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		2.4110amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
diphenyleneiodonium
diphenyleneiodonium: structure in first source; NADPH oxidase inhibitor. dibenziodolium : An organic cation that is fluorene in which the methylene group is replaced by a positively charged iodine.		2.0810organic cation
valproic acid
Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.		3.4110branched-chain fatty acid;
branched-chain saturated fatty acid		anticonvulsant;
antimanic drug;
EC 3.5.1.98 (histone deacetylase) inhibitor;
GABA agent;
neuroprotective agent;
psychotropic drug;
teratogenic agent
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		4.7480nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
ibuprofen
Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine		3.2510monocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
radical scavenger;
xenobiotic
nocodazole
[no description available]		4.05130aromatic ketone;
benzimidazoles;
carbamate ester;
thiophenes		antimitotic;
antineoplastic agent;
microtubule-destabilising agent;
tubulin modulator
mitoxantrone
Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.		2.8220dihydroxyanthraquinoneanalgesic;
antineoplastic agent
entinostat
[no description available]		2.2110benzamides;
carbamate ester;
primary amino compound;
pyridines;
substituted aniline		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
myoseverin
myoseverin: a micotubule-binding molecule with cellular effects; structure in first source		2.2110
myristicin
myristicin: asaricin is an isomer; structure; a methylene dioxy version of elemicin;		2.0510organic molecular entitymetabolite
nevirapine
Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection.		2.0410cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
pentamidine
Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.		2.1110aromatic ether;
carboxamidine;
diether		anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
procaine
Procaine: A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016).. procaine : A benzoate ester, formally the result of esterification of 4-aminobenzoic acid with 2-diethylaminoethanol but formed experimentally by reaction of ethyl 4-aminobenzoate with 2-diethylaminoethanol.		2.1710benzoate ester;
substituted aniline;
tertiary amino compound		central nervous system depressant;
drug allergen;
local anaesthetic;
peripheral nervous system drug
propafenone
Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias.		2.4110aromatic ketone;
secondary alcohol;
secondary amino compound		anti-arrhythmia drug
propranolol
Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.		3.3660naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
raloxifene
raloxifene : A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively.		3.23101-benzothiophenes;
aromatic ketone;
N-oxyethylpiperidine;
phenols		bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
rolipram
[no description available]		2.3110pyrrolidin-2-onesantidepressant;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
scriptaid
scriptide: provokes translocation of GLUT4 to increase glucose uptake; structure in first source		2.4110isoquinolines
vorinostat
Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).		5.0190dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
sulfamethoxazole
Sulfamethoxazole: A bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. Its broad spectrum of activity has been limited by the development of resistance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p208). sulfamethoxazole : An isoxazole (1,2-oxazole) compound having a methyl substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 3-position.		3.5110isoxazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial agent;
antiinfective agent;
antimicrobial agent;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
epitope;
P450 inhibitor;
xenobiotic
temozolomide
[no description available]		2.3110imidazotetrazine;
monocarboxylic acid amide;
triazene derivative		alkylating agent;
antineoplastic agent;
prodrug
terfenadine
Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.		2.4920diarylmethane
thenoyltrifluoroacetone
Thenoyltrifluoroacetone: Chelating agent and inhibitor of cellular respiration.		3.2510
mitomycin
Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae.		3.8620mitomycinalkylating agent;
antineoplastic agent
vincristine
[no description available]		5.53200acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
colchicine
(S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.		7.691090alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
ampicillin
Ampicillin: Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.. ampicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-phenylacetamido group.		3.5110beta-lactam antibiotic;
penicillin allergen;
penicillin		antibacterial drug
2-aminobenzothiazole
[no description available]		2.0710benzothiazoles
kokusaginine
kokusaginine: antimalarial alkaloid from Teclea afzelii; structure in first source		2.1710organic heterotricyclic compound;
organonitrogen heterocyclic compound;
oxacycle
Dillapiole
5-allyl 6,7-dimethoxy 1,3-benzodioxole: a plant based insecticide; structure in first source		2.0510benzodioxolesmetabolite
podophyllotoxin
Podophyllum: A genus of poisonous American herbs, family BERBERIDACEAE. The roots yield PODOPHYLLOTOXIN and other pharmacologically important agents. The plant was formerly used as a cholagogue and cathartic. It is different from the European mandrake, MANDRAGORA.		5.83290furonaphthodioxole;
lignan;
organic heterotetracyclic compound		antimitotic;
antineoplastic agent;
keratolytic drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
apiole
apiole: crystalline essential oil isolated directly from commercial oil of parsley		2.0510benzodioxolesmetabolite
vinblastine
[no description available]		4.31180
desacetamidocolchicine
desacetamidocolchicine: structure given in first source		3.3510
thiocholchicine
thiocholchicine: RN refers to (S)-isomer		4.3660
n-methylcolchiceinamide, (s)-isomer
[no description available]		3.3510
colchicenamide
colchicenamide: RN given refers to (S)-isomer; structure given in first source		3.3510
n,n'-ethylenebis(iodoacetamide)
[no description available]		2.0610
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		4.450delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
parbendazole
parbendazole: anthelmintic used against a variety of gastrointestinal parasites; minor descriptor (75-86); on-line & INDEX MEDICUS search BENZIMIDAZOLES; RN given refers to parent cpd		2.4110benzimidazoles;
carbamate ester
daunorubicin
Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola.		2.0310aminoglycoside antibiotic;
anthracycline;
p-quinones;
tetracenequinones		antineoplastic agent;
bacterial metabolite
7-ethoxycoumarin
7-ethoxycoumarin : A member of the class of coumarins that is umbelliferone in which the hydroxy group at position 7 is replaced by an ethoxy group.		2.7830aromatic ether;
coumarins
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		6.131090taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
etoposide
[no description available]		5.79150beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound		antineoplastic agent;
DNA synthesis inhibitor
2-methoxy-5-(2',3',4'-trimethoxyphenyl)tropone
2-methoxy-5-(2',3',4'-trimethoxyphenyl)tropone: structure given in first source		2.0310
oltipraz
oltipraz : A 1,2-dithiole that is 3H-1,2-dithiole-3-thione substituted at positions 4 and 5 by methyl and pyrazin-2-yl groups respectively.		2.13101,2-dithiole;
pyrazines		angiogenesis modulating agent;
antimutagen;
antineoplastic agent;
antioxidant;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
neurotoxin;
protective agent;
schistosomicide drug
irinotecan
[no description available]		3.6420carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
capecitabine
Capecitabine: A deoxycytidine derivative and fluorouracil PRODRUG that is used as an ANTINEOPLASTIC ANTIMETABOLITE in the treatment of COLON CANCER; BREAST CANCER and GASTRIC CANCER.. capecitabine : A carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers.		2.2110carbamate ester;
cytidines;
organofluorine compound		antimetabolite;
antineoplastic agent;
prodrug
bendamustine
[no description available]		3.0730benzimidazoles
2-methoxyestradiol
2-methoxy-17beta-estradiol : A 17beta-hydroxy steroid, being 17beta-estradiol methoxylated at C-2.		34017beta-hydroxy steroid;
3-hydroxy steroid		angiogenesis modulating agent;
antimitotic;
antineoplastic agent;
human metabolite;
metabolite;
mouse metabolite
isoflavone
[no description available]		2.4110isoflavones
5-(biotinamido)pentylamine
[no description available]		2.2110
parthenolide
[no description available]		2.0810germacranolide
4'-demethylepipodophyllotoxin
4'-demethylepipodophyllotoxin: structure in first source. 4'-demethylepipodophyllotoxin : An organic heterotetracyclic compound that is the 9- epimer of 4'-demethylpodophyllotoxin.		2.3110furonaphthodioxole;
organic heterotetracyclic compound;
phenols		antineoplastic agent
imatinib mesylate
imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.		2.3110methanesulfonate saltanticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
gefitinib
[no description available]		2.1110aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
rb 6145
RB 6145: structure given in first source; prodrug to RSU 1069; PD 144872 is the R-enantiomer of RB 6145		2.2510
azatoxin
azatoxin: structure given in first source; a topoisomerase II inhibitor		2.1710
methotrexate
[no description available]		2.0510dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
estrone-3-o-sulfamate
estrone-3-O-sulfamate: a steroid sulfatase inhibitor		2.3110
combretastatin b-1
combretastatin B-1: structure in first source		2.420
gl 331
GL 331: structure in first source		3.3510
docetaxel
[no description available]		2.520hydrate;
secondary alpha-hydroxy ketone		antineoplastic agent
docetaxel anhydrous
Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.		2.1510secondary alpha-hydroxy ketone;
tetracyclic diterpenoid		antimalarial;
antineoplastic agent;
photosensitizing agent
2-phenyl-4-oxohydroquinoline
2-phenyl-4-oxohydroquinoline: structure given in first source		2.420
2'-hydroxyflavone
2'-hydroxyflavone: isolated from Daphnopsis sellowiana; structure given in first source		2.1710flavones
erlotinib
[no description available]		3.4160aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor
2'-hydroxyflavanone
[no description available]		2.1710
lapatinib
[no description available]		2.110furans;
organochlorine compound;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor
sorafenib
[no description available]		2.2110(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
demecolcine
Demecolcine: An alkaloid isolated from Colchicum autumnale L. and used as an antineoplastic.. (-)-demecolcine : A secondary amino compound that is (S)-colchicine in which the N-acetyl group is replaced by an N-methyl group. Isolable from the autumn crocus, Colchicum autumnale, it is less toxic than colchicine and is used as an antineoplastic.		2.4110alkaloid;
secondary amino compound		antineoplastic agent;
microtubule-destabilising agent
vincaleukoblastine
[no description available]		3.1140acetate ester;
indole alkaloid fundamental parent;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
immunosuppressive agent;
microtubule-destabilising agent;
plant metabolite
n-acetylcolchinol
N-acetylcolchinol: structure		3.3510
vincristine sulfate
[no description available]		2.0710organic sulfate saltantineoplastic agent;
geroprotector
noscapine
Noscapine: A naturally occurring opium alkaloid that is a centrally acting antitussive agent.. (-)-noscapine : A benzylisoquinoline alkaloid that is 1,2,3,4-tetrahydroisoquinoline which is substituted by a 4,5-dimethoxy-3-oxo-1,3-dihydro-2-benzofuran-1-yl group at position 1, a methylenedioxy group at positions 6-7 and a methoxy group at position 8. Obtained from plants of the Papaveraceae family, it lacks significant painkilling properties and is primarily used for its antitussive (cough-suppressing) effects.		2.110aromatic ether;
benzylisoquinoline alkaloid;
cyclic acetal;
isobenzofuranone;
organic heterobicyclic compound;
organic heterotricyclic compound;
tertiary amino compound		antineoplastic agent;
antitussive;
apoptosis inducer;
plant metabolite
anthricin
anthricin: antitumor constituent from Anthriscus sylvestris (L.) Hoffm; structure in first source. deoxypodophyllotoxin : A member of the class of furonaphthodioxoles that is (5R,5aR,8aR)-5,8,8a,9-tetrahydro-2H-furo[3',4':6,7]naphtho[2,3-d][1,3]dioxol-6(5aH)-one substituted at position 5 by a 3,4,5-trimethoxyphenyl group.		340furonaphthodioxole;
gamma-lactone;
lignan;
methoxybenzenes		antineoplastic agent;
apoptosis inducer;
plant metabolite
erianin
Erianin: from Dendrobium chrysotoxum; structure in first source		3.2460
(4-methoxyphenyl)(3,4,5-trimethoxyphenyl)methanone
(4-methoxyphenyl)(3,4,5-trimethoxyphenyl)methanone: a tubulin inhibitor with antineoplastic activity; structure in first source		2.730
5,3'-dihydroxy-3,6,7,8,4'-pentamethoxyflavone
5,3'-dihydroxy-3,6,7,8,4'-pentamethoxyflavone: an antineoplastic flavonol isolated from Polanisia dodecandra; structure given in first source		2.4320
adam ii
ADAM II: an alkenyldiarylmethane compound; structure in first source		2.0410
5f-203
2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole: structure in first source		2.1510
4-amino-5-benzoyl-2-(4-methoxyphenylamino)thiazole
4-amino-5-benzoyl-2-(4-methoxyphenylamino)thiazole: upregulates the DR5 receptor; structure in first source		2.0510
indoximod
[no description available]		2.2510
naringenin
(S)-naringenin : The (S)-enantiomer of naringenin.		3.2310(2S)-flavan-4-one;
naringenin		expectorant;
plant metabolite
tosylphenylalanyl chloromethyl ketone
Tosylphenylalanyl Chloromethyl Ketone: An inhibitor of Serine Endopeptidases. Acts as alkylating agent and is known to interfere with the translation process.. N-tosyl-L-phenylalanyl chloromethyl ketone : The N-tosyl derivative of L-phenylalanyl chloromethyl ketone.		3.2310alpha-chloroketone;
sulfonamide		alkylating agent;
serine proteinase inhibitor
taccalonolide a
taccalonolide A: has microtubule stabilizing activity; isolated from Tacca chantrieri; structure in first source		2.0810withanolide
doxorubicin hydrochloride
[no description available]		3.86100anthracycline
trichostatin a
trichostatin A: chelates zinc ion in the active site of histone deacetylases, resulting in preventing histone unpacking so DNA is less available for transcription; do not confuse with TRICHOSANTHIN which is a protein; found in STREPTOMYCES		4.0830antibiotic antifungal agent;
hydroxamic acid;
trichostatin		bacterial metabolite;
EC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector
resveratrol
trans-resveratrol : A resveratrol in which the double bond has E configuration.		3.1450resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
octreotide
[no description available]		2.1710
teniposide
[no description available]		3.3510aromatic ether;
beta-D-glucoside;
cyclic acetal;
furonaphthodioxole;
gamma-lactone;
monosaccharide derivative;
phenols;
thiophenes		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
melphalan
Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.		2.0610L-phenylalanine derivative;
nitrogen mustard;
non-proteinogenic L-alpha-amino acid;
organochlorine compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
shikonin
shikonin: a naphthazarin; has antineoplastic and angiogenesis inhibiting activities		2.2510hydroxy-1,4-naphthoquinone
4-phenylcoumarin
4-phenylcoumarin: structure given in first source. 4-phenylcoumarin : The simplest member of the class of neoflavones that is coumarin substituted by a phenyl group at position 4.		2.1510neoflavones
chalcone
trans-chalcone : The trans-isomer of chalcone.		2.5220chalconeEC 3.2.1.1 (alpha-amylase) inhibitor
piplartine
piplartine: Antineoplastic Agent, Phytogenic; alkaloid from Piper; structure in first source		2.5420cinnamamides;
dicarboximide
piperine
piperine : A N-acylpiperidine that is piperidine substituted by a (1E,3E)-1-(1,3-benzodioxol-5-yl)-5-oxopenta-1,3-dien-5-yl group at the nitrogen atom. It is an alkaloid isolated from the plant Piper nigrum.		2.1510benzodioxoles;
N-acylpiperidine;
piperidine alkaloid;
tertiary carboxamide		food component;
human blood serum metabolite;
NF-kappaB inhibitor;
plant metabolite
3,3',4,5'-tetrahydroxystilbene
3,3',4,5'-tetrahydroxystilbene: demethyl derivative of isorhapontigenin; structure in first source; a Syk kinase inhibitor; found in heartwood of FABACEAE; inhibitor of photosynthesis in spinach chloroplasts; may be inhibitor of plant growth; RN given refers to (E)-isomer. piceatannol : A stilbenol that is trans-stilbene in which one of the phenyl groups is substituted by hydroxy groups at positions 3 and 4, while the other phenyl group is substituted by hydroxy groups at positions 3 and 5.		210catechols;
polyphenol;
resorcinols;
stilbenol		antineoplastic agent;
apoptosis inducer;
geroprotector;
hypoglycemic agent;
plant metabolite;
protein kinase inhibitor;
tyrosine kinase inhibitor
3,4-methylenedioxy-beta-nitrostyrene
3,4-methylenedioxy-beta-nitrostyrene: tyrosine kinase inhibitor that prevents platelet glycoprotein IIb/IIIa activation; structure in first source		2.0510
1-(4-Methoxyphenyl)-2-nitroethylene
4-methoxy-beta-nitrostyrene: has vasodilator activity; structure in first source		2.0510methoxybenzenes
curcumin
Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.. curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.		2.6120aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol		anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger
cis-resveratrol
cis-resveratrol : The cis-stereoisomer of resveratrol.		2.9540resveratrol
tamoxifen
[no description available]		3.5820stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
brassinin
[no description available]		2.0810dithiocarbamic ester;
indole phytoalexin
e 7010
E 7010: inhibits tubulin polymerization; structure given in first source		4.5160sulfonamide
zd 6474
CH 331: structure in first source		2.110aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine		antineoplastic agent;
tyrosine kinase inhibitor
sodium butyrate
[no description available]		3.4110organic sodium saltEC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector
quercetin
[no description available]		2.41107-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
3-methylkaempferol
3-methylkaempferol: structure in first source. 3-methoxyapigenin : A trihydroxyflavone that is apigenin substituted by a methoxy group at position 3.		2.1110monomethoxyflavone;
trihydroxyflavone		plant metabolite
kaempferol
[no description available]		2.11107-hydroxyflavonol;
flavonols;
tetrahydroxyflavone		antibacterial agent;
geroprotector;
human blood serum metabolite;
human urinary metabolite;
human xenobiotic metabolite;
plant metabolite
amphotericin b
Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections.		2.1110antibiotic antifungal drug;
macrolide antibiotic;
polyene antibiotic		antiamoebic agent;
antiprotozoal drug;
bacterial metabolite
chrysin
chrysin : A dihydroxyflavone in which the two hydroxy groups are located at positions 5 and 7.		2.31107-hydroxyflavonol;
dihydroxyflavone		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
EC 2.7.11.18 (myosin-light-chain kinase) inhibitor;
hepatoprotective agent;
plant metabolite
santin
santin: from Tanacetum microphyllum; structure given in first source. santin : A trimethoxyflavone that is flavone substituted by methoxy groups at positions 3, 6 and 4' and hydroxy groups at positions 5 and 7 respectively.		2.1110dihydroxyflavone;
trimethoxyflavone		plant metabolite
polydatin
trans-piceid : A stilbenoid that is trans-resveratrol substituted at position 3 by a beta-D-glucosyl residue.		1.9910beta-D-glucoside;
monosaccharide derivative;
polyphenol;
stilbenoid		anti-arrhythmia drug;
antioxidant;
geroprotector;
hepatoprotective agent;
metabolite;
nephroprotective agent;
potassium channel modulator
pterostilbene
[no description available]		2.0110diether;
methoxybenzenes;
stilbenol		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
hypoglycemic agent;
neuroprotective agent;
neurotransmitter;
plant metabolite;
radical scavenger
cyclosporine
ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF		2.0610homodetic cyclic peptideanti-asthmatic drug;
anticoronaviral agent;
antifungal agent;
antirheumatic drug;
carcinogenic agent;
dermatologic drug;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
geroprotector;
immunosuppressive agent;
metabolite
vinorelbine
[no description available]		3.250acetate ester;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
ring assembly;
vinca alkaloid		antineoplastic agent;
photosensitizing agent
desoxyrhaponticin
[no description available]		1.9910glycoside;
stilbenoid
Kumatakenin
[no description available]		2.1110ether;
flavonoids
semaxinib
semaxanib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is replaced by a 3,5-dimethylpyrrol-2-yl group.		3.2250olefinic compound;
oxindoles;
pyrroles		angiogenesis modulating agent;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist
su 11248
[no description available]		3.6680monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
4',5,7-trihydroxy-3,6-dimethoxyflavone
viscosine: a GABA-A receptor agonist with anxiolytic and anticonvulsant activities; isolated from Dodonaea viscosa; structure in first source		2.1110
3,3',4,5'-tetramethoxy-trans-stilbene
(E)-3,4,3',5'-tetramethoxystilbene: from the leaves of Eugenia rigida; structure in first source		2.4120
3,4',5-trimethoxystilbene
3,4',5-trimethoxystilbene: structure in first source		2.9340
dmu-212
[no description available]		1.9710
1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene
[no description available]		3.3970
enalapril
Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).		2.3110dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug
vinblastine sulfate
[no description available]		2.0110
nsc 600032
combretastatin A-1: from Combretum caffrum; structure given in first source		4.23170
7-fluoro-2-phenyl-4-quinolone
7-fluoro-2-phenyl-4-quinolone: structure given in first source; interacts with tubulin and prevents colchicine binding to tubulin		1.9810
metochalcone
metochalcone: structure		2.0510
3',4',5',3,4,5-hexamethoxy-chalcone
[no description available]		2.0510
3,5-dihydroxy-4'-methoxystilbene
4'-methoxyresveratrol: has anti-inflammatory effects in cell culture model		2.420
psammaplin a
psammaplin A: isolated from marine sponges Poecillastra and Jaspis; structure in second source		3.4110
pironetin
pironetin: a microbial secondary metabolite having the activity of shortening plant height from Streptomyces sp.; structure in first source		2.110aliphatic alcohol
mdl 27048
MDL 27048: structure given in first source; powerful & reversible microtubule inhibitor		2.9940
combretastatin a3
combretastatin A3: RN given for (Z)-isomer; structure in first source		2.7430
axitinib
[no description available]		2.2510aryl sulfide;
benzamides;
indazoles;
pyridines		antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist
aurone
[no description available]		2.4110aurones;
cyclic ketone
combretastatin a-4 disodium phosphate
[no description available]		4.91330
ac 7700
AC 7700: a vascular disrupting agent; structure in first source		2.7630
hti-286
HTI-286: a synthetic analog of the tripeptide hemiasterlin; structure in first source		2.4420
ave-8063
AVE-8063: has both antivascular and antineoplastic activities; structure in first source		4.25170
2-methoxyestradiol-3,17-o,o-bis(sulfamate)
2-methoxyestradiol-3,17-O,O-bis(sulfamate): an antiangiogenic microtubule disruptor; antineoplastic agent; structure in first source		2.4720
dolastatin 10
dolastatin 10: from mollusk Dolabella auricularia; contains four amino acids, dolavaline, dolaisoleucine, dolaproine, valine and the primary amine dolaphenine; deo-dolastatin 10 is a new dolastatin 10 chiral derivative with MW of 784. dolastatin 10 : A tetrapeptide that is isolated from the sea hare Dolabella auricularia. It is a potent anticancer agent which inhibits tubulin polymerization.		2.02101,3-thiazoles;
tetrapeptide		animal metabolite;
antineoplastic agent;
apoptosis inducer;
marine metabolite;
microtubule-destabilising agent
2-meoemate
[no description available]		2.0510
3-hydroxy-4,3',4',5'-tetramethoxychalcone
3-hydroxy-4,3',4',5'-tetramethoxychalcone: structure in first source		3.82100
nsc 348103
[no description available]		2.4420
cediranib
[no description available]		2.1310aromatic ether
npi 2358
NPI 2358: antineoplastic; structure in first source. plinabulin : A member of the class of 2,5-diketopiperazines that is piperazine-2,5-dione substituted by benzylidene and (5-tert-butyl-1H-imidazol-4-yl)methylidene groups at positions 3 and 6, respectively. It is a vascular disrupting agent and a microtubule destabalising agent which was in clinical trials (now discontinued) for the treatment of non-small cell lung cancer.		2.48202,5-diketopiperazines;
benzenes;
imidazoles;
olefinic compound		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
microtubule-destabilising agent
blestriarene c
blestriarene C: structure in first source		2.0210
3,4-methylenedioxy-3',4',5'-trimethoxy chalcone
[no description available]		2.0510
3'-Hydroxy-5,7,4'-trimethoxy-4-phenylcoumarin
[no description available]		3.5920neoflavonoid
bpr0l075
[no description available]		3.360
(1,2-bis(1,2-benzisoselenazolone-3(2h)-ketone))ethane
(1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone))ethane: has antineoplastic activity; structure in first source		2.4110
calycopterin
calycopterin: an immunoinhibitory compound from the extract of Dracocephalum kotschyi; structure in first source		2.0610ether;
flavonoids
cis-3,4',5-trimethoxy-3'-aminostilbene
cis-3,4',5-trimethoxy-3'-aminostilbene: structure in first source		2.0510
5-Hydroxyauranetin
5-hydroxy-3,6,7,8,4'-pentamethoxyflavone: has diuretic activity; isolated from Rubus rosaefolius		2.0610ether;
flavonoids
verubulin
verubulin: antineoplastic; a small-molecule inhibitor of microtubule formation that is not a substrate for multidrug resistance pumps; structure in first source		2.6320
2-ethylestradiol sulfamate
2-ethyloestradiol-bis-sulfamate: structure in first source		2.0510
vindesine
[no description available]		2.0110
combretastatin a-2
combretastatin A-2: isolated from Combretum caffrum; RN from first source; structure given in first source		3.6590
tubulysin a
tubulysin A: has both antiangiogenic and antineoplastic activities; structure in first source		2.0410carboxylic acid;
diester
tubulysin d
tubulysin D: structure in first source		2.0410carboxylic acid;
diester
mdv 3100
[no description available]		2.1710(trifluoromethyl)benzenes;
benzamides;
imidazolidinone;
monofluorobenzenes;
nitrile;
thiocarbonyl compound		androgen antagonist;
antineoplastic agent
somatostatin
[no description available]		2.1710heterodetic cyclic peptide;
peptide hormone
crolibulin
crolibulin: a vascular disrupting agent with antineoplastic activity; structure in first source		2.1710neoflavonoid
pci 34051
PCI 34051: an HDAC8 inhibitor		2.4110indolecarboxamide
largazole
largazole: an antiproliferative agent from Symploca; structure in first source		3.4110
ponatinib
[no description available]		2.3110(trifluoromethyl)benzenes;
acetylenic compound;
benzamides;
imidazopyridazine;
N-methylpiperazine		antineoplastic agent;
tyrosine kinase inhibitor
isocombretastatin a-4
[no description available]		3.99120
(2-phenylthiazol-4-yl)-(3,4,5-trimethoxyphenyl)methanone
(2-phenylthiazol-4-yl)-(3,4,5-trimethoxyphenyl)methanone: a microtubule modulator; structure in first source		2.9130
isoerianin
[no description available]		3.250
3-(6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenol
3-(6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenol: inhibits ALK2 protein; structure in first source		2.2510
abi-274
ABI-274: a tubulin inhibitor; structure in first source		2.0510
2-ethylphenyl 4-(3-ethylureido)benzenesulfonate
2-ethylphenyl 4-(3-ethylureido)benzenesulfonate: has antineoplastic activity; structure in first source		2.0710
millepachine
millepachine: isolated from Millettia pachycarpa Benth (Leguminosae); structure in first source		2.1510
dacarbazine
(E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration.		2.0510dacarbazine
2-styrylquinazolin-4(3h)-one
2-styrylquinazolin-4(3H)-one: structure given in first source		210
tirapazamine
Tirapazamine: A triazine derivative that introduces breaks into DNA strands in hypoxic cells, sensitizing tumor cells to the cytotoxic activity of other drugs and radiation.. tirapazamine : A member of the class of benzotriazines that is 1,2,4-benzotriazine carrying an amino substituent at position 3 and two oxido substituents at positions 1 and 4.		2.2510aromatic amine;
benzotriazines;
N-oxide		antibacterial agent;
antineoplastic agent;
apoptosis inducer
2-(4-methoxyphenyl)-1H-quinazolin-4-one
[no description available]		210quinazolines
ConditionIndicatedRelationship StrengthStudiesTrials
Experimental Neoplasms
[description not available]		07.49440
Angiogenesis, Pathologic
[description not available]		013.42924
Cancer of Stomach
[description not available]		02.4920
Stomach Neoplasms
Tumors or cancer of the STOMACH.		02.4920
Benign Neoplasms
[description not available]		013.5612212
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		115.5612212
Experimental Hepatoma
[description not available]		03.5370
Glial Cell Tumors
[description not available]		03.78100
Glioma
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)		03.78100
Breast Cancer
[description not available]		06.72511
Breast Neoplasms
Tumors or cancer of the human BREAST.		06.72511
ER-Negative PR-Negative HER2-Negative Breast Cancer
[description not available]		02.6320
Triple Negative Breast Neoplasms
Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN.		02.6320
Local Neoplasm Recurrence
[description not available]		07.0153
Cancer of Lung
[description not available]		08.19322
Lung Neoplasms
Tumors or cancer of the LUNG.		08.19322
Cancer of Liver
[description not available]		04.89310
Liver Neoplasms
Tumors or cancer of the LIVER.		04.89310
Necrosis
The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.		07.07290
Cardiac Toxicity
[description not available]		05.0721
Cardiotoxicity
Damage to the HEART or its function secondary to exposure to toxic substances such as drugs used in CHEMOTHERAPY; IMMUNOTHERAPY; or RADIATION.		05.0721
Hepatocellular Carcinoma
[description not available]		04.33170
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		04.33170
Benign Neoplasms, Brain
[description not available]		03.2950
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		03.2950
Cancer of Cervix
[description not available]		03.0740
Uterine Cervical Neoplasms
Tumors or cancer of the UTERINE CERVIX.		03.0740
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		05.84340
Adenocarcinoma, Basal Cell
[description not available]		05.11101
Experimental Mammary Neoplasms
[description not available]		04.22170
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		05.11101
Cancer of Colon
[description not available]		04.64260
Cancer of Ovary
[description not available]		08.34155
Colonic Neoplasms
Tumors or cancer of the COLON.		04.64260
Ovarian Neoplasms
Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.		110.34155
Metastase
[description not available]		07.2881
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		07.2881
Epithelial Ovarian Cancer
[description not available]		04.5511
Carcinoma, Ovarian Epithelial
A malignant neoplasm that originates in cells on the surface EPITHELIUM of the ovary and is the most common form of ovarian cancer. There are five histologic subtypes: papillary serous, endometrioid, mucinous, clear cell, and transitional cell. Mutations in BRCA1, OPCML, PRKN, PIK3CA, AKT1, CTNNB1, RRAS2, and CDH1 genes are associated with this cancer.		04.5511
B16 Melanoma
[description not available]		04.85120
Anoxemia
[description not available]		03.6930
Hypoxia
Sub-optimal OXYGEN levels in the ambient air of living organisms.		03.6930
Diabetes Mellitus, Adult-Onset
[description not available]		05.8554
Germinoblastoma
[description not available]		04.441
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		05.8554
Lymphoma
A general term for various neoplastic diseases of the lymphoid tissue.		04.441
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		03.711
Colorectal Cancer
[description not available]		03.4470
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		03.4470
Cancer of Pancreas
[description not available]		03.1140
Pancreatic Neoplasms
Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).		03.1140
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		0340
Bone Cancer
[description not available]		02.7830
Osteogenic Sarcoma
[description not available]		02.8330
Bone Neoplasms
Tumors or cancer located in bone tissue or specific BONES.		02.7830
Osteosarcoma
A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)		02.8330
Carcinoma, Non-Small Cell Lung
[description not available]		06.92151
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		06.92151
Diarrhea
An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight.		02.4520
Nausea
An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.		05.0831
Anterior Cervical Pain
[description not available]		03.0610
Thyroid Cancer, Anaplastic
[description not available]		06.6861
Dysphagia
[description not available]		03.0610
Breathlessness
[description not available]		03.0610
Breathing Sounds
[description not available]		03.0610
Cancer of the Thyroid
[description not available]		09.05102
Hoarseness
An unnaturally deep or rough quality of voice.		03.0610
Deglutition Disorders
Difficulty in SWALLOWING which may result from neuromuscular disorder or mechanical obstruction. Dysphagia is classified into two distinct types: oropharyngeal dysphagia due to malfunction of the PHARYNX and UPPER ESOPHAGEAL SPHINCTER; and esophageal dysphagia due to malfunction of the ESOPHAGUS.		03.0610
Dyspnea
Difficult or labored breathing.		03.0610
Respiratory Sounds
Noises, normal and abnormal, heard on auscultation over any part of the RESPIRATORY TRACT.		03.0610
Thyroid Neoplasms
Tumors or cancer of the THYROID GLAND.		111.05102
Neck Pain
Discomfort or more intense forms of pain that are localized to the cervical region. This term generally refers to pain in the posterior or lateral regions of the neck.		03.0610
Thyroid Carcinoma, Anaplastic
An aggressive THYROID GLAND malignancy which generally occurs in IODINE-deficient areas in people with previous thyroid pathology such as GOITER. It is associated with CELL DEDIFFERENTIATION of THYROID CARCINOMA (e.g., FOLLICULAR THYROID CARCINOMA; PAPILLARY THYROID CANCER). Typical initial presentation is a rapidly growing neck mass which upon metastasis is associated with DYSPHAGIA; NECK PAIN; bone pain; DYSPNEA; and NEUROLOGIC DEFICITS.		06.6861
Cell Transformation, Neoplastic
Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.		02.5220
Canine Diseases
[description not available]		02.1710
HbS Disease
[description not available]		02.2110
Anemia, Sickle Cell
A disease characterized by chronic hemolytic anemia, episodic painful crises, and pathologic involvement of many organs. It is the clinical expression of homozygosity for hemoglobin S.		02.2110
Carcinoma, Lewis Lung
A carcinoma discovered by Dr. Margaret R. Lewis of the Wistar Institute in 1951. This tumor originated spontaneously as a carcinoma of the lung of a C57BL mouse. The tumor does not appear to be grossly hemorrhagic and the majority of the tumor tissue is a semifirm homogeneous mass. (From Cancer Chemother Rep 2 1972 Nov;(3)1:325) It is also called 3LL and LLC and is used as a transplantable malignancy.		02.4620
Cancer of Prostate
[description not available]		04.651
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		04.651
Neoplasms, Vascular
[description not available]		02.2110
Sarcoma 180
An experimental sarcoma of mice.		02.7630
Fibrosarcoma
A sarcoma derived from deep fibrous tissue, characterized by bundles of immature proliferating fibroblasts with variable collagen formation, which tends to invade locally and metastasize by the bloodstream. (Stedman, 25th ed)		03.1550
Dermatitis, Contact, Phototoxic
[description not available]		02.4920
Neutropenia
A decrease in the number of NEUTROPHILS found in the blood.		04.422
Endometrioma
An enlarged area of ENDOMETRIOSIS that resembles a tumor. It is usually found in the OVARY. When it is filled with old blood, it is known as a chocolate cyst.		02.4920
Endometriosis
A condition in which functional endometrial tissue is present outside the UTERUS. It is often confined to the PELVIS involving the OVARY, the ligaments, cul-de-sac, and the uterovesical peritoneum.		02.4920
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.4420
Carcinoma, Anaplastic
[description not available]		06.4391
Carcinoma
A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.		011.4391
Cells, Neoplasm Circulating
[description not available]		02.1110
Blood Pressure, High
[description not available]		04.821
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		04.821
Animal Mammary Carcinoma
[description not available]		02.9640
Neointima
The new and thickened layer of scar tissue that forms on a PROSTHESIS, or as a result of vessel injury especially following ANGIOPLASTY or stent placement.		02.1110
Nasopharyngeal Carcinoma
A carcinoma that originates in the EPITHELIUM of the NASOPHARYNX and includes four subtypes: keratinizing squamous cell, non-keratinizing, basaloid squamous cell, and PAPILLARY ADENOCARCINOMA. It is most prevalent in Southeast Asian populations and is associated with EPSTEIN-BARR VIRUS INFECTIONS. Somatic mutations associated with this cancer have been identified in NPCR, BAP1, UBAP1, ERBB2, ERBB3, MLL2, PIK3CA, KRAS, NRAS, and ARID1A genes.		02.1110
Cancer of Nasopharynx
[description not available]		02.4220
Nasopharyngeal Neoplasms
Tumors or cancer of the NASOPHARYNX.		02.4220
B-Cell Chronic Lymphocytic Leukemia
[description not available]		02.4520
Leukemia, Lymphocytic, Chronic, B-Cell
A chronic leukemia characterized by abnormal B-lymphocytes and often generalized lymphadenopathy. In patients presenting predominately with blood and bone marrow involvement it is called chronic lymphocytic leukemia (CLL); in those predominately with enlarged lymph nodes it is called small lymphocytic lymphoma. These terms represent spectrums of the same disease.		02.4520
Peritoneal Carcinomatosis
[description not available]		04.4311
Cancer of the Fallopian Tube
[description not available]		04.4311
Fallopian Tube Neoplasms
Benign or malignant neoplasms of the FALLOPIAN TUBES. They are uncommon. If they develop, they may be located in the wall or within the lumen as a growth attached to the wall by a stalk.		04.4311
Peritoneal Neoplasms
Tumors or cancer of the PERITONEUM.		04.4311
Multiple Chronic Conditions
Two or more concurrent chronic physical, mental, or behavioral health problems in an individual.		02.1310
Familial Nonmedullary Thyroid Cancer
[description not available]		02.1310
Carcinoma, Papillary
A malignant neoplasm characterized by the formation of numerous, irregular, finger-like projections of fibrous stroma that is covered with a surface layer of neoplastic epithelial cells. (Stedman, 25th ed)		02.1310
EHS Tumor
[description not available]		04.73110
Leukemia P388
An experimental lymphocytic leukemia originally induced in DBA/2 mice by painting with methylcholanthrene.		03.87120
Rhabdomyosarcoma
A malignant solid tumor arising from mesenchymal tissues which normally differentiate to form striated muscle. It can occur in a wide variety of sites. It is divided into four distinct types: pleomorphic, predominantly in male adults; alveolar (RHABDOMYOSARCOMA, ALVEOLAR), mainly in adolescents and young adults; embryonal (RHABDOMYOSARCOMA, EMBRYONAL), predominantly in infants and children; and botryoidal, also in young children. It is one of the most frequently occurring soft tissue sarcomas and the most common in children under 15. (From Dorland, 27th ed; Holland et al., Cancer Medicine, 3d ed, p2186; DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, pp1647-9)		04.81120
Ewing Sarcoma
[description not available]		02.0510
Sarcoma, Ewing
A malignant tumor of the bone which always arises in the medullary tissue, occurring more often in cylindrical bones. The tumor occurs usually before the age of 20, about twice as frequently in males as in females.		02.0510
Choroid Neovascularization
[description not available]		05.0431
Cancer of Gastrointestinal Tract
[description not available]		03.4311
Malignant Melanoma
[description not available]		05.65102
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		05.65102
Carcinoma, Oat Cell
[description not available]		04.0931
Ataxia
Impairment of the ability to perform smoothly coordinated voluntary movements. This condition may affect the limbs, trunk, eyes, pharynx, larynx, and other structures. Ataxia may result from impaired sensory or motor function. Sensory ataxia may result from posterior column injury or PERIPHERAL NERVE DISEASES. Motor ataxia may be associated with CEREBELLAR DISEASES; CEREBRAL CORTEX diseases; THALAMIC DISEASES; BASAL GANGLIA DISEASES; injury to the RED NUCLEUS; and other conditions.		03.4411
Cancer of Esophagus
[description not available]		03.4411
Esophageal Neoplasms
Tumors or cancer of the ESOPHAGUS.		03.4411
Carcinoma, Small Cell
An anaplastic, highly malignant, and usually bronchogenic carcinoma composed of small ovoid cells with scanty neoplasm. It is characterized by a dominant, deeply basophilic nucleus, and absent or indistinct nucleoli. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1286-7)		04.0931
Bladder Cancer
[description not available]		02.7330
Invasiveness, Neoplasm
[description not available]		02.4520
Urinary Bladder Neoplasms
Tumors or cancer of the URINARY BLADDER.		02.7330
Cancer, Embryonal
[description not available]		02.4620
Cancer of Testis
[description not available]		02.4620
Neoplasms, Germ Cell and Embryonal
Neoplasms composed of primordial GERM CELLS of embryonic GONADS or of elements of the germ layers of the EMBRYO, MAMMALIAN. The concept does not refer to neoplasms located in the gonads or present in an embryo or FETUS.		02.4620
Testicular Neoplasms
Tumors or cancer of the TESTIS. Germ cell tumors (GERMINOMA) of the testis constitute 95% of all testicular neoplasms.		02.4620
Sarcoma, Epithelioid
[description not available]		02.7330
Sarcoma
A connective tissue neoplasm formed by proliferation of mesodermal cells; it is usually highly malignant.		02.7330
Leukemia L 1210
[description not available]		03.3970
Astrocytoma, Grade IV
[description not available]		02.8330
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		02.8330
Carcinoma, Squamous Cell of Head and Neck
[description not available]		03.9421
Carcinoma, Epidermoid
[description not available]		03.8221
Cancer of Head
[description not available]		03.9421
Squamous Cell Carcinoma of Head and Neck
The most common type of head and neck carcinoma that originates from cells on the surface of the NASAL CAVITY; MOUTH; PARANASAL SINUSES, SALIVARY GLANDS, and LARYNX. Mutations in TNFRSF10B, PTEN, and ING1 genes are associated with this cancer.		03.9421
Carcinoma, Squamous Cell
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)		03.8221
Head and Neck Neoplasms
Soft tissue tumors or cancer arising from the mucosal surfaces of the LIP; oral cavity; PHARYNX; LARYNX; and cervical esophagus. Other sites included are the NOSE and PARANASAL SINUSES; SALIVARY GLANDS; THYROID GLAND and PARATHYROID GLANDS; and MELANOMA and non-melanoma skin cancers of the head and neck. (from Holland et al., Cancer Medicine, 4th ed, p1651)		03.9421
Hyperuricemia
Excessive URIC ACID or urate in blood as defined by its solubility in plasma at 37 degrees C; greater than 0.42mmol per liter (7.0mg/dL) in men or 0.36mmol per liter (6.0mg/dL) in women. This condition is caused by overproduction of uric acid or impaired renal clearance. Hyperuricemia can be acquired, drug-induced or genetically determined (LESCH-NYHAN SYNDROME). It is associated with HYPERTENSION and GOUT.		02.0710
Pyrexia
[description not available]		04.3911
Bilateral Headache
[description not available]		04.3911
Electrocardiogram QT Prolonged
[description not available]		04.3911
Age-Related Macular Degeneration
[description not available]		06.1421
Fever
An abnormal elevation of body temperature, usually as a result of a pathologic process.		04.3911
Headache
The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.		04.3911
Long QT Syndrome
A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.		04.3911
Macular Degeneration
Degenerative changes in the RETINA usually of older adults which results in a loss of vision in the center of the visual field (the MACULA LUTEA) because of damage to the retina. It occurs in dry and wet forms.		06.1421
Carcinosarcoma
A malignant neoplasm that contains elements of carcinoma and sarcoma so extensively intermixed as to indicate neoplasia of epithelial and mesenchymal tissue. (Stedman, 25th ed)		02.4120
Carcinoma, Adenosquamous
A mixed adenocarcinoma and squamous cell or epidermoid carcinoma.		02.0110
Soft Tissue Neoplasms
Neoplasms of whatever cell type or origin, occurring in the extraskeletal connective tissue framework of the body including the organs of locomotion and their various component structures, such as nerves, blood vessels, lymphatics, etc.		03.6330
Coronary Heart Disease
[description not available]		03.8121
Coronary Disease
An imbalance between myocardial functional requirements and the capacity of the CORONARY VESSELS to supply sufficient blood flow. It is a form of MYOCARDIAL ISCHEMIA (insufficient blood supply to the heart muscle) caused by a decreased capacity of the coronary vessels.		03.8121
Blood Clot
[description not available]		02.0110
Thrombosis
Formation and development of a thrombus or blood clot in the blood vessel.		02.0110
Cancer of the Retina
[description not available]		02.4320
Eye Cancer, Retinoblastoma
[description not available]		02.4320
Retinoblastoma
A malignant tumor arising from the nuclear layer of the retina that is the most common primary tumor of the eye in children. The tumor tends to occur in early childhood or infancy and may be present at birth. The majority are sporadic, but the condition may be transmitted as an autosomal dominant trait. Histologic features include dense cellularity, small round polygonal cells, and areas of calcification and necrosis. An abnormal pupil reflex (leukokoria); NYSTAGMUS, PATHOLOGIC; STRABISMUS; and visual loss represent common clinical characteristics of this condition. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, p2104)		02.4320
Thrombopenia
[description not available]		03.4111
Emesis
[description not available]		03.4111
Thrombocytopenia
A subnormal level of BLOOD PLATELETS.		03.4111
Vomiting
The forcible expulsion of the contents of the STOMACH through the MOUTH.		03.4111
Aging
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.		03.8610
Leucocythaemia
[description not available]		03.1450
Leukemia
A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)		03.1450
Neuroblastoma
A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)		02.7230
Adenocarcinoma Of Kidney
[description not available]		02.0310
Cancer of Kidney
[description not available]		02.0310
Carcinoma, Renal Cell
A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.		02.0310
Kidney Neoplasms
Tumors or cancers of the KIDNEY.		02.0310
Cardiac Diseases
[description not available]		02.9410
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		02.9410
Heart Diseases
Pathological conditions involving the HEART including its structural and functional abnormalities.		02.9410
Ischemia
A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION.		02.0310
Neovascularization, Optic Disc
[description not available]		02.0310
Aphakia
Absence of crystalline lens totally or partially from field of vision, from any cause except after cataract extraction. Aphakia is mainly congenital or as result of LENS DISLOCATION AND SUBLUXATION.		02.0310
Diabetic Retinopathy
Disease of the RETINA as a complication of DIABETES MELLITUS. It is characterized by the progressive microvascular complications, such as ANEURYSM, interretinal EDEMA, and intraocular PATHOLOGIC NEOVASCULARIZATION.		02.0310
Intraocular Pressure
The pressure of the fluids in the eye.		02.0310
Retinal Neovascularization
Formation of new blood vessels originating from the retinal veins and extending along the inner (vitreal) surface of the retina.		02.0310
Acute Myelogenous Leukemia
[description not available]		02.0410
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		02.0410
Lymph Node Metastasis
[description not available]		0210
B-Cell Lymphoma
[description not available]		02.4620
Lymphoma, B-Cell
A group of heterogeneous lymphoid tumors generally expressing one or more B-cell antigens or representing malignant transformations of B-lymphocytes.		02.4620
Endothelioma, Vascular
[description not available]		0210
Hemangioendothelioma
A neoplasm derived from blood vessels, characterized by numerous prominent endothelial cells that occur singly, in aggregates, and as the lining of congeries of vascular tubes or channels. Hemangioendotheliomas are relatively rare and are of intermediate malignancy (between benign hemangiomas and conventional angiosarcomas). They affect men and women about equally and rarely develop in childhood. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1866)		0210
Clostridioides difficile Infection
[description not available]		0210
Clostridium Infections
Infections with bacteria of the genus CLOSTRIDIUM and closely related CLOSTRIDIOIDES species.		0210
Diffuse Mixed Small and Large Cell Lymphoma
[description not available]		0210
Lymphoma, Non-Hodgkin
Any of a group of malignant tumors of lymphoid tissue that differ from HODGKIN DISEASE, being more heterogeneous with respect to malignant cell lineage, clinical course, prognosis, and therapy. The only common feature among these tumors is the absence of giant REED-STERNBERG CELLS, a characteristic of Hodgkin's disease.		0210
Cancer of Skin
[description not available]		0210
Skin Neoplasms
Tumors or cancer of the SKIN.		0210
Retinal Diseases
Diseases involving the RETINA.		02.0110
Diffuse Large B-Cell Lymphoma
[description not available]		02.4120
Lymphoma, Large B-Cell, Diffuse
Malignant lymphoma composed of large B lymphoid cells whose nuclear size can exceed normal macrophage nuclei, or more than twice the size of a normal lymphocyte. The pattern is predominantly diffuse. Most of these lymphomas represent the malignant counterpart of B-lymphocytes at midstage in the process of differentiation.		02.4120
Kaposi Sarcoma
[description not available]		02.4120
Sarcoma, Kaposi
A multicentric, malignant neoplastic vascular proliferation characterized by the development of bluish-red cutaneous nodules, usually on the lower extremities, most often on the toes or feet, and slowly increasing in size and number and spreading to more proximal areas. The tumors have endothelium-lined channels and vascular spaces admixed with variably sized aggregates of spindle-shaped cells, and often remain confined to the skin and subcutaneous tissue, but widespread visceral involvement may occur. Kaposi's sarcoma occurs spontaneously in Jewish and Italian males in Europe and the United States. An aggressive variant in young children is endemic in some areas of Africa. A third form occurs in about 0.04% of kidney transplant patients. There is also a high incidence in AIDS patients. (From Dorland, 27th ed & Holland et al., Cancer Medicine, 3d ed, pp2105-7) HHV-8 is the suspected cause.		02.4120
Acquired Immune Deficiency Syndrome
[description not available]		02.0110
Acquired Immunodeficiency Syndrome
An acquired defect of cellular immunity associated with infection by the human immunodeficiency virus (HIV), a CD4-positive T-lymphocyte count under 200 cells/microliter or less than 14% of total lymphocytes, and increased susceptibility to opportunistic infections and malignant neoplasms. Clinical manifestations also include emaciation (wasting) and dementia. These elements reflect criteria for AIDS as defined by the CDC in 1993.		02.0110
Central Nervous System Neoplasm
[description not available]		01.9810
Central Nervous System Neoplasms
Benign and malignant neoplastic processes that arise from or secondarily involve the brain, spinal cord, or meninges.		01.9810
Cancer of Intestines
[description not available]		01.9810
Intestinal Neoplasms
Tumors or cancer of the INTESTINES.		01.9810
HIV Coinfection
[description not available]		0210
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		0210
Cancer of Duodenum
[description not available]		02.0710
Disease
A definite pathologic process with a characteristic set of signs and symptoms. It may affect the whole body or any of its parts, and its etiology, pathology, and prognosis may be known or unknown.		03.0610
Adenocarcinoma, Endometrioid
[description not available]		02.2110
Carcinoma, Endometrioid
An adenocarcinoma characterized by the presence of cells resembling the glandular cells of the ENDOMETRIUM. It is a common histological type of ovarian CARCINOMA and ENDOMETRIAL CARCINOMA. There is a high frequency of co-occurrence of this form of adenocarcinoma in both tissues.		02.2110
Granulocytic Leukemia, Chronic
[description not available]		02.3110
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Clonal hematopoetic disorder caused by an acquired genetic defect in PLURIPOTENT STEM CELLS. It starts in MYELOID CELLS of the bone marrow, invades the blood and then other organs. The condition progresses from a stable, more indolent, chronic phase (LEUKEMIA, MYELOID, CHRONIC PHASE) lasting up to 7 years, to an advanced phase composed of an accelerated phase (LEUKEMIA, MYELOID, ACCELERATED PHASE) and BLAST CRISIS.		02.3110