Colchicine is a natural alkaloid extracted from the autumn crocus (Colchicum autumnale). It has been used for centuries in traditional medicine for various ailments, including gout. Colchicine inhibits microtubule polymerization, a process essential for cell division and other cellular functions. This property makes colchicine a potent anti-inflammatory agent, particularly effective in treating acute gout attacks. Colchicine is also used in research to study microtubule dynamics and its role in various cellular processes. Its unique ability to interfere with microtubule assembly makes it a valuable tool for investigating cell division, migration, and other cellular functions. While colchicine has been used for centuries, research continues to explore its potential therapeutic uses and its effects on different cellular pathways.'
(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. [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]
| Flora | Rank | Flora Definition | Family | Family Definition |
|---|---|---|---|---|
| Colchicum | genus | A genus of poisonous, liliaceous plants. The roots (corms) of Colchicum autumnale, the fall crocus or meadow saffron, yield COLCHICINE, which is used as a biochemical tool and to treat gout. Other members of this genus yield saffron dye, flavoring agents, and aromatics.[MeSH] | Colchicaceae | A family in the order Liliales.[MeSH] |
| Colchicum autumnale | species | Colchicum autumnale L. is the source of COLCHICINE.[MeSH] | Colchicaceae | A family in the order Liliales.[MeSH] |
| ID Source | ID |
|---|---|
| PubMed CID | 6167 |
| CHEMBL ID | 107 |
| CHEBI ID | 27882 |
| SCHEMBL ID | 8469 |
| MeSH ID | M0004732 |
| Synonym |
|---|
| MLS002153786 |
| BRD-K00259736-001-06-5 |
| MLS001055448-02 |
| xd25 |
| gtpl2367 |
| n-[(7s)-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5h-benzo[d]heptalen-7-yl]acetamide |
| DIVK1C_000753 |
| KBIO1_000753 |
| NCI60_041659 |
| mpc-004 |
| colstat |
| SDCCGMLS-0066633.P001 |
| colcrys |
| (s)-n-(5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo[a]heptalen-7-yl)acetamide |
| n-[(7s)-5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo[a]heptalen-7-yl]acetamide |
| EU-0100310 |
| colchicine, >=95% (hplc), powder |
| SPECTRUM_000842 |
| ACON1_000353 |
| MEGXP0_001879 |
| binds to tubulin; inhibits microtubular assembly |
| spindle poison |
| PRESTWICK_695 |
| NCGC00025125-01 |
| tocris-1364 |
| PRESTWICK3_000363 |
| IDI1_000753 |
| BSPBIO_002083 |
| BSPBIO_000485 |
| LOPAC0_000310 |
| SPECTRUM5_000787 |
| goutnil |
| colchicinum |
| CHEBI:27882 , |
| mitigare |
| (-)-colchicine |
| kolkicin |
| n-(5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo[.alpha.]heptalen-7-yl)-acetamide |
| n-[(7s)-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5h-benzo[a]heptalen-7-yl]acetamide |
| NCGC00025125-03 |
| NCGC00025125-02 |
| UPCMLD-DP065:001 |
| smr000058323 |
| MLS001055448 |
| n-(5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(a)heptalen-7-yl)acetamide |
| acetamide, n-((7s)-5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(a)heptalen-7-yl)- |
| ccris 691 |
| 7-alpha-h-colchicine |
| colchicine [jan] |
| acetamide, n-(5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(a)heptalen-7-yl)-, (s)- |
| benzo(a)heptalen-9(5h)-one, 7-acetamido-6,7-dihydro-1,2,3,10-tetramethoxy- |
| 7alphah-colchicine |
| ai3-31149 |
| colchicin [german] |
| einecs 200-598-5 |
| colchicina [italian] |
| hsdb 3044 |
| 7.alpha.h-colchicine |
| colchisol |
| wln: l b677 mv&t&j co1 do1 eo1 jmv1 no1 |
| nsc 757 |
| colsaloid |
| nsc757 , |
| 64-86-8 |
| condylon |
| colcin |
| colchicina |
| n-acetyl trimethylcolchicinic acid methylether |
| colchineos |
| colchicine , |
| acetamide,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(.alpha.)heptalen-7-yl)- |
| acetamide,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo[.alpha.]heptalen-7-yl)- |
| colchicin |
| C07592 |
| benzo[a]heptalen-9(5h)-one,7-dihydro-1,2,3,10-tetramethoxy- |
| nsc-757 |
| colchicine, bioreagent, plant cell culture tested, >=95% (hplc) |
| UPCMLD-DP065 |
| D00570 |
| colchicine (jp17/usp) |
| colchicine (tn) |
| BPBIO1_000535 |
| NCGC00025125-07 |
| NCGC00025125-05 |
| KBIO2_001322 |
| KBIOSS_001322 |
| KBIO2_006458 |
| KBIO3_001303 |
| KBIO2_003890 |
| KBIOGR_000856 |
| SPBIO_000289 |
| SPECTRUM2_000075 |
| NINDS_000753 |
| SPECTRUM4_000298 |
| PRESTWICK1_000363 |
| SPECTRUM3_000362 |
| SPBIO_002406 |
| PRESTWICK0_000363 |
| SPECTRUM1500205 |
| n-((7s)-5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(a)heptalen-7-yl)- acetamide |
| PRESTWICK2_000363 |
| NCGC00025125-06 |
| NCGC00169157-01 |
| NCGC00169157-02 |
| NCGC00025125-04 |
| MLS001304089 |
| NCGC00169157-03 |
| n-[(7s)-1,2,3,10-tetramethoxy-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide |
| n-[(7s)-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5h-benzo[d]heptalen-7-yl]ethanamide |
| LOC , |
| (s)-colchicine |
| (s)-colchicina |
| (s)-colchicin |
| C 9754 , |
| HMS2091G16 |
| NCGC00025125-11 |
| DB08117 |
| CHEMBL107 , |
| colchcine |
| HMS502F15 |
| HMS1569I07 |
| HMS1920A08 |
| bdbm50014846 |
| AKOS001582887 |
| NCGC00025125-14 |
| NCGC00025125-09 |
| NCGC00025125-12 |
| NCGC00025125-13 |
| NCGC00025125-10 |
| NCGC00025125-15 |
| NCGC00025125-08 |
| HMS2096I07 |
| HMS3260N22 |
| ec 200-598-5 |
| sml2y3j35t , |
| colchicine [usp:jan] |
| colchysat |
| unii-sml2y3j35t |
| NCGC00254359-01 |
| tox21_300582 |
| tox21_201547 |
| NCGC00259096-01 |
| pharmakon1600-01500205 |
| nsc-756702 |
| nsc756702 |
| dtxcid204845 |
| tox21_110947 |
| dtxsid5024845 , |
| HMS2231C05 |
| CCG-39910 |
| HY-16569 |
| CS-1141 |
| FT-0603187 |
| NCGC00025125-20 |
| LP00310 |
| colchicine [mi] |
| colchicinum [hpus] |
| colchicine [usp monograph] |
| colchicine [ep monograph] |
| col-probenecid component colchicine |
| colchicine component of mitigare |
| colchicine component of colbenemid |
| colchicine [who-dd] |
| colchicine [ep impurity] |
| colchicine [who-ip] |
| lodoco |
| colchicine component of proben-c |
| colbenemid component colchicine |
| acetamide, n-(5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(a)heptalen-7-yl)-,(s)- |
| colchicine [usp-rs] |
| colchicine [hsdb] |
| proben-c component colchicine |
| mitigare component colchicine |
| (s)-n-(5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(a)heptalen-7-yl)acetamide |
| gloperba |
| colchcine [vandf] |
| colchicine [orange book] |
| colchicine component of col-probenecid |
| colchicinum [who-ip latin] |
| colchicine [mart.] |
| S2284 |
| SCHEMBL8469 |
| tox21_110947_1 |
| NCGC00025125-18 |
| C-7100 |
| NCGC00260995-01 |
| tox21_500310 |
| acetamide, n-[(7s)-5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo[a]heptalen-7-yl]- |
| mfcd00078484 |
| colchicine (contains 5% ethyl acetate at maximum) |
| 4O2B |
| 4LZR |
| colchicine, (european pharmacopoeia (ep) reference standard) |
| M01514 |
| SR-01000597576-1 |
| SR-01000597576-3 |
| sr-01000597576 |
| colchicine, >=96.0% (hplc) |
| colchicine, united states pharmacopeia (usp) reference standard |
| colchicine for system suitability, european pharmacopoeia (ep) reference standard |
| colchicine, pharmaceutical secondary standard; certified reference material |
| colchicine; thiocolchicoside impurity a |
| SR-01000075794-1 |
| SR-01000075794-6 |
| SR-01000075794-3 |
| SR-01000075794-7 |
| sr-01000075794 |
| SBI-0050298.P004 |
| 30512-31-3 |
| HMS3713I07 |
| 7alpha-h-colchicine |
| nsc-813203 |
| nsc813203 |
| AS-13686 |
| BRD-K00259736-001-10-7 |
| SDCCGSBI-0050298.P006 |
| NCGC00025125-33 |
| (1e)-n-[(7s)-1,2,3,10-tetramethoxy-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl] ethanimidic acid |
| colchicine (ep monograph) |
| colchicine tablets 0.5 mg |
| n-acetyltrimethylcolchicinic acid methyl ether |
| n-((7s)-5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo |
| colchicine (usp monograph) |
| 7-acetamido-6,7-dihydro-1,2,3,10-tetramethoxy-benzo(a)heptalen-9(5h)-one |
| colchicenos |
| colchicine (usp-rs) |
| n-((7s)-1,2,3,10-tetramethoxy-9-oxo-5,6,7,9-tetrahydrobenzo(a)heptalen-7-yl)acetamide |
| colchicine (usp:jan) |
| n-acetyl trimethylcolchicinic acid, methyl ether |
| colcigel |
| acetamide, n-(5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(a)heptalen-7-yl) |
| 7-acetamido-6,7-dihydro-1,2,3,10-tetramethoxybenzo(a)heptalen-9(5h)-one |
| n-(5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(alpha)heptalen-7-yl)-acetamide |
| n-(5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenzo(a)heptalen-7-yl)-acetamide |
| colchiceine methyl ether |
| n-((7s)-(1,2,3,10-tetramethoxy-9-oxo-5,6,7,9-tetrahydrobenzo(a)heptalen-7-yl))acetamide |
| colchicine (ep impurity) |
| benzo(a)heptalene, acetamide deriv. |
| (-)-n- |
| n-((7s)-5,6,7,9-tetrahydro-1,2,3,10-tetramethoxy-9-oxobenz(a)heptalen-7-yl)-acetamide |
| colchicine (mart.) |
| colchicinum 4x |
| 7JX9WZ3SJ5 |
| colchicine conformational isomer |
| n-[(7s,12ap)-1,2,3,10-tetramethoxy-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide |
| colchicine impurity b [ep impurity] |
Colchicine is a plant alkaloid with a broad spectrum of biological and pharmacological properties. It is an effective anti-inflammatory agent used to treat gout, coronary artery disease, viral pericarditis, and familial Mediterranean fever.
Colchicine poisoning has a high risk of mortality, and death can be seen in doses less than a single acute dose of 0.5 mg/kg. It has a good binding affinity with MMP-9, NOX2 and TGF-β1 based on the value of -8.3 Kcal/mol.
Colchicine has broad anti-inflammatory effects and part of the atheroprotective effects have been suggested to be the result of NLRP3 inflammasome inhibition. The potential in reducing patient morbidity and mortality in COVID-19 infection owing to its anti- inflammatory properties.
Colchicine had a lower pooled RR of ischemic stroke (0.28, 95% CI 0.12-0.65, P = 0.003) for patients with acute compared with chronic CAD. It did not increase the incidence of infections (OR 1.42; 95%CI 0.82-2.46, p’=”0.22), pneumonia (or 1.55; 95 % CI 0.58-4.18, p″=0.39), cancers (or 0.98; 95°C 0.79-1.22, püs: “0.80) or bleeding. Coadministration with other myotoxic drugs may increase the risk of myopathy and rhabdomyolysis.
In colchicine-treated cats, the pattern of CGRP-containing fibers was basically unchanged, despite a reduction of both the number of fibers and the intensity of fiber staining. In CCl4-cirrhotic animals, treatment with Co reduced DBH activity to control levels. Colchicined animals showed intense staining in the external layer of the median eminence.
There are no data with regards to safe dosing schedule of colchicine in hemodialysis patients. Its chemical structure consists of col chicine, a sugar (ose) and a sulphur-containing radical (thio), and its adverse effects are therefore likely to be similar to those of colChicine.
Two Phase I studies assessed the effects of multiple daily consumptions of Seville orange juice or grapefruit juice on the pharmacokinetic properties of colchicine in healthy volunteers. The concomitant use of HP501, febuxostat, and col chicine did not produce clinically meaningful DDIs.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The half-life was 57." | ( Colchicine clearance is impaired in alcoholic cirrhosis. Bay, MK; Leighton, JA; Maldonado, AL; Schenker, S; Speeg, KV, 1991) | 1.72 |
| "kg, a half-life of 16." | ( The effect of liver dysfunction on colchicine pharmacokinetics in the rat. Bay, MK; Johnson, RF; Leighton, JA; Maldonado, AL; Schenker, S; Speeg, KV, 1990) | 0.56 |
| " Pharmacokinetic parameters t1/2 beta, AUC, MRT, CIT/F, CIR, Vd area/F) were calculated by model-independent methods and compared across doses by multiway analysis of variance." | ( Model-independent pharmacokinetics of colchicine after oral administration to healthy volunteers. Crouzette, J; Fournier, PE; Girre, C; Scherrmann, JM; Thomas, G, 1989) | 0.55 |
| " Recently, using a specific and sensitive radioimmunoassay, the investigation of plasma concentrations during single and multiple dose studies has allowed to define the colchicine pharmacokinetic parameters." | ( [Colchicine: recent data on pharmacokinetics and clinical pharmacology]. Chappey, O; Scherrmann, JM, 1995) | 1.4 |
| "8 L/hr, and the terminal half-life (t1/2) was 57." | ( Oral absorption characteristics and pharmacokinetics of colchicine in healthy volunteers after single and multiple doses. Ferron, GM; Jusko, WJ; Rochdi, M; Scherrmann, JM, 1996) | 0.54 |
| "The comparative pharmacokinetic and bioavailability profile of two different formulations (tablets and capsules) of thiocolchicoside was investigated in 8 healthy male volunteers after administration of single oral 8 mg doses." | ( Comparative pharmacokinetics and bioavailability of two oral formulations of thiocolchicoside, a GABA-mimetic muscle relaxant drug, in normal volunteers. Perucca, E; Pifferi, G; Poitou, P, ) | 0.13 |
| " The use of microdialysis for pharmacokinetic studies was validated by comparing the blood concentrations of colchicine obtained by microdialysis with those obtained by direct blood sampling." | ( Effect of the P-glycoprotein inhibitor, SDZ PSC 833, on the blood and brain pharmacokinetics of colchicine. Desrayaud, S; Guntz, P; Lemaire, M; Scherrmann, JM, 1997) | 0.73 |
| " The pharmacokinetic parameters between the first and the last days were compared using Student's t-test." | ( Single- and repeated-dose pharmacokinetics of intramuscular thiocolchicoside in healthy volunteers. Debray, M; Sandouk, P; Scherrmann, JM; Weinling, E, 1999) | 0.3 |
| "Thiocolchicoside pharmacokinetic parameters, calculated after the single dose using non-compartmental analysis, were in good agreement with those obtained in previous studies." | ( Single- and repeated-dose pharmacokinetics of intramuscular thiocolchicoside in healthy volunteers. Debray, M; Sandouk, P; Scherrmann, JM; Weinling, E, 1999) | 0.3 |
| " Therefore, our results indicate that the most likely reasons for the changed pharmacokinetic behaviour of colchicine in the presence of Solutol HS 15 are alterations of metabolism and/or transport as well as distribution and elimination processes." | ( Impact of Solutol HS 15 on the pharmacokinetic behaviour of colchicine upon intravenous administration to male Wistar rats. Bittner, B; González, RC; Huwyler, J; Kapps, M; Walter, I, 2003) | 0.77 |
| " A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals." | ( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004) | 0.32 |
| "To identify the ethnic, clinical, genetic, and pharmacokinetic correlates of colchicine treatment failure in patients with familial Mediterranean fever (FMF)." | ( Colchicine nonresponsiveness in familial Mediterranean fever: clinical, genetic, pharmacokinetic, and socioeconomic characterization. Chetrit, A; Gershoni-Baruch, R; Langevitz, P; Lidar, M; Livneh, A; Niel, E; Scherrmann, JM; Shinar, Y, 2004) | 2 |
| "Thiocolchicoside (TCC) has been prescribed for several years as a muscle relaxant drug, but its pharmacokinetic (PK) profile and metabolism still remain largely unknown." | ( New metabolic and pharmacokinetic characteristics of thiocolchicoside and its active metabolite in healthy humans. Adam, R; Dubruc, C; Filali-Ansary, A; Françon, D; Lluel, P; Thénot, JP; Trellu, M, 2004) | 0.32 |
| " pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data." | ( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Lombardo, F; Obach, RS; Waters, NJ, 2008) | 0.35 |
| "Two Phase I studies assessed the effects of multiple daily consumptions of Seville orange juice or grapefruit juice on the pharmacokinetic properties of colchicine in healthy volunteers." | ( Effects of grapefruit and Seville orange juices on the pharmacokinetic properties of colchicine in healthy subjects. Davis, MW; DiGiacinto, JL; Wason, S, 2012) | 0.8 |
| " Although it is considered to be a moderate concentration-dependent CYP3A4 inhibitor, grapefruit juice did not significantly affect the pharmacokinetic parameters of colchicine." | ( Effects of grapefruit and Seville orange juices on the pharmacokinetic properties of colchicine in healthy subjects. Davis, MW; DiGiacinto, JL; Wason, S, 2012) | 0.8 |
| "We have developed a new series of immunosuppressant with improved pharmacokinetic properties as the second-generation of colchicine analogs, which were designed based on the privileged structure derived from our previous work." | ( Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties. Chang, DJ; Jang, J; Kim, SO; Kim, WJ; Lee, S; Suh, YG, 2012) | 0.88 |
| "2 mg/day [from 16 to less than 65 years]), the observed steady-state pharmacokinetic parameters were comparable across age groups, despite the higher doses of colchicine on a mg/kg/day basis in the younger age groups." | ( Pharmacokinetics of colchicine in pediatric and adult patients with familial Mediterranean fever. Ben-Chetrit, E; Berkun, Y; Brik, R; Butbul, Y; Davis, MW; Faulkner, R; Hashkes, PJ; Livneh, A; Ozdogan, H; Ozen, S; Wason, S, ) | 0.65 |
| " Open-label pharmacokinetic studies were performed in volunteers or subjects with hyperuricemia (serum uric acid ≥ 8 mg/dL) to investigate interactions of lesinurad (with and without concurrent XOIs) with colchicine and 2 nonsteroidal anti-inflammatory drugs: naproxen and indomethacin." | ( Evaluation of Pharmacokinetic Interactions Between Lesinurad, a New Selective Urate Reabsorption Inhibitor, and Commonly Used Drugs for Gout Treatment. Bucci, G; Gillen, M; Kerr, B; Lee, C; Shen, Z; Tieu, K; Wilson, D, 2017) | 0.64 |
| " This concise paper attempts to give a brief review of its pharmacokinetic properties and its main mechanisms of action." | ( Colchicine Pharmacokinetics and Mechanism of Action. Angelidis, C; Giannopoulos, G; Kekeris, V; Kolokathis, F; Kossyvakis, C; Kotsialou, Z; Vrettou, AR; Zacharoulis, A, 2018) | 1.92 |
| " Therefore, the present study attempts to evaluate the pharmacokinetic and pharmacodynamic properties of nasal liposomal and PLGA nanoparticle formulations of rivastigmine in acute scopolamine-induced amnesia and chronic colchicine induced cognitive dysfunction animal models, and validate the best formulation by employing pharmacokinetic and pharmacodynamic (PK-PD) modeling." | ( Pharmacokinetic and pharmacodynamic evaluation of nasal liposome and nanoparticle based rivastigmine formulations in acute and chronic models of Alzheimer's disease. Arumugam, K; Bojja, SL; Kumar, N; Rao, CM; Rompicherla, SKL, 2021) | 0.81 |
| " The primary aim of the present study was to study the pharmacokinetic drug‒drug interactions (DDIs) of HP501, febuxostat, and colchicine in hyperuricemic patients." | ( A Phase I Study to Evaluate the Pharmacokinetic Drug‒Drug Interaction of HP501, Febuxostat, and Colchicine in Male Chinese Patients with Hyperuricemia. Chen, H; Chen, L; Ding, R; Hu, X; Jiang, F; Li, X; Li, Y; Liu, K; Peng, Q; Wu, J; Xiong, T; Zhou, Y, 2023) | 1.33 |
| " Coadministration of HP501 and febuxostat did not significantly change the pharmacokinetic profiles of either drug." | ( A Phase I Study to Evaluate the Pharmacokinetic Drug‒Drug Interaction of HP501, Febuxostat, and Colchicine in Male Chinese Patients with Hyperuricemia. Chen, H; Chen, L; Ding, R; Hu, X; Jiang, F; Li, X; Li, Y; Liu, K; Peng, Q; Wu, J; Xiong, T; Zhou, Y, 2023) | 1.13 |
| "The concomitant use of HP501, febuxostat, and colchicine did not produce clinically meaningful DDIs in terms of their pharmacokinetic properties." | ( A Phase I Study to Evaluate the Pharmacokinetic Drug‒Drug Interaction of HP501, Febuxostat, and Colchicine in Male Chinese Patients with Hyperuricemia. Chen, H; Chen, L; Ding, R; Hu, X; Jiang, F; Li, X; Li, Y; Liu, K; Peng, Q; Wu, J; Xiong, T; Zhou, Y, 2023) | 1.39 |
Colchicine in combination with non-steroidal anti-inflammatory drugs (NSAIDs) has become the "gold standard" for recurrent pericarditis treatment.
In situ intestinal re-circulating perfusion experiments showed that the absorption rate of fluorescein isothiocyanate (FITC)-labeled OVA in the distal intestine was higher than that for a marker of non-specific absorption, FITC-dextran (FD-40) Colchicine, a general endocytosis inhibitor, suppressed OVA absorption.
Colchicine poisoning can occur not only by taking dosage form but also by ingesting a plant containing colchichine. There is poor adherence to recommended practice for dosing of colchicines in acute gout.
| Role | Description |
|---|---|
| mutagen | An agent that increases the frequency of mutations above the normal background level, usually by interacting directly with DNA and causing it damage, including base substitution. |
| anti-inflammatory agent | Any compound that has anti-inflammatory effects. |
| gout suppressant | A drug that increases uric acid excretion by the kidney (uricosuric drug), decreases uric acid production (antihyperuricemic), or alleviates the pain and inflammation of acute attacks of gout. |
| [role 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] | |
| Class | Description |
|---|---|
| colchicine | An alkaloid that is a carbotricyclic compound comprising 5,6,7,9-tetrahydrobenzo[a]heptalene having four methoxy substituents at the 1-, 2-, 3- and 10-positions as well as an oxo group at the 9-position and an acetamido group at the 7-position. It has been isolated from the plants belonging to genus Colchicum. |
| alkaloid | Any of the naturally occurring, basic nitrogen compounds (mostly heterocyclic) occurring mostly in the plant kingdom, but also found in bacteria, fungi, and animals. By extension, certain neutral compounds biogenetically related to basic alkaloids are also classed as alkaloids. Amino acids, peptides, proteins, nucleotides, nucleic acids, amino sugars and antibiotics are not normally regarded as alkaloids. Compounds in which the nitrogen is exocyclic (dopamine, mescaline, serotonin, etc.) are usually classed as amines rather than alkaloids. |
| [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] | |
| Pathway | Proteins | Compounds |
|---|---|---|
| colchicine biosynthesis | 0 | 18 |
| colchicine biosynthesis | 0 | 21 |
| Drug induction of bile acid pathway | 0 | 25 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 47.1983 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 5.0119 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 35.4813 | 5.6234 | 17.2929 | 31.6228 | AID2323 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 62.5391 | 0.0072 | 15.7588 | 89.3584 | AID1224835 |
| interleukin 8 | Homo sapiens (human) | Potency | 0.0502 | 0.0473 | 49.4806 | 74.9780 | AID651758 |
| endonuclease IV | Escherichia coli | Potency | 2.5119 | 0.7079 | 12.4324 | 31.6228 | AID1708 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 10.2721 | 0.1000 | 20.8793 | 79.4328 | AID488773; AID588453; AID588456 |
| pregnane X receptor | Rattus norvegicus (Norway rat) | Potency | 6.3396 | 0.0251 | 27.9203 | 501.1870 | AID651751 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 60.9290 | 3.1890 | 29.8841 | 59.4836 | AID1224846 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 0.4547 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 11.7804 | 0.0041 | 10.8903 | 31.5287 | AID493106; AID504467 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 0.0037 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 25.1189 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
| PPM1D protein | Homo sapiens (human) | Potency | 0.0466 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| TDP1 protein | Homo sapiens (human) | Potency | 0.0989 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 0.0085 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| Thrombopoietin | Homo sapiens (human) | Potency | 0.5012 | 0.0251 | 7.3048 | 31.6228 | AID917; AID918 |
| AR protein | Homo sapiens (human) | Potency | 5.8749 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID588516; AID743035; AID743036; AID743042; AID743053; AID743054; AID743063 |
| Smad3 | Homo sapiens (human) | Potency | 1.1220 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 10.3075 | 0.0013 | 18.0743 | 39.8107 | AID926; AID938 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 30.2644 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 0.0643 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 12.4501 | 0.0123 | 7.9835 | 43.2770 | AID1346984; AID1645841 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 1.1306 | 0.0002 | 14.3764 | 60.0339 | AID588532; AID588533; AID720692 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 0.0841 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 0.1126 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531; AID588544; AID588546 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 16.4942 | 0.0015 | 30.6073 | 15,848.9004 | AID1224821; AID1224841; AID1224842; AID1224849; AID1259401; AID1259403 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 0.0320 | 0.3758 | 27.4851 | 61.6524 | AID588526; AID588527; AID743217 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 0.7102 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID1346985; AID720659 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 2.7271 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID588513; AID743069; AID743075; AID743077; AID743078; AID743079; AID743080; AID743091 |
| polyprotein | Zika virus | Potency | 0.0037 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| 67.9K protein | Vaccinia virus | Potency | 0.5318 | 0.0001 | 8.4406 | 100.0000 | AID720579; AID720580 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 39.8107 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 1.5940 | 0.0010 | 24.5048 | 61.6448 | AID588534; AID588535; AID743215 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 0.0353 | 0.0010 | 19.4141 | 70.9645 | AID588537 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 2.2218 | 0.0237 | 23.2282 | 63.5986 | AID588541; AID743241 |
| IDH1 | Homo sapiens (human) | Potency | 0.0073 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 10.0000 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 12.5977 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 32.3513 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 0.2939 | 0.1434 | 27.6121 | 59.8106 | AID1159516 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 0.1726 | 0.0578 | 21.1097 | 61.2679 | AID1159526; AID1159528 |
| nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 17.7828 | 0.1000 | 9.1916 | 31.6228 | AID1346983 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 0.7943 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 1.5849 | 0.3162 | 12.4435 | 31.6228 | AID902 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 12.5893 | 0.0025 | 5.8400 | 31.6228 | AID899 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 3.1623 | 0.0063 | 6.9043 | 39.8107 | AID883 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 0.0038 | 0.0060 | 26.1688 | 89.1251 | AID488953 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 0.0230 | 0.0100 | 39.5371 | 1,122.0200 | AID588547 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 0.0580 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 0.2633 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| atrial natriuretic peptide receptor 2 precursor | Homo sapiens (human) | Potency | 1.8493 | 0.0066 | 9.8094 | 18.4927 | AID1347050 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 6.7016 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
| ras-related protein Rab-9A | Homo sapiens (human) | Potency | 291.2372 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 0.0674 | 0.0006 | 27.2152 | 1,122.0200 | AID651741; AID743202; AID743219 |
| geminin | Homo sapiens (human) | Potency | 0.0673 | 0.0046 | 11.3741 | 33.4983 | AID463097; AID504364; AID624296; AID624297 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 0.0955 | 0.0056 | 12.3677 | 36.1254 | AID624032; AID624044 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 2.5119 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 14.2191 | 0.0041 | 9.9625 | 28.1838 | AID2675 |
| caspase-1 isoform alpha precursor | Homo sapiens (human) | Potency | 39.8107 | 0.0003 | 11.4484 | 31.6228 | AID900 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 0.8913 | 0.0010 | 6.0009 | 35.4813 | AID943 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 10.5910 | 0.0200 | 10.7869 | 31.6228 | AID912 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.0685 | 0.8913 | 12.0676 | 28.1838 | AID1459; AID1487 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 2.5119 | 0.0158 | 12.3113 | 615.5000 | AID1461 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 9.0191 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Interferon beta | Homo sapiens (human) | Potency | 0.0466 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 0.1188 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 9.0191 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 3.1623 | 0.0063 | 8.2350 | 39.8107 | AID883 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 0.2268 | 0.0266 | 22.4482 | 66.8242 | AID651802 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| CREB-binding protein | Homo sapiens (human) | Potency | 5.0119 | 0.0282 | 2.3600 | 12.5893 | AID907; AID916 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 0.1359 | 0.0119 | 17.9420 | 71.5630 | AID651632; AID720516 |
| Ataxin-2 | Homo sapiens (human) | Potency | 0.1228 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 0.0379 | 0.0601 | 10.7453 | 37.9330 | AID485368 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Tubulin alpha-1A chain | Sus scrofa (pig) | Kd | 7.5000 | 1.0000 | 1.5760 | 3.7000 | AID1582227; AID551510 |
| Tubulin beta chain | Sus scrofa (pig) | Kd | 7.5000 | 1.0000 | 1.5760 | 3.7000 | AID1582227; AID551510 |
| Tubulin beta-4A chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin beta-4A chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6443 | 1.8600 | AID1492879; AID1549930 |
| Tubulin beta chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin beta chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6443 | 1.8600 | AID1492879; AID1549930 |
| Tubulin alpha-3C chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin alpha-3C chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6574 | 1.8600 | AID1492879; AID1549930 |
| Tubulin alpha-1B chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin alpha-1B chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6574 | 1.8600 | AID1492879; AID1549930 |
| Tubulin alpha-4A chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin alpha-4A chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6574 | 1.8600 | AID1492879; AID1549930 |
| Tubulin beta-4B chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin beta-4B chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6443 | 1.8600 | AID1492879; AID1549930 |
| Tubulin beta-3 chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin beta-3 chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6443 | 1.8600 | AID1492879; AID1549930 |
| Tubulin beta-2A chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin beta-2A chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6443 | 1.8600 | AID1492879; AID1549930 |
| Tubulin polymerization-promoting protein | Bos taurus (cattle) | EC50 (µMol) | 0.7500 | 0.7500 | 3.5000 | 6.2500 | AID1110727 |
| Tubulin beta-8 chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin beta-8 chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6443 | 1.8600 | AID1492879; AID1549930 |
| Tubulin alpha-3E chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin alpha-3E chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6574 | 1.8600 | AID1492879; AID1549930 |
| Tubulin alpha-1A chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin alpha-1A chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6574 | 1.8600 | AID1492879; AID1549930 |
| Tubulin alpha-1C chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin alpha-1C chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6574 | 1.8600 | AID1492879; AID1549930 |
| Tubulin beta-6 chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin beta-6 chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6443 | 1.8600 | AID1492879; AID1549930 |
| Tubulin beta-2B chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin beta-2B chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.6443 | 1.8600 | AID1492879; AID1549930 |
| Tubulin beta-1 chain | Homo sapiens (human) | EC50 (µMol) | 0.2000 | 0.0090 | 0.3685 | 1.2300 | AID1732749 |
| Tubulin beta-1 chain | Homo sapiens (human) | Kd | 5.6790 | 0.0580 | 0.5894 | 1.8600 | AID1492879; AID1549930 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1163572 | Antiproliferative activity against mouse C26 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Synthesis and biological evaluation of novel millepachine derivatives as a new class of tubulin polymerization inhibitors. |
| AID340148 | Growth inhibition of human MKN45 cells after 72 hrs by methylene blue dye assay | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors. |
| AID1333473 | Effect on Cdk6 mRNA expression in human MDA-MB-231 cells assessed as ratio of Cdk6 to GAPDH expression level at 5 uM after 24 hrs by RT-PCR method (Rvb = 1.37 No_unit) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1527065 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
| AID347971 | Antiproliferative activity against human KB/HeLa cells by XTT assay | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1435797 | Induction of mitochondrial membrane hyperpolarization in 3D culture of human MIAPaCa2 cells at 1 uM measured after 48 hrs by DiOC6 dye based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID156331 | Compound was evaluated for growth inhibition against PC-3 cells using cellular assay | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9 | The synthesis and evaluation of benzannelated-azatoxins: the benzazatoxins. |
| AID732808 | Cytotoxicity against human AGS cells assessed as growth inhibition | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Design, synthesis, biological evaluation and molecular modeling studies of 1-aryl-6-(3,4,5-trimethoxyphenyl)-3(Z)-hexen-1,5-diynes as a new class of potent antitumor agents. |
| AID1695273 | Cytotoxicity against human COLO-357 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
| AID1473712 | Antimigratory activity in human RPMI7951 cells at 5 nM after 18 hrs by wound healing assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID1722125 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines. |
| AID214011 | Inhibition of tubulin polymerization using isolated calf brain at 37 degrees C | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22 | Inhibition of tubulin polymerization by 5,6-dihydroindolo[2,1-alpha]isoquinoline derivatives. |
| AID1407731 | Induction of apoptosis in human A375 cells assessed as late apoptotic cells at 1000 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 3.33%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID303699 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G2/M phase after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1274782 | Binding 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 analysis | 2016 | Journal 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. |
| AID1877704 | Cell cycle arrest in human A549 cells assessed as accumulation at G1 phase at 4 uM measured after 36 hrs by flow cytometry (Rvb = 77.38%) | 2022 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 57 | Shikonin N-benzyl matrinic acid ester derivatives as novel telomerase inhibitors with potent activity against lung cancer cell lines. |
| AID1333460 | Induction of apoptosis in human MDA-MB-231 cells assessed as necrotic cells at 5 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.3%) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1736485 | Cell cycle arrest in human HT29 cells assessed as cell accumulation at G2 phase at 1 uM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 10.37 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID214021 | Inhibition of tubulin polymerization with preincubation for 15 minutes at 37 degree Centigrade prior to addition of the GTP required for polymerization | 1993 | Journal 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 |
| AID1773135 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery 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. |
| AID1704313 | Inhibition of tubulin assembly in human COLO357 cells assessed as disruption of mitotic spindle at 5 nM incubated for 24 hrs by Hoechst 33342 staining based confocal microscopic analysis | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1903079 | Antiproliferative activity against human HT-29 cells over expressing GLUT1 assessed as cell viability measured after 48 hrs in presence of GLUT1-specific inhibitor quercetin by MTT assay relative to control | 2022 | Bioorganic & medicinal chemistry, 03-15, Volume: 58 | Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors. |
| AID1732749 | Inhibition of tubulin polymerization in human HeLa cells assessed as dynamic tyrosinated microtubules content by incubated for 2 hrs by immunofluorescence staining based assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies. |
| AID1817854 | Inhibition of microtubule polymerization in human MCF7 cells assessed as disorganisation of microtubule by measuring short and wrapped structure at 2 times IC50 incubated for 24 hrs by DAPI staining based immunofluorescence assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and bioevaluation of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d]imidazoles as tubulin polymerization inhibitors. |
| AID1237724 | Cytotoxicity against Pgp overexpressing human NCI-ADR-RES cells assessed as growth inhibition after 48 hrs by SRB assay | 2015 | Journal 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. |
| AID733782 | Cytotoxicity against taxol-resistant human HCT8 cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID1754732 | Antiproliferative activity against human MCF-7 cells assessed as inhibition of proliferation after 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Synthesis and antiproliferative screening of novel doubly modified colchicines containing urea, thiourea and guanidine moieties. |
| AID274826 | Cell cycle arrest in KB/HeLa cells by accumulation at G1 phase at 0.3 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1153766 | Cytotoxicity against human M38L cells after 48 hrs by MTS assay | 2014 | Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13 | Synthesis of a novel legumain-cleavable colchicine prodrug with cell-specific toxicity. |
| AID1407710 | Antiproliferative activity against human HeLa cells after 72 hrs by MTS assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1473703 | Half life in human liver microsomes by UPLC-MS analysis | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID1694415 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase after 24 to 74 hrs at 5 times of IC50 by propidium iodide staining-based flow cytometric analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
| AID1668778 | Cytotoxicity against Parkinson's disease patient derived human ONS cells assessed as effect on cell morphology parameters at 10 uM after 24 hrs by DAPI staining based fluorescence assay | 2020 | Journal of natural products, 05-22, Volume: 83, Issue:5 | A Grand Challenge. 3. Unbiased Phenotypic Function of Metabolites from Australia Plants |
| AID668145 | Antiproliferative activity against human PC3 cells after 96 hrs by SRB assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | New substituted 4H-chromenes as anticancer agents. |
| AID1435778 | Cytotoxicity against 2D culture of human Colo-357 cells measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1566305 | Cell cycle arrest in human ALL5 cells assessed as accumulation in G2 phase at 5 times of antiproliferative IC50 incubated for 24 hrs by propidium iodide based flow cytometry (Rvb = 10.6 %) | |||
| AID1503400 | Cytotoxic activity in HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID317732 | Cytotoxicity against human HIV1RF infected CEM-SS cells by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
| AID202649 | In vitro inhibitory activity against SK-OV-3 cells using XTT proliferation assay. | 2001 | Journal of medicinal chemistry, Dec-20, Volume: 44, Issue:26 | Synthetic 2-aroylindole derivatives as a new class of potent tubulin-inhibitory, antimitotic agents. |
| AID1186699 | Cytotoxicity against human A431 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | New benzimidazole-2-urea derivates as tubulin inhibitors. |
| AID1822542 | Inhibition of microtubule depolymerization in human A2780S cells at 10 nM incubated for 24 hrs by immunofluorescence method | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents. |
| AID1203384 | Antiproliferative activity in sea urchin embryo assessed as antimitotic activity by measuring cleavage arrest exposed for 8 to 20 mins after fertilization and 45 to 55 mins before first mitotic cycle completion measured 2.5 to 5.5 hrs after fertilization | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines. |
| AID780967 | Induction of microtubule depolymerization in human KB cells at 1 uM after 6 hrs by immunofluorescence microscopic analysis | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Furanylazaindoles: potent anticancer agents in vitro and in vivo. |
| AID160673 | Concentration of compound required to inhibit tubulin polymerization (Microtubule assembly) was determined by the turbidity formation after 20 min of incubation | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity. |
| AID336354 | Cytotoxicity against human U373 cells | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID716403 | Induction of morphological changes in human SKv-a cells assessed as loss of radial distribution of structured microtubules at 10 '-6 M by confocal microscopy | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4. |
| AID780975 | Cytotoxicity against human KB-7d cells overexpressing MRP assessed as growth inhibition after 72 hrs by methylene blue staining-based assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Furanylazaindoles: potent anticancer agents in vitro and in vivo. |
| AID347976 | Antiproliferative activity against human RKO cells containing ecdysone-inducible expression vector of p27kipl by XTT assay | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID109716 | Antitumor activity against P388 lymphocytic leukemia in mice | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
| AID348167 | Cytotoxicity against human MIAPaCa2 cells after 48 hrs by alamar blue assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Design, synthesis and biological evaluation of novel stilbene-based antitumor agents. |
| AID1194048 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | Synthesis and biological evaluation of benzimidazole acridine derivatives as potential DNA-binding and apoptosis-inducing agents. |
| AID605849 | Antiproliferative activity against human COLO205 cells after 48 hrs by alamar blue assay | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1773137 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery 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. |
| AID1163576 | Antiproliferative activity against human NCI-H358 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Synthesis and biological evaluation of novel millepachine derivatives as a new class of tubulin polymerization inhibitors. |
| AID331410 | Cell cycle arrest in human MCF7 cells assessed as increase in G2/M phase accumulation at 0.1 uM after 16 hrs by FACS analysis | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Cycloalkyl-substituted aryl chloroethylureas inhibiting cell cycle progression in G0/G1 phase and thioredoxin-1 nuclear translocation. |
| AID458390 | Anticancer activity against human NUGC3 cells after 72 hrs by MTS/PMS assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Synthesis and biological activities of 2-amino-1-arylidenamino imidazoles as orally active anticancer agents. |
| AID1193496 | Thermodynamic equilibrium solubility, log S of the compound in water at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
| AID132884 | Percent increase in life-span against in vivo P388 murine leukemia at a dose 1 mg/kg in trail 2; Toxic | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID277281 | Cytotoxicity against KB-3-1 cell line | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Highly potent triazole-based tubulin polymerization inhibitors. |
| AID778898 | Inhibition of purified bovine tubulin polymerization preincubated at 2 uM for 2 mins before GTP addition measured every 60 seconds for 60 mins by spectrophotometry | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Design, synthesis and biological evaluation of millepachine derivatives as a new class of tubulin polymerization inhibitors. |
| AID1431310 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for human A549 cells | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID1238302 | Inhibition of Myc mRNA expression in human HT-29 cells assessed as Myc mRNA level at 5 ug/ml incubated for 48 hrs by RT-PCR method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes. |
| AID1674006 | Cytotoxicity against human HT-29 cells incubated for 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1704312 | Induction of cell cycle arrest in human SW-620 cells assessed as accumulation at apoptotic phase at 5 nM incubated for 48 hrs by RNase/PI staining based flow cytometry analysis (Rvb = 0.8 %) | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1877695 | Cell cycle arrest in human A549 cells assessed as accumulation at G1 phase at 8 uM measured after 24 hrs by flow cytometry (Rvb = 73.33%) | 2022 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 57 | Shikonin N-benzyl matrinic acid ester derivatives as novel telomerase inhibitors with potent activity against lung cancer cell lines. |
| AID1492837 | Antiproliferative activity against human HeLa cells after 96 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. |
| AID1566295 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay | |||
| AID733780 | Cytotoxicity against taxol-resistant human A2780 cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID348002 | Cell cycle arrest in human KB/HeLa cells assessed as S phase accumulation at 100 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID412964 | Growth inhibition of human MKN45 cells after 72 hrs by methylene blue dye assay | 2008 | Journal 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. |
| AID1368410 | Inhibition of porcine brain tubulin polymerization at 1 uM measured every 1 min for 30 mins | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | N-Arylsulfonylsubstituted-1H indole derivatives as small molecule dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and tubulin. |
| AID1413543 | Selectivity index, ratio of CC50 for hTERT-RPE1 cells to GI50 for human Caco2 cells | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | Synthesis and biological evaluation of novel 5-chloro- |
| AID1754731 | Antiproliferative activity against human Lovo/DX cells assessed as inhibition of proliferation after 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Synthesis and antiproliferative screening of novel doubly modified colchicines containing urea, thiourea and guanidine moieties. |
| AID1407717 | Antiproliferative activity against HUVEC after 72 hrs by MTS assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1875314 | Cytotoxicity in human MCF7/Vin cells assessed as growth inhibition level after 48 hrs by SRB assay | 2022 | Journal of natural products, 10-28, Volume: 85, Issue:10 | Resin Glycosides from |
| AID1736480 | Cell cycle arrest in human HT29 cells assessed as cell accumulation at S phase at 0.25 uM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 20.44 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1125810 | Displacement of [3H]colchicine from tubulin (unknown origin) at 1 uM after 2 hrs by scintillation counting analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Antimitotic and vascular disrupting agents: 2-hydroxy-3,4,5-trimethoxybenzophenones. |
| AID1305706 | Permeability across basolateral side at pH 6.5 to apical side at pH 7.4 in human Caco2 cells at 10 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Coumarin carboxylic acids as monocarboxylate transporter 1 inhibitors: In vitro and in vivo studies as potential anticancer agents. |
| AID1822547 | Induction of abnormal aggregation in microtubule network in human A2780S cells assessed as bundling of microtubule fibers in chromosome at 100 nM for 24 hrs | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents. |
| AID1359652 | Antiproliferative activity against human A549 cells after 48 to 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Discovery of novel β-carboline/acylhydrazone hybrids as potent antitumor agents and overcome drug resistance. |
| AID1414050 | Antifungal activity against Aspergillus versicolor BAM8 ATCC 11730 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1435790 | Disruption of mitotic spindle in human Colo-357 cells at 1 uM measured after 72 hrs by Hoechst 33342 staining based confocal microscopic analysis | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1063555 | Inhibition of tubulin polymerization (unknown origin) at 20 uM by spectrophotometric analysis | 2014 | Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2 | Synthesis and biological evaluation of 6H-pyrido[2',1':2,3]imidazo[4,5-c]isoquinolin-5(6H)-ones as antimitotic agents and inhibitors of tubulin polymerization. |
| AID1236572 | Cytotoxicity against human NCI-ADR-RES cells expressing ABCB1 | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Progress Toward the Development of Noscapine and Derivatives as Anticancer Agents. |
| AID681128 | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID1610963 | Induction of tubulin depolymerization in human A549 cells at 1 uM after 24 hrs by DAPI staining based fluorescence microscopic analysis | 2019 | Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23 | Design, synthesis and biological evaluation of benzoylacrylic acid shikonin ester derivatives as irreversible dual inhibitors of tubulin and EGFR. |
| AID106134 | Inhibitory concentration against the growth of HET-SR-2SC-LNM cell line after 72 hr of drug exposure by MTT test | 2002 | Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24 | Effects of isoprenoid analogues of SDB-ethylenediamine on multidrug resistant tumor cells alone and in combination with chemotherapeutic drugs. |
| AID397098 | Inhibition of bovine brain tubulin polymerization | |||
| AID228462 | Inhibition of tubulin polymerization, induced by 10 mM taxol at a concentration of 2 uM. | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Fluorinated colchicinoids: antitubulin and cytotoxic properties. |
| AID733794 | Cytotoxicity against human HT-29 cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID1566313 | Cell cycle arrest in human ALL5 cells assessed as accumulation in subG1 phase at 5 times of antiproliferative IC50 incubated for 72 hrs by propidium iodide based flow cytometry (Rvb = 15.5 %) | |||
| AID1359653 | Resistance index, ratio of IC50 for human A549/TR cells to IC50 for human A549 cells | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Discovery of novel β-carboline/acylhydrazone hybrids as potent antitumor agents and overcome drug resistance. |
| AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2 | Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
| AID1186702 | Cytotoxicity against human MDA-MB-435S cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | New benzimidazole-2-urea derivates as tubulin inhibitors. |
| AID1532041 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24 | Optimization of substituted cinnamic acyl sulfonamide derivatives as tubulin polymerization inhibitors with anticancer activity. |
| AID744716 | Cytotoxicity against human Jurkat cells after 48 hrs by MTT assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID1850712 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2022 | RSC medicinal chemistry, May-25, Volume: 13, Issue:5 | Morpholine substituted quinazoline derivatives as anticancer agents against MCF-7, A549 and SHSY-5Y cancer cell lines and mechanistic studies. |
| AID729161 | Cytotoxicity against human MDA-MB-435/LCC6MDR1 cells assessed as growth inhibition after 48 hrs by SRB assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery of 4-Aryl-2-benzoyl-imidazoles as tubulin polymerization inhibitor with potent antiproliferative properties. |
| AID388960 | Toxicity in C57BL/J6 mouse assessed as liver alanine aminotransferase level | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID1882714 | Antitubulin activity against bovine brain tubulin polymerization preincubated with compound followed by GTP addition and measured after 20 mins by turbidimetry-based spectrophotometric method | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Recent advances of antitumor shikonin/alkannin derivatives: A comprehensive overview focusing on structural classification, synthetic approaches, and mechanisms of action. |
| AID780973 | Inhibition of bovine brain MAP-rich tubulin polymerization measured every 30 secs for 30 mins by turbidometric method | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Furanylazaindoles: potent anticancer agents in vitro and in vivo. |
| AID1736526 | Induction of apoptosis in human HT-29 cells assessed as viable cells at 0.25 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 98.3 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID336337 | Cytotoxicity against human Lu1 cells | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID642529 | Growth inhibition of human HT-29 cells after 72 hrs by methylene blue assay | 2011 | Journal 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. |
| AID1566293 | Antiproliferative activity against human ALL5 cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay | |||
| AID733784 | Cytotoxicity against human A2780S cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID1625726 | Antiproliferative activity against human A2780S cells after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID614578 | Cytotoxicity against human A549 cells after 24 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | Synthesis and SAR requirements of adamantane-colchicine conjugates with both microtubule depolymerizing and tubulin clustering activities. |
| AID28236 | Unbound fraction (tissues) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID1899074 | Antiproliferative activity against human K562/Adr cells measured after 72 hrs by SRB assay | |||
| AID404609 | Inhibition of sheep brain tubulin polymerization | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | New C5-alkylated indolobenzazepinones acting as inhibitors of tubulin polymerization: cytotoxic and antitumor activities. |
| AID1668046 | Cell cycle arrest in human SK-MEL-28 cells assessed as accumulation at G2/M phase at 5 nM after 24 hrs by Hoechst 33324 dye staining based fluorescence assay | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Drug repurposing and rediscovery: Design, synthesis and preliminary biological evaluation of 1-arylamino-3-aryloxypropan-2-ols as anti-melanoma agents. |
| AID1566317 | Cell cycle arrest in human MCF7 cells assessed as accumulation in G1 phase at 5 times of antiproliferative IC50 incubated for 24 hrs by propidium iodide based flow cytometry (Rvb = 49.9 %) | |||
| AID249634 | Effect to arrest S-phase on HEK 293 cells at 10 uM was determined | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Discovery of S-phase arresting agents derived from noscapine. |
| AID75554 | Ability to inhibit the dibutyryl-cAMP-induced change of an immature glioma cell to a mature, differentiated astrocyte by in vitro astrocytoma assay at 1 ug/mL dose (Experiment #1); value may range from 51 to 70 | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | In vivo antitumor activity of 6-benzyl-1,3-benzodioxole derivatives against the P388, L1210, B16, and M5076 murine models. |
| AID1452439 | Inhibition of human PIM1 measured after 5 mins by ELISA relative to control | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | Eco-friendly synthesis of novel cyanopyridine derivatives and their anticancer and PIM-1 kinase inhibitory activities. |
| AID1566309 | Cell cycle arrest in human ALL5 cells assessed as accumulation in G1 phase at 5 times of antiproliferative IC50 incubated for 48 hrs by propidium iodide based flow cytometry (Rvb = 67.4 %) | |||
| AID735506 | Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells in G0/G1 phase at 4 uM concentration after 24 hrs by propidium iodide staining based cytofluorimetric analysis (Rvb = 39.55%) | 2013 | European 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. |
| AID1541704 | Inhibition of anchorage-independent colony formation in human MDA-MB-231 cells at 5 uM measured upto 21 days by soft agar colony formation assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis, and validation of novel nitrogen-based chalcone analogs against triple negative breast cancer. |
| AID677621 | Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17 | Identification of selective tubulin inhibitors as potential anti-trypanosomal agents. |
| AID1389597 | Inhibition of MSU-induced TNFalpha level in synovial homogenate of acute gouty arthritis Sprague-Dawley rat model at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last dose measured up to 24 hrs by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID1903071 | Antiproliferative activity against human Hep3B cells measured after 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 03-15, Volume: 58 | Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors. |
| AID1500626 | Binding affinity to beta-tubulin colchicine binding site in human HepG2 cells assessed as reduction in EBI-beta-tubulin adduct formation at 5 uM preincubated for 2 hrs followed by EBI addition measured after 1.5 hrs by Western blot analysis | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents. |
| AID1389611 | Inhibition of MSU-induced p65 NFkappaB protein level in synovial homogenate of acute gouty arthritis Sprague-Dawley rat model at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last dose measured up to 24 hrs by Wes | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID1407749 | Inhibition of porcine brain tubulin polymerization at 10 uM measured every 60 secs for 2 hrs by spectrophotometric method | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1732754 | Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies. |
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| AID1882892 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
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| AID730205 | Antiangiogenic activity in quesicent HUVECs assessed as disruption of preformed capillaries at 0.1 uM after 4 hrs by light microscopic analysis (Rvb = 11%) | 2013 | Journal 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. |
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| AID1142147 | Antivascular activity in HMEC1 cells assessed as destruction of cord like structure at 0.3 to 1 uM after 90 mins by matrigel assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach. |
| AID1435793 | Induction of beta-tubulin expression in human Colo-357 cells assessed as mean fluorescence intensity at 1 uM measured after 24 hrs by Hoechst 33342 staining based confocal microscopic analysis (Rvb = 52 +/- 12) | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1704301 | Antiproliferative activity against human SW-620 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1333467 | Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 5 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 4.23%) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
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| AID1585584 | Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents. |
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| AID1142153 | Antiproliferative activity against human MDA-MB-231 cells at 0.08 uM after 17 hrs | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach. |
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| AID291507 | Cell cycle arrest in HL60 cells assessed as accumulation in G0/M phase at 600 nM | 2007 | Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14 | Discovery of novel antitumor antimitotic agents that also reverse tumor resistance. |
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| AID1610976 | Inhibition of microtubule polymerization in human A549 cells assessed as polymerized tubulin expression at 1 uM after 24 hrs by immuno blot analysis (Rvb = 0.85 No_unit) | 2019 | Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23 | Design, synthesis and biological evaluation of benzoylacrylic acid shikonin ester derivatives as irreversible dual inhibitors of tubulin and EGFR. |
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| AID1897672 | Induction of microtubule disruption in human HCT-116 cells assessed as disintegrated microtubules at 20 nM incubated for 48 hrs by DAPI staining based confocal microscopic immunofluorescence analysis | 2022 | Bioorganic & medicinal chemistry, 12-15, Volume: 76 | Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities. |
| AID625277 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16 | FDA-approved drug labeling for the study of drug-induced liver injury. |
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| AID303716 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G2M phase at 316 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
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| AID347988 | Cell cycle arrest in human KB/HeLa cells assessed as G2/M phase accumulation at 0.3 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
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| AID1407725 | Induction of apoptosis in human A375 cells assessed as live cells at 100 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 94.2%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID758709 | Growth inhibition of human K562 cells after 24 hrs by trypan blue exclusion assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
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| AID1898094 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID536766 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis and cytotoxicity evaluation of novel 1,4-disubstituted 1,2,3-triazoles via CuI catalysed 1,3-dipolar cycloaddition. |
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| AID1897655 | Induction of cell cycle arrest in human HCT-116 cells assessed as G1 phase cells at 20 nM measured after 48 hrs by propidium iodide/RNase staining based flow cytometry analysis (Rvb = 61.51 %) | 2022 | Bioorganic & medicinal chemistry, 12-15, Volume: 76 | Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities. |
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| AID1435407 | Inhibition of tubulin beta polymerization in human MCF7 cells after 18 to 24 hrs by spectrophotometric method relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and cytotoxic activity of certain novel chalcone analogous compounds. |
| AID1395530 | Antiproliferative activity against human HT-29 cells after 2 days by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID1917310 | Inhibition of pig brain tubulin polymerization at 10 uM by spectrometric method relative to control | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors. |
| AID1320430 | Growth inhibition of HUVEC after 72 hrs by crystal violet staining-based assay | 2016 | Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20 | Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4. |
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| AID1822509 | Antiproliferative activity against human A2780S cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents. |
| AID1822508 | Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents. |
| AID1917312 | Cytotoxicity against mouse HT-22 cells measured after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors. |
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| AID1898066 | Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID1582216 | Antiproliferative activity against human PC3 cells measured after 72 hrs by MTS assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties. |
| AID1625723 | Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1860524 | Antiproliferative activity against human HN-6 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC. |
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| AID1424777 | Growth inhibition of human MCF7 cells after 96 hrs by trypan blue exclusion assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors. |
| AID1722132 | Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells at 5 uM measured after 24 hrs by annexin-V/FITC staining based flow cytometry analysis (Rvb = 2.4 %) | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines. |
| AID1785478 | Induction of microtubule depolymerization in human A2780S assessed as inhibition of microtubule network polymerization at 5 uM incubated for 16 hrs by DAPI staining based fluorescence microscopic method | |||
| AID422575 | Cytotoxicity against human KB cells after 72 hrs by methylene blue dye assay | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and evaluation of 3-aroylindoles as anticancer agents: metabolite approach. |
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| AID1582214 | Antiproliferative activity against human M14 cells measured after 72 hrs by MTS assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties. |
| AID1698822 | Antimitotic activity against sea urchin embryo assessed as cleavage alteration measured 2.5 to 6 hrs post-fertilization by light microscopy analysis | 2020 | Bioorganic & 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. |
| AID770269 | Effect on actin depolymerization in rat REF52 cells assessed as effect on ratio of soluble to insoluble protein fraction at 0.1 uM after 30 mins by Western blot analysis | 2013 | Journal of natural products, Sep-27, Volume: 76, Issue:9 | Enantioselective effects of (+)- and (-)-citronellal on animal and plant microtubules. |
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| AID1272835 | Inhibition of microtubule-stimulated N-terminal MKLP-2 (56 to 505 residues) ATPase activity isolated from human hepatocellular carcinoma cells up to 100 uM by pyruvate kinase/lactate dehydrogenase enzyme linked assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | New MKLP-2 inhibitors in the paprotrain series: Design, synthesis and biological evaluations. |
| AID1638300 | Antiproliferative activity against human MGC803 cells measured after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Molecular diversity of trimethoxyphenyl-1,2,3-triazole hybrids as novel colchicine site tubulin polymerization inhibitors. |
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| AID1593959 | Induction of apoptosis in human PHK160b cells assessed as induction of multiple fragmented segregated bodies at 100 uM incubated for 48 hrs Hoechst 33,342 staining based fluorescent microscopy | |||
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| AID1333480 | Inhibition of Akt in human MDA-MB-231 cells assessed as ratio of phosphorylated Akt to GAPDH expression level at 5 uM after 48 hrs by immunoblot analysis (Rvb = 0.33 to 0.81 No_unit) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
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| AID1267202 | Cytotoxicity against multidrug resistant human MES-SA/Dx5 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer. |
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| AID1785509 | Antiproliferative activity against human Ramos cells incubated for 72 hrs by MTT assay | |||
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| AID214550 | Inhibition of Tubulin polymerization after 20 minutes of administration at 30 degree Centigrade | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | Antitumor agents. 172. Synthesis and biological evaluation of novel deacetamidothiocolchicin-7-ols and ester analogs as antitubulin agents. |
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| AID1722131 | Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells at 5 uM measured after 24 hrs by annexin-V/FITC staining based flow cytometry analysis (Rvb = 0.3 %) | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines. |
| AID744714 | Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID659043 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 30 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 16.2 %) | 2012 | Journal 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. |
| AID1389576 | Antiarthritic activity in MSU-induced acute gouty arthritis Sprague-Dawley rat model assessed as reduction in ankle swelling by measuring perimeter of ankle at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last do | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID132966 | In vivo antitumor activity against P388 mouse leukemia and minimum affective dose (MED) which produced a T/C greater than the threshold value of 125 was reported. | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | A novel synthesis of colchicide and analogues from thiocolchicine and congeners: reevaluation of colchicide as a potential antitumor agent. |
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| AID1722128 | Inhibition of tubulin polymerization in human HCT-116 cells assessed as cell cycle arrest at S phase at 12.5 uM measured after 24 hrs by propidium iodide staining based analysis (Rvb = 16.2 %) | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines. |
| AID711174 | Cytotoxicity against human A2780AD cells expressing p-gp after 96 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID1399020 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18 | Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors. |
| AID524791 | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID1407734 | Induction of apoptosis in human A375 cells assessed as early apoptotic cells at 10 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.4%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1899073 | Antiproliferative activity against human K562 cells measured after 72 hrs by SRB assay | |||
| AID1527074 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
| AID1863087 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway. |
| AID538695 | Cell cycle arrest in human MCF7 cells assessed as accumulation at sub-G1 phase after 24 hrs by flow cytometry relative to control | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Synthesis, molecular modeling and biological evaluation of guanidine derivatives as novel antitubulin agents. |
| AID1189965 | Toxicity 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 fluorimetry | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Synthesis and biological evaluation of furanoallocolchicinoids. |
| AID744713 | Cytotoxicity against human PBMC cells after 24 hrs by MTT assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID1382776 | Antiproliferative activity against human HeLa cells after 3 days by coulter counting method | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity. |
| AID1305707 | Permeability across apical side at pH 6.5 to basolateral side at pH 7.4 in human Caco2 cells assessed as compound recovery at 10 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Coumarin carboxylic acids as monocarboxylate transporter 1 inhibitors: In vitro and in vivo studies as potential anticancer agents. |
| AID1354607 | Inhibition of cell migration in human MDA-MB-231 cells at 10 uM incubated for 24 hrs by scratch wound healing assay relative to control | 2018 | Journal of natural products, 05-25, Volume: 81, Issue:5 | Inhibition of Breast Cancer Cell Migration by Cyclotides Isolated from Pombalia calceolaria. |
| AID347992 | Cell cycle arrest in human KB/HeLa cells assessed as G1 phase accumulation at 1 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1504728 | Cytotoxicity in human HeLa cells assessed as reduction in cell viability after 4 days under dark condition by MTT assay | |||
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| AID744708 | Antimitotic activity in human HeLa cells assessed as increase in phosphohistone H3 level after 24 hrs by Hoechst 33342 staining | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID377078 | Antimicrobial activity against Saccharomyces cerevisiae after 3 days | 2005 | Journal of natural products, Feb, Volume: 68, Issue:2 | New colchicinoids from a native Jordanian meadow saffron, colchicum brachyphyllum: isolation of the first naturally occurring dextrorotatory colchicinoid. |
| AID274811 | Cell cycle arrest in KB/HeLa cells by accumulation at S phase at 1 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1821559 | Antiproliferative activity against human KYSE-450 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis and evaluation of novel bis-substituted aromatic amide dithiocarbamate derivatives as colchicine site tubulin polymerization inhibitors with potent anticancer activities. |
| AID1267533 | Antiproliferative activity against human IC8 cells after 72 hrs by MTT assay | 2016 | Bioorganic & 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. |
| AID1167520 | Antiproliferative activity against BAEC assessed as inhibition of cell proliferation after 3 days by Coulter counter based cell counting method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Synthesis and antiproliferative activity of 6-phenylaminopurines. |
| AID1198455 | Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents. |
| AID1413545 | Selectivity index, ratio of CC50 for hTERT-RPE1 cells to GI50 for human MDA-MB-231 cells | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | Synthesis and biological evaluation of novel 5-chloro- |
| AID336340 | Cytotoxicity against human HT cells | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID1917313 | Cytotoxicity against human NCM460 cells measured after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors. |
| AID1549906 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain. |
| AID1435795 | Induction of F-actin expression in 3d culture of human MIAPaCa2 cells at 1 uM measured after 48 hrs by propidium staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1883546 | Disruption of microtubule network in human HGC-27 cells assessed as cytoskeleton disruption at 25 nM measured after 48 hrs by DAPI staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID1785459 | Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay | |||
| AID95875 | The compound was tested for its cytotoxic concentration required to inhibit the replication of human tumor nasopharynx (KB) cell lines | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20 | Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids. |
| AID1888931 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Synthesis and biological evaluation of 3β-O-neoglycosides of caudatin and its analogues as potential anticancer agents. |
| AID637198 | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 5 ug/ml after 24 hrs by flow cytometric analysis (Rvb = 66%) | 2012 | Bioorganic & 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. |
| AID1203386 | Antiproliferative activity in sea urchin embryo assessed as destabilization of microtubule by tuberculate eggs after 15 mins to 20 hrs | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines. |
| AID1915565 | Inhibition of tubulin polymerization (unknown origin) incubated for 15 mins in presence of GTP by fluorescence-based tubulin polymerization assay kit | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
| AID1189184 | Displacement of (E)-3-(4-(Dimethylamino)phenyl)-1-(4'-fluoro[1,1'-biphenyl]-2-yl)prop-2-en-1-one from tubulin (unknown origin) by fluorescence assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1201726 | Cytotoxicity against human SW620 cells assessed as growth inhibition after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID1651305 | Antiarthritic activity against MSU-induced acute gout arthritis rat model assessed as degree of ankle joint swelling after 8 hrs (Rvb = 7.8 +/- 1.6 No_unit) | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Development of novel NLRP3-XOD dual inhibitors for the treatment of gout. |
| AID605843 | Antiproliferative activity against human NCI-H460 cells after 48 hrs by alamar blue assay | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID388961 | Toxicity in C57BL/J6 mouse assessed as liver alkaline phosphatase level | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis. |
| AID1809652 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Synthesis of thiocolchicine amine derivatives and evaluation of their antiproliferative activity. |
| AID1722126 | Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines. |
| AID1194695 | Antiproliferative activity against human PANC1 cells after 48 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10 | Synthesis and evaluation of benzosuberone embedded with 1,3,4-oxadiazole, 1,3,4-thiadiazole and 1,2,4-triazole moieties as new potential anti proliferative agents. |
| AID297419 | Growth inhibition of human KB cells after 72 hrs by methylene blue dye assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | 4- and 5-aroylindoles as novel classes of potent antitubulin agents. |
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| AID1582304 | Inhibition of porcine brain tubulin polymerization measured at 1 min interval over 20 mins by absorbance based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Scaffold Hopping of Natural Product Evodiamine: Discovery of a Novel Antitumor Scaffold with Excellent Potency against Colon Cancer. |
| AID613282 | Antiproliferative activity against human KB cells after 72 hrs by methylene blue assay | 2011 | European 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. |
| AID1500636 | Cytotoxicity against mouse HT22 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of 9H-purins as potential tubulin polymerization inhibitors: Synthesis, biological evaluation and structure-activity relationships. |
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| AID1353641 | Inhibition of EBI binding to beta-tubulin colchicine binding site in human MDA-MB-231 cells at 3 uM preincubated for 16 hrs followed by EBI addition and measured after 1.5 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Mar-10, Volume: 147 | Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents. |
| AID1395534 | Induction of apoptosis in human HT-29 cells assessed as viable cells at 40 nM after 48 hrs by Annexin V-FITC staining-based flow cytometric analysis (Rvb = 82 +/- 1%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID1407735 | Induction of apoptosis in human A375 cells assessed as late apoptotic cells at 10 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.96%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1736535 | Induction of apoptosis in human HT-29 cells assessed as early apoptotic cells at 1 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.6 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1189590 | Selectivity ratio of IC50 for human HEK293 cells to IC50 for human MCF7 cells | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID1167528 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G1 phase at 0.1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 45%) | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Synthesis and antiproliferative activity of 6-phenylaminopurines. |
| AID1758696 | Inhibition of tubulin polymerization (unknown origin) at 40 uM measured every 30 secs for 90 mins relative to control | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Synthesis and structure-activity relationships of 5-phenyloxazole-2-carboxylic acid derivatives as novel inhibitors of tubulin polymerization. |
| AID735027 | Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells in S phase at 8 uM concentration after 24 hrs by propidium iodide staining based cytofluorimetric analysis (Rvb = 26.17%) | 2013 | European 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. |
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| AID1142145 | Binding affinity to tubulin in human MDA-MB-231 cells assessed as inhibition of mitotic spindle formation at 0.1 uM after 8 hrs by DAPI staining-based fluorescence microscopic analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach. |
| AID1389608 | Inhibition of MSU-induced TLR4 protein level in synovial homogenate of acute gouty arthritis Sprague-Dawley rat model at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last dose measured up to 24 hrs by Western blo | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
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| AID1389596 | Inhibition of MSU-induced IL-1beta level in synovial homogenate of acute gouty arthritis Sprague-Dawley rat model at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last dose measured up to 24 hrs by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
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| AID1338402 | Cell cycle arrest in human 786-0 cells assessed as accumulation at sub-G1 phase at 1.25 uM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb=3.7+/-0.9%) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and evaluation of novel hybrids β-carboline-4-thiazolidinones as potential antitumor and antiviral agents. |
| AID1189587 | Cytotoxicity against human MCF7 cells after 3 days by MTT assay | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID730213 | Cytotoxicity against human A549 cells after 72 hrs by CCK-8 assay | 2013 | Journal 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. |
| AID1569054 | Antimigratory activity in human A375 cells assessed as wound closure at 25 nM after 22 hrs by scratch migration assay (Rvb = 60.7 +/- 3.5%) | |||
| AID274820 | Cell cycle arrest in KB/HeLa cells by accumulation at G2/M phase at 3.16 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1695279 | Induction of cell cycle arrest in human COLO357 cells assessed as G1 phase at 5 uM incubated for 72 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 91.1 %) | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
| AID340146 | Growth inhibition of human KB cells after 72 hrs by methylene blue dye assay | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors. |
| AID1694409 | Resistance index, ratio of IC50 for antiproliferative activity against human Lovo/DX cells to IC50 for antiproliferative activity against human LoVo cells | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
| AID1414063 | Fungicidal activity against Aureobasidium pullulans BAM10 ATCC 9348 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID397289 | Cytotoxicity against human HCT116 cells after 72 hrs | 2009 | Journal 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. |
| AID273359 | Inhibition of tubulin polymerization | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21 | 2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents. |
| AID1807382 | Cytotoxicity against paclitaxel resistant human A-375/TxR cells measured after 72 hrs by western blot | |||
| AID1585581 | Cytotoxicity against human A2780 cells after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents. |
| AID1272838 | Induction of of sheep brain microtubule disassembly by UV spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | New MKLP-2 inhibitors in the paprotrain series: Design, synthesis and biological evaluations. |
| AID1899071 | Antiproliferative activity against human KB-V1 cells measured after 72 hrs by SRB assay | |||
| AID277278 | Cytotoxicity against HCT116 cell line | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Highly potent triazole-based tubulin polymerization inhibitors. |
| AID605715 | Antiproliferative activity against CHO cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID1354604 | Inhibition of cell migration in human MDA-MB-231 cells at 1 uM incubated for 24 hrs by scratch wound healing assay relative to control | 2018 | Journal of natural products, 05-25, Volume: 81, Issue:5 | Inhibition of Breast Cancer Cell Migration by Cyclotides Isolated from Pombalia calceolaria. |
| AID150751 | Inhibition of P-glycoprotein using ATPase in MDR1 membranes | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID1189964 | Toxicity 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 fluorimetry | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Synthesis and biological evaluation of furanoallocolchicinoids. |
| AID618916 | Anticancer activity against P-gp overexpressing human NCI/ADR-RES cells after 96 hrs by SRB assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Design, synthesis, and SAR studies of 4-substituted methoxylbenzoyl-aryl-thiazoles analogues as potent and orally bioavailable anticancer agents. |
| AID553909 | Cell cycle arrest in human NCI-H522 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. |
| AID1807437 | Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Design, structure-activity relationship study and biological evaluation of the thieno[3,2-c]isoquinoline scaffold as a potential anti-cancer agent. |
| AID1189149 | Antiproliferative activity against vincristine-resistant human HCT8 cells after 48 hrs by SRB method | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1221968 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1898096 | Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID1473700 | Cytotoxicity against human A375 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID342518 | Ratio of IC50 of drug to IC50 of colchicine for calf brain tubulin polymerization | 2008 | Bioorganic & 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. |
| AID336343 | Inhibition of calf thymus tubulin polymerization by turbidimetric analysis | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID1233602 | Induction of cell cycle arrest in human M21 cells assessed as cells accumulation at G2/M phase at 24 nM after 24 hrs by flow cytometry (Rvb = 22.1%) | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model. |
| AID23271 | Partition coefficient (logD7.4) | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Structure-activity relationships of antineoplastic agents in multidrug resistance. |
| AID1238301 | Inhibition of hTERT mRNA expression in human HT-29 cells assessed as hTERT mRNA level at 5 ug/ml incubated for 48 hrs by RT-PCR method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes. |
| AID1668781 | Effect on autophagosome in Parkinson's disease patient derived human ONS cells assessed as LC3b parameters at 10 uM after 24 hrs by anti-LC3b 1/335 staining based fluorescence assay | 2020 | Journal of natural products, 05-22, Volume: 83, Issue:5 | A Grand Challenge. 3. Unbiased Phenotypic Function of Metabolites from Australia Plants |
| AID1898106 | Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID1296729 | Cytotoxicity against human Jurkat cells after 48 hrs by Celltiter-Glo luminescent cell viability assay | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology. |
| AID1695282 | Induction of cell cycle arrest in human L929 cells assessed as G1 phase at 5 uM incubated for 72 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 91 %) | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
| AID1562388 | Antiproliferative activity against human A549 cells harboring katanin siRNA after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin. |
| AID1817858 | Inhibition of porcine brain tubulin polymerization measured every 1 min for 90 mins by microplate based assay in the presence of GTP | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and bioevaluation of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d]imidazoles as tubulin polymerization inhibitors. |
| AID657580 | Cell cycle arrest in human MCF7 cells assessed as accumulation in G2/M phase at 5 ug/ml after 24 hrs by flow cytometry (Rvb = 12.99%) | 2012 | Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10 | Design, synthesis and biological evaluation of novel chalcone derivatives as antitubulin agents. |
| AID540212 | Mean residence time in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1750234 | Antiproliferative activity against human A2780S cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | |||
| AID1832109 | Antiproliferative activity against human HCT-116 assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors. |
| AID758707 | Growth inhibition of human HepG2 cells after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID1431294 | Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID1428410 | Cytotoxicity against multidrug resistant human MCF7 cells cultured in vinblastine free medium assessed as growth inhibition after 72 hrs by SRB assay | |||
| AID1407733 | Induction of apoptosis in human A375 cells assessed as live cells at 10 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 92.3%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1198224 | Inhibition of tubulin (unknown origin) polymerization preincubated for 45 mins followed by GTP addition measured after 2 hrs by fluorescence assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Antivascular and anti-parasite activities of natural and hemisynthetic flavonoids from New Caledonian Gardenia species (Rubiaceae). |
| AID1771090 | Antiproliferative activity against human A375/TxR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID1435781 | Cytotoxicity against 2D culture of human MSC measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID679098 | TP_TRANSPORTER: transepithelial transport of Colchicine at a concentration of 25 uM in MDR1-expressing MDCK cells | 2003 | Pharmaceutical research, Aug, Volume: 20, Issue:8 | Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. |
| AID106133 | Inhibitory concentration against the growth of 2SC/20 cell line after 72 hr of drug exposure by MTT test | 2002 | Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24 | Effects of isoprenoid analogues of SDB-ethylenediamine on multidrug resistant tumor cells alone and in combination with chemotherapeutic drugs. |
| AID1673969 | Antiproliferative activity against human LoVo/DX cells incubated for 72 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID202815 | The compound was tested for the cytotoxicity for the cell lines of human melanoma cancer (SKMEL-2) using SRB assay. | 1998 | Journal 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. |
| AID1359656 | Antiproliferative activity against human A2780T cells after 48 to 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Discovery of novel β-carboline/acylhydrazone hybrids as potent antitumor agents and overcome drug resistance. |
| AID744700 | Antimigratory activity against human MDA-MB-231 cells after 6 hrs by Boyden chamber migration assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID1316903 | Cytotoxicity against human HeLa cells assessed as reduction in cell growth measured after 48 hrs by WST-8 assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Discovery of O |
| AID348004 | Cell cycle arrest in human KB/HeLa cells assessed as G1 phase accumulation at 100 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1465169 | Antiproliferative activity against human HeLa cells by SRB assay | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | Design, synthesis and biological evaluation of 2-phenylquinoline-4-carboxamide derivatives as a new class of tubulin polymerization inhibitors. |
| AID1435802 | Disruption of preformed spheroids in human PANC1 cells at 1 uM measured after 48 hrs by propidium staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1625806 | Binding affinity to microtubule in human HepG2 cells assessed as abnormal aggregation of chromosome at 200 nM after 24 hrs by immunofluorescence staining-based confocal microscopy | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1613462 | Inhibition of tubulin polymerization in human HeLa cells assessed as induction of shorter microtubule fibers at 0.05 uM after 12 hrs by DAPI staining-based confocal fluorescence microscopic analysis | |||
| AID613265 | Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetry analysis | 2011 | European 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. |
| AID1384278 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for human HT-29 cells | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID348003 | Cell cycle arrest in human KB/HeLa cells assessed as G2/M phase accumulation at 100 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1686605 | Toxicity in Balb/C mouse | 2016 | Journal 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. |
| AID551512 | Cytotoxicity against human HT-29 cells after 72 hrs by XTT/PMS method | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Tubulin photoaffinity labeling study with a plinabulin chemical probe possessing a biotin tag at the oxazole. |
| AID636393 | Cell cycle arrest in mouse B16F10 cells assessed as accumulation at Go/G1 phase at 1 ug/ml after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 68 %) | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis, biological evaluation and molecular docking studies of resveratrol derivatives possessing curcumin moiety as potent antitubulin agents. |
| AID404613 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | New C5-alkylated indolobenzazepinones acting as inhibitors of tubulin polymerization: cytotoxic and antitumor activities. |
| AID1906174 | Antiproliferation activity against human HeLa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay | |||
| AID303692 | Cytotoxicity against human RKO cells with ectopic-inducible expression of p27kip1 after 48 hrs by XTT assay | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID95519 | In vitro growth inhibition of KB, epidermoid carcinoma of the nasopharynx. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors. |
| AID605771 | Resistant ratio of IC50 for paclitaxel-resistant CHO-TAX 5-6 cells to IC50 for CHO cells | 2011 | Journal 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. |
| AID103260 | In vitro growth inhibition of MCF-7, breast adenocarcinoma. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors. |
| AID1435780 | Cytotoxicity against 2D culture of human A549 cells measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1407744 | Induction of apoptosis in human A375 cells assessed as necrotic cells at 1000 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.3%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID362356 | Binding affinity to pig brain tubulin at 10 uM after 15 mins relative to control | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | Structure-activity relationship studies on a novel class of antiproliferative agents derived from Lavendustin A. Part I: Ring A modifications. |
| AID94198 | The compound was tested for its cytotoxic concentration required to inhibit the replication of human tumor nasopharynx (KB-VIN) cell lines which is drug resistant | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20 | Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids. |
| AID277279 | Cytotoxicity against ZR-75-1 cell line | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Highly potent triazole-based tubulin polymerization inhibitors. |
| AID1492838 | Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. |
| AID282688 | Cell cycle arrest in HEK293EBNA cells by accumulation at S phase cell at 10 uM relative to DMSO | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Identification of novel and improved antimitotic agents derived from noscapine. |
| AID393414 | Cell cycle arrest in human K562 cells assessed as accumulation in G2/M phase at 10 uM after 24 hrs by flow cytometry analysis | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis and biological evaluation of novel symmetry bis-enediynes. |
| AID1236600 | Inhibition of pig microtubule polymerization after 30 mins by turbidimetric assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Synthesis and biological evaluation of diarylthiazole derivatives as antimitotic and antivascular agents with potent antitumor activity. |
| AID1736536 | Induction of apoptosis in human HT-29 cells assessed as late apoptotic cells at 1 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.0 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID553908 | Cell cycle arrest in human U266 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. |
| AID1500635 | Antiproliferative activity against human AGS cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of 9H-purins as potential tubulin polymerization inhibitors: Synthesis, biological evaluation and structure-activity relationships. |
| AID1189158 | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 31.25 nM after 24 hrs by Hoechst 33342 staining-based ArrayScanVTI analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1736484 | Cell cycle arrest in human HT29 cells assessed as cell accumulation at G1 phase at 1 uM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 69.19 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID274789 | Antiproliferative activity against NCI-H460 cells by XTT assay after 48 hrs | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID132744 | Percent increase in life-span against in vivo P388 murine leukemia at a dose 0.12 mg/kg in trail 2 | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID218985 | Compound was evaluated for inhibition of tubulin polymerization in bovine brain tubulin | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9 | The synthesis and evaluation of benzannelated-azatoxins: the benzazatoxins. |
| AID412963 | Growth inhibition of human HT-29 cells after 72 hrs by methylene blue dye assay | 2008 | Journal 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. |
| AID337650 | Cytotoxicity against human KBVIN cells in presence of 1 ug/ml vinblastine after 3 days by SRB assay | 1994 | Journal of natural products, Oct, Volume: 57, Issue:10 | Cytotoxic diterpenoids from Isodon megathyrsus. |
| AID758704 | Selectivity index, ratio of IC50 for human HuDe cells by MTT assay to IC50 for human K562 cells by trypan blue exclusion assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID711168 | Cytotoxicity against human HeLa cells expressing class 3 tubulin after 96 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID1585582 | Cytotoxicity against human A2780AD cells after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents. |
| AID1651321 | Inhibition of MSU-induced NLRP3 protein expression in synovial tissue of MSU-induced acute gout arthritis rat model at 10 mg/kg by western blot analysis | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Development of novel NLRP3-XOD dual inhibitors for the treatment of gout. |
| AID1785496 | Non-covalent binding affinity to tubulin (unknown origin) assessed as percentage in tubulin at 450 pmol incubated for 1 hr by UFLC-MS/MS analysis | |||
| AID1435804 | Disruption of preformed spheroids in human Colo-357 cells at 1 uM measured after 48 hrs by propidium staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1822507 | Antiproliferative activity against human Raji cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents. |
| AID1566322 | Cell cycle arrest in human MCF7 cells assessed as accumulation in subG1 phase at 5 times of antiproliferative IC50 incubated for 72 hrs by propidium iodide based flow cytometry (Rvb = 3.59 %) | |||
| AID665240 | Induction of mitotic arrest in human HeLa cells assessed as reduction in tubulin intensity by Hoechst 33342 staining | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | N⁴-Phenyl-substituted 2-acetylpyridine thiosemicarbazones: cytotoxicity against human tumor cells, structure-activity relationship studies and investigation on the mechanism of action. |
| AID602821 | Growth inhibition of human K562 cells after 48 hrs by trypan blue assay | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis, antiproliferative activity, and mechanism of action of a series of 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides. |
| AID347993 | Cell cycle arrest in human KB/HeLa cells assessed as S phase accumulation at 3.16 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1189141 | Antiproliferative activity against human A549 cells after 48 hrs by SRB method | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID336351 | Cytotoxicity against human Col2 cells | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID355580 | Antiproliferative activity against human HT-29 cells at 1 ug after 48 hrs by two-layer agar-diffusion method | |||
| AID1384280 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for human A549 cells | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID1817857 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and bioevaluation of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d]imidazoles as tubulin polymerization inhibitors. |
| AID336339 | Cytotoxicity against human KB cells | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID711172 | Induction of ABCG2 mRNA expression in human HT-29 cells at 1/10 IC50 to IC50 after 96 hrs by RT-PCR analysis | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID1549930 | Binding affinity to tubulin (unknown origin) assessed as dissociation constant by SPR analysis | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain. |
| AID1407716 | Antiproliferative activity against human Jurkat cells after 72 hrs by MTS assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1407729 | Induction of apoptosis in human A375 cells assessed as live cells at 1000 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 94.2%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID626620 | Antiproliferative activity against colchicine and vinblastine-resistant CHO-VV 3-2 cells after 48 hrs by SRB assay | 2011 | European 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. |
| AID101492 | In vitro inhibitory concentration against human chronic myelogenous leukemia K562 cell growth | 2003 | Journal 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. |
| AID730201 | Antiproliferative activity against activated HUVECs after 48 hrs by CCK-8 assay | 2013 | Journal 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. |
| AID1703292 | Binding affinity to pig brain tubulin at 37 degree C preincubated for 5 mins | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities. |
| AID749381 | Cytotoxicity against human PC3 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | The discovery of colchicine-SAHA hybrids as a new class of antitumor agents. |
| AID494521 | Inhibition of tubulin polymerization in human K562 cells | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis, antiproliferative activity and inhibition of tubulin polymerization by anthracenone-based oxime derivatives. |
| AID303719 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G1 phase at 0.3 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID661637 | Cytotoxicity against human HT-29 cells | 2012 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 22, Issue:11 | Bio-inspired synthesis and biological evaluation of a colchicine-related compound library. |
| AID1625715 | Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1316906 | Inhibition of [3H]colchicine binding to microtubule associated proteins free porcine brain alpha/beta-tubulin assessed as remaining radiolabeled binding at 100 uM measured after 5 mins by centrifugal gel filtration method relative to control | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Discovery of O |
| AID312975 | Growth inhibition of human HCT116 cells after 48 hrs | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions. |
| AID716401 | Induction of morphological changes in human HaCaT cells assessed as loss of radial distribution of structured microtubules at 10 '-6 M by confocal microscopy | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4. |
| AID347975 | Antiproliferative activity against human RKO cells by XTT assay | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1384287 | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 50 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 11 +/- 4%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID1296730 | Cytotoxicity against human THP1 cells after 24 hrs by Celltiter-Glo luminescent cell viability assay | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology. |
| AID132742 | Percent increase in life-span against in vivo P388 murine leukemia at a dose 0.06 mg/kg in trail 2 | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID1613461 | Inhibition of tubulin polymerization in human HeLa cells assessed as induction of microtubule fiber breakdown at 0.05 uM after 12 hrs by DAPI staining-based confocal fluorescence microscopic analysis | |||
| AID1898105 | Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID1882701 | Inhibition of bovine brain tubulin polymerization preincubated with compound followed by GTP addition and measured after 20 mins by turbidimetry-based spectrophotometric method | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Recent advances of antitumor shikonin/alkannin derivatives: A comprehensive overview focusing on structural classification, synthetic approaches, and mechanisms of action. |
| AID1625714 | Antiproliferative activity against human HCT116 cells after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1892876 | Destabilization of tubulin (unknown origin) assessed as melting temperature at 30 uM incubated for 20 mins by differential scanning fluorimetry (Rvb = 61.1 degC) | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13 | Small Molecules Promote Selective Denaturation and Degradation of Tubulin Heterodimers through a Low-Barrier Hydrogen Bond. |
| AID1237706 | Inhibition of tubulin (unknown origin) assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric analysis | 2015 | Journal 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. |
| AID247402 | Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5 | CHMIS-C: a comprehensive herbal medicine information system for cancer. |
| AID1566304 | Resistance index, ratio of IC50 of human LoVo/DX cells to IC50 of human LoVo cells | |||
| AID1899080 | Metabolic stability in human liver microsomes assessed as intrinsic clearance at 1 uM in presence of NADPH measured by LC-MS/MS analysis | |||
| AID1402704 | Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design and characterization of α-lipoic acyl shikonin ester twin drugs as tubulin and PDK1 dual inhibitors. |
| AID626619 | Ratio of IC50 for paclitaxel-resistant CHO-TAX 5-6 cells to IC50 for CHO cells | 2011 | European 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. |
| AID1822543 | Inhibition of tubulin polymerization in human A2780S cells assessed as microtubule spindle formation at 10 nM after 24 hrs by immunofluorescence analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents. |
| AID1566302 | Selectivity index, ratio of IC50 of mouse BALB/3T3 cells to IC50 of human LoVo cells | |||
| AID611264 | Cytotoxicity against ponasterone A-induced human RKOp27 cells with ectopic inducible expression of CDK inhibitor-kip1 after 48 hrs by XTT assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Phenylimino-10H-anthracen-9-ones as novel antimicrotubule agents-synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID1407712 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID303686 | Displacement of [3H]colchicine from biotinylated tubulin by scintillation proximity assay | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1736532 | Induction of apoptosis in human HT-29 cells assessed as late apoptotic cells at 0.5 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.0 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID637199 | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 5 ug/ml after 24 hrs by flow cytometric analysis (Rvb = 12%) | 2012 | Bioorganic & 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. |
| AID1898095 | Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID526943 | Displacement of [3H]-Colchicine from tubulin alpha/beta after 45 mins by scintillation proximity assay | 2010 | Journal 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. |
| AID605850 | Antiproliferative activity against human DLD1 cells after 48 hrs by alamar blue assay | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1333472 | Effect on Cdk2 mRNA expression in human MDA-MB-231 cells assessed as ratio of Cdk2 to GAPDH expression level at 5 uM after 24 hrs by RT-PCR method (Rvb = 0.26 No_unit) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1674009 | Cytotoxicity against human BHP-1 cells incubated for 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1898104 | Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID42553 | Inhibits the growth of the human Burkitt lymphoma CA46 cell | 1997 | Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6 | Antitumor agents. 172. Synthesis and biological evaluation of novel deacetamidothiocolchicin-7-ols and ester analogs as antitubulin agents. |
| AID1193494 | Thermodynamic equilibrium solubility, log S of the compound in simulated gastric fluid at pH 1.2 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
| AID1877705 | Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 4 uM measured after 36 hrs by flow cytometry (Rvb = 12.6%) | 2022 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 57 | Shikonin N-benzyl matrinic acid ester derivatives as novel telomerase inhibitors with potent activity against lung cancer cell lines. |
| AID595057 | Cell cycle arrest in mouse B16F10 cells assessed as accumulation at Go/G1 phase at 1 ug/ml after 24 hrs by flow cytometry (Rbv = 66.15%) | 2011 | Bioorganic & 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. |
| AID1431312 | Induction of microtubule depolymerization in human A549 cells at 100 nM after 4 hrs by immunofluorescence microscopic method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID75548 | Ability to inhibit the dibutyryl-cAMP-induced change of an immature glioma cell to a mature, differentiated astrocyte by in vitro astrocytoma assay at 10 ug/mL dose (Experiment #2); value may range from 91 to up | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | In vivo antitumor activity of 6-benzyl-1,3-benzodioxole derivatives against the P388, L1210, B16, and M5076 murine models. |
| AID1058421 | Cytotoxicity against human MDA-MB-468 cells assessed as cell viability after 4 days by MTS assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation. |
| AID1507350 | Cell cycle arrest in human HT-29 cells assessed as accumulation at G1 phase at 1.25 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 46.1 +/- 2.1%) | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Thiosemicarbazones and 4-thiazolidinones indole-based derivatives: Synthesis, evaluation of antiproliferative activity, cell death mechanisms and topoisomerase inhibition assay. |
| AID1395536 | Induction of apoptosis in human HT-29 cells assessed as necrotic cells at 40 nM after 48 hrs by Annexin V-FITC staining-based flow cytometric analysis (Rvb = 2 +/- 6%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID1058414 | Inhibition of CYP2C9 (unknown origin) at 3 uM | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation. |
| AID1832107 | Antiproliferative activity against human A549 assessed as reduction in cell viability measured after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors. |
| AID1704304 | Cytotoxicity against human HaCat cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID661636 | Cytotoxicity against human HT-29 cells after 96 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 22, Issue:11 | Bio-inspired synthesis and biological evaluation of a colchicine-related compound library. |
| AID658921 | Induction 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 %) | 2012 | Journal 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. |
| AID1221976 | Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1473710 | Antimigratory activity in human A375 cells assessed as wound closure at 25 nM after 22 hrs (Rvb = 60.7 +/- 3.5%) | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID758708 | Growth inhibition of human NCI-H460 cells after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID388959 | Toxicity in C57BL/J6 mouse assessed as liver aspartate aminotransferase level | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis. |
| AID337649 | Cytotoxicity against human KB cells after 3 days by SRB assay | 1994 | Journal of natural products, Oct, Volume: 57, Issue:10 | Cytotoxic diterpenoids from Isodon megathyrsus. |
| AID627395 | Antiproliferative activity against human CHO after 48 hrs by SRB assay | 2011 | European 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. |
| AID711183 | Cytotoxicity against human DLD1 cells after 96 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID1585586 | Ratio of IC50 for mouse NIH/3T3 cells harboring MDR G185 to IC50 for mouse NIH/3T3 cells | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents. |
| AID375808 | Induction of apoptosis in human H1299 cells assessed as caspase activation after 48 hrs by HTS assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylthieno[2,3-d]pyrimidines as potent apoptosis inducers. |
| AID518932 | Inhibition of tubulin in Acanthamoeba castellanii by alamar blue assay | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Molecular basis for resistance of acanthamoeba tubulins to all major classes of antitubulin compounds. |
| AID627401 | Antiproliferative activity against human HT1080 after 48 hrs by SRB assay | 2011 | European 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. |
| AID1416436 | Anti-inflammatory activity in C57BL6 mouse model of CCl4-induced hepatic fibrosis assessed as reduction in blue collagen fibers in hepatic tissue at 0.1 mg/kg, ig administered 2 times per week for 4 weeks by masson staining based assay | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 18α-Glycyrrhetinic acid monoglucuronide as an anti-inflammatory agent through suppression of the NF-κB and MAPK signaling pathway. |
| AID744711 | Antimitotic activity in human HeLa cells assessed as chromatin condensation after 24 hrs by Hoechst 33342 staining | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID679152 | TP_TRANSPORTER: drug resistance in Mrp1-expressing HEK293 cells | 1997 | Molecular pharmacology, Sep, Volume: 52, Issue:3 | Pharmacological characterization of the murine and human orthologs of multidrug-resistance protein in transfected human embryonic kidney cells. |
| AID1863113 | Binding affinity to beta-tubulin colchicine binding site in human SGC-7901 cells assessed as inhibition of EBI-beta-tubulin adduct band formation at 10 uM preincubated for 2 hrs followed by EBI addition and measured after 2 hrs by EBI competition based We | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway. |
| AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1185443 | Inhibition of tubulin (unknown origin) polymerization by spectrophotometry | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Concise syntheses of 7-anilino-indoline-N-benzenesulfonamides as antimitotic and vascular disrupting agents. |
| AID1201721 | Inhibition of recombinant human HDAC3 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 hrs by fluorescence assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID249637 | Effect to arrest GI-phase on HEK 293 cells at 10 uM was determined | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Discovery of S-phase arresting agents derived from noscapine. |
| AID774673 | Cytotoxicity against human H460 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18 | New phenstatin-fatty acid conjugates: synthesis and evaluation. |
| AID1519872 | Cytotoxicity against human MCF7 cells assessed as reduction in cell growth incubated for 96 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structure-activity relationship studies and in vitro and in vivo anticancer activity of novel 3-aroyl-1,4-diarylpyrroles against solid tumors and hematological malignancies. |
| AID1668780 | Effect on mitochondria parameters in Parkinson's disease patient derived human ONS cells at 10 uM after 24 hrs by MitoTracker Orange CMTMRos staining based fluorescence assay | 2020 | Journal of natural products, 05-22, Volume: 83, Issue:5 | A Grand Challenge. 3. Unbiased Phenotypic Function of Metabolites from Australia Plants |
| AID1737760 | Inhibition of porcine brain tubulin polymerization assessed as inhibition of microtubule assembly by measuring decrease in absorbance at 10 uM measured for 60 mins by fluorescence based analysis | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Design, synthesis and anticancer properties of isocombretapyridines as potent colchicine binding site inhibitors. |
| AID1703289 | Inhibition of pig brain tubulin polymerization measured by light scattering based spectrophotometer method | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities. |
| AID150758 | P-gp activity was measured by a direct transport assay, using polarized LLC-PK1 epithelial cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID642528 | Growth inhibition of human KB cells after 72 hrs by methylene blue assay | 2011 | Journal 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. |
| AID1407736 | Induction of apoptosis in human A375 cells assessed as necrotic cells at 10 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.3%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID288667 | Inhibition of tubulin polymerization | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies. |
| AID377075 | Toxicity in brine shrimp | 2005 | Journal of natural products, Feb, Volume: 68, Issue:2 | New colchicinoids from a native Jordanian meadow saffron, colchicum brachyphyllum: isolation of the first naturally occurring dextrorotatory colchicinoid. |
| AID1389595 | Inhibition of MSU-induced TNFalpha level in serum of acute gouty arthritis Sprague-Dawley rat model at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last dose measured up to 24 hrs by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID23461 | Partition coefficient (logP) | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Quantitative structure-activity relationships of colchicines against P388 leukemia in mice. |
| AID1500602 | Antiproliferative activity against human LO2 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents. |
| AID1883549 | Binding affinity to beta-tubulin colchicine binding site in human MGC-803 cells assessed as decrease in beta-tubulin adduct band at 10 uM incubated for 2 hrs by EBI alkylate competition assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID626622 | Antiproliferative activity against human multidrug-resistant CEM/VLB cells after 48 hrs by SRB assay | 2011 | European 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. |
| AID1435791 | Induction of beta-tubulin expression in human Colo-357 cells at 1 uM measured after 24 hrs by Hoechst 33342 staining based confocal microscopic analysis | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID538698 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase after 24 hrs by flow cytometry relative to control | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Synthesis, molecular modeling and biological evaluation of guanidine derivatives as novel antitubulin agents. |
| AID1389603 | Inhibition of MSU-induced caspase-1 protein level in synovial homogenate of acute gouty arthritis Sprague-Dawley rat model at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last dose measured up to 24 hrs by Wester | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID274813 | Cell cycle arrest in KB/HeLa cells by accumulation at S phase at 10 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID486600 | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | Synthesis, molecular modeling and biological evaluation of dithiocarbamates as novel antitubulin agents. |
| AID1406859 | Antiproliferative activity against human MGC803 cells after 48 hrs by MTT assay | |||
| AID612320 | Antiproliferative activity against human PPC1 cells after 96 hrs by sulforhodamine B assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis and antiproliferative activity of novel 2-aryl-4-benzoyl-imidazole derivatives targeting tubulin polymerization. |
| AID394855 | Cytotoxicity against human PPC1 cells after 48 hrs by SRB assay | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships. |
| AID1625805 | Disruption of microtubule network in cytosol of human HepG2 cells at 200 nM after 24 hrs by immunofluorescence staining-based confocal microscopy | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1058423 | Cytotoxicity against human BT474 cells assessed as cell viability after 4 days by MTS assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation. |
| AID1189592 | Depolymerization of microtubule cytoskeleton in human A549 cells at 50 nM after 24 hrs by hoechst 33342-based fluorescence microscopy | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID357047 | Cytotoxicity against human HeLa cells after 72 hrs by MTT assay | 2001 | Journal of natural products, Jul, Volume: 64, Issue:7 | Isolation and bioactivities of constitutents of the roots of Garcinia atroviridis. |
| AID1333459 | Induction of apoptosis in human MDA-MB-231 cells assessed as late apoptotic cells at 5 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.8%) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID347994 | Cell cycle arrest in human KB/HeLa cells assessed as G2/M phase accumulation at 3.16 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID355583 | Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay | |||
| AID1179659 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 1 ug/ml after 24 hrs by flow cytometry (Rvb = 62.34 %) | 2014 | Bioorganic & 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. |
| AID347972 | Antiproliferative activity against human SKOV3 cells by XTT assay | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID612319 | Antiproliferative activity against human DU145 cells after 96 hrs by sulforhodamine B assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis and antiproliferative activity of novel 2-aryl-4-benzoyl-imidazole derivatives targeting tubulin polymerization. |
| AID1414062 | Fungicidal activity against Penicillium cyclopium Westling after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID483369 | Cytotoxicity against human PC3 cells after 72 hrs by crystal violet staining | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Syntheses and biological evaluation of ring-C modified colchicine analogs. |
| AID1221973 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1413548 | Inhibition of tubulin beta polymerization in human MCF7 cells after 48 hrs by ELISA | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | Synthesis and biological evaluation of novel 5-chloro- |
| AID1807387 | Cytotoxicity against human M14 cells measured after 72 hrs by western blot | |||
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| AID383994 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of 2N cells at 2 uM after 72 hrs by flow cytometry | 2008 | Journal 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. |
| AID1701001 | Induction of apoptosis in human HepG2 cells assessed as PARP cleavage at 20 nM incubated for 24 hrs by western blot analysis | |||
| AID611265 | Cytotoxicity against human KB/HeLa cells after 48 hrs by XTT assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Phenylimino-10H-anthracen-9-ones as novel antimicrotubule agents-synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID1860526 | Antiproliferative activity against human FaDu cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC. |
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| AID758693 | Induction of apoptosis in human HepG2 cells assessed as necrotic cells at 10 uM after 72 hrs by annexin V-FITC/PI staining-based FACS flow cytometric analysis (Rvb = 0.7 +/- 0.2%) | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID1470810 | Growth inhibition of human K562 cells at 10 uM after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Anthranilamide-based 2-phenylcyclopropane-1-carboxamides, 1,1'-biphenyl-4-carboxamides and 1,1'-biphenyl-2-carboxamides: Synthesis biological evaluation and mechanism of action. |
| AID335772 | Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 20 ug/mL | 1993 | Journal of natural products, Oct, Volume: 56, Issue:10 | Cytotoxic constituents from Hyptis verticillata. |
| AID1498598 | Inhibition of porcine MAP-rich tubulin polymerization at 20 uM measured every 30 secs for 30 mins | 2018 | Bioorganic & 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. |
| AID473624 | Antiproliferative activity against human U937 cells by sulforhodamine B assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | N-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)arylamide as a new scaffold that provides rapid access to antimicrotubule agents: synthesis and evaluation of antiproliferative activity against select cancer cell lines. |
| AID1420818 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | |||
| AID1785494 | Non-covalent binding affinity to tubulin (unknown origin) assessed as percentage in filtrate at 450 pmol incubated for 1 hr by UFLC-MS/MS analysis | |||
| AID274784 | Antiproliferative activity against human K562 cell line | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1897647 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 12-15, Volume: 76 | Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities. |
| AID1758692 | Cytotoxicity against human A549 cells assessed as reduction in cell growth by CCK8 assay | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Synthesis and structure-activity relationships of 5-phenyloxazole-2-carboxylic acid derivatives as novel inhibitors of tubulin polymerization. |
| AID1819686 | Inhibition of porcine brain tubulin polymerization at 10 uM measured for 60 mins by spectrophotometric method relative to control | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Design, Synthesis, and Biological Evaluation of Apcin-Based CDC20 Inhibitors. |
| AID1221963 | Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
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| AID1785482 | Induction of microtubule (unknown origin) depolymerization at 5 uM measured for 55 mins by absorbance method | |||
| AID1191356 | Cytotoxicity against human DU145 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and structure-activity relationships of pyridinyl-1H-1,2,3-triazolyldihydroisoxazoles as potent inhibitors of tubulin polymerization. |
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| AID1226630 | Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 100 nM after 24 hrs by propidium iodide staining based flow cytometry | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10 | Methyl 3-((6-methoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)amino)benzoate (GN39482) as a tubulin polymerization inhibitor identified by MorphoBase and ChemProteoBase profiling methods. |
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| AID1382777 | Antiproliferative activity against human HMEC1 cells after 4 days by coulter counting method | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity. |
| AID347581 | Antiproliferative activity against human K562 cells after 48 hrs | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
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| AID1272833 | Inhibition of N-terminal MKLP2 (56 to 505 residues) ATPase basal activity isolated from human hepatocellular carcinoma cells up to 100 uM by pyruvate kinase/lactate dehydrogenase enzyme linked assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | New MKLP-2 inhibitors in the paprotrain series: Design, synthesis and biological evaluations. |
| AID1785486 | Induction of mitotic block in human A2780S cells at 100 uM incubated for 12 hrs | |||
| AID9451 | Cytotoxicity against Beta- tubulin mutant expressing A9-PTX10 cell line of humans was tested | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20 | Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids. |
| AID1651297 | Antiarthritic activity against MSU-induced acute gout arthritis rat model assessed as degree of ankle joint swelling after 2 hrs (Rvb = 7.5 +/- 1.6 No_unit) | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Development of novel NLRP3-XOD dual inhibitors for the treatment of gout. |
| AID1167536 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 0.1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 31%) | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Synthesis and antiproliferative activity of 6-phenylaminopurines. |
| AID1736478 | Cell cycle arrest in human HT29 cells assessed as cell accumulation at G1 phase at 0.25 uM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 69.19 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
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| AID758700 | Cell cycle arrest in human K562 cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs by annexin V-FITC/PI staining-based FACS flow cytometric analysis (Rvb = 28.9 +/- 1.3%) | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID732806 | Cytotoxicity against human PC3 cells assessed as growth inhibition | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Design, synthesis, biological evaluation and molecular modeling studies of 1-aryl-6-(3,4,5-trimethoxyphenyl)-3(Z)-hexen-1,5-diynes as a new class of potent antitumor agents. |
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| AID1395533 | Antiproliferative activity against human HEK293 cells after 2 days by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID212934 | In vitro minimum inhibition concentration to inhibit the regeneration of cilia in Tetrahymena pyriformis W. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Absolute structure-cytotoxic activity relationships of steganacin congeners and analogues. |
| AID1500598 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents. |
| AID761835 | Inhibition of bovine brain tubulin polymerization incubated for 15 mins prior to GTP addition measured after 20 mins by spectrophotometry | 2013 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16 | Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity. |
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| AID159533 | In vitro inhibition of maximum porcine tubulin assembly rate after 20 min at 37 degrees C | 2003 | Journal 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. |
| AID1771031 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID711185 | Binding affinity to pig brain tubulin | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID19468 | Partition coefficient (logP) | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID1189147 | Antiproliferative activity against taxol-resistant human A2780 cells after 48 hrs by SRB method | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1566301 | Selectivity index, ratio of IC50 of mouse BALB/3T3 cells to IC50 of human MCF7 cells | |||
| AID758706 | Growth inhibition of human HT-29 cells after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID28235 | Unbound fraction (plasma) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID404658 | Antitumor activity against human U87 tumor transplanted in chick chorio-allantoic membrane assessed as reduction of tumor volume at 10 uM after 4 days | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | New C5-alkylated indolobenzazepinones acting as inhibitors of tubulin polymerization: cytotoxic and antitumor activities. |
| AID303724 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G1 phase at 100 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1189155 | Drug resistance index, ratio of IC50 for doxorubicin-resistant human MCF7 cells to IC50 for human MCF7 cells | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1535574 | Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay | 2019 | Bioorganic & 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. |
| AID1883540 | Disruption of microtubule network in human MGC-803 cells assessed as cytoskeleton disruption at 25 nM measured after 48 hrs by DAPI staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID1750233 | Antiproliferative activity against human A2780T cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | |||
| AID1722127 | Inhibition of tubulin polymerization in human HCT-116 cells assessed as cell cycle arrest at G1/G0 phase at 12.5 uM measured after 24 hrs by propidium iodide staining based analysis (Rvb = 50.1 %) | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines. |
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| AID1320439 | Disruption of interphase microtubule in HUVEC assessed as formation of actin stress fiber at 1 uM preincubated for 30 mins followed by compound washout measured after 60 mins by DAPI staining-based immunofluorescence assay | 2016 | Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20 | Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4. |
| AID1235360 | Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes. |
| AID1221974 | Fold activity change at MRP2 ATPase (unknown origin) relative to control | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1549934 | Inhibition of tubulin polymerization in human HeLa cells assessed as contracted and rounded cells with disordered abnormal spindles and chromosomal misalignment at 500 nM after 24 hrs by immunofluorescence based confocal microscopy | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain. |
| AID1566296 | Antiproliferative activity against human LoVo cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay | |||
| AID1754735 | Antiproliferative activity against mouse BALB/3T3 cells assessed as inhibition of proliferation after 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Synthesis and antiproliferative screening of novel doubly modified colchicines containing urea, thiourea and guanidine moieties. |
| AID758692 | Induction of apoptosis in human HepG2 cells assessed as ratio of apoptotic to dead cells at 10 uM after 72 hrs by annexin V-FITC/PI staining-based FACS flow cytometric analysis | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID744718 | Cytotoxicity against mouse L1210 cells after 24 hrs by MTT assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID1414049 | Antifungal activity against Aspergillus niger van Tiegen BAM4 ATCC 6275 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1562380 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin. |
| AID1736451 | Antiproliferative activity against drug-resistant human MCF7 cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID275870 | Induction of apoptosis in HeLa cells assessed as effect on sub-G1 population | 2007 | Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2 | Synthesis and SAR of [1,2,4]triazolo[1,5-a]pyrimidines, a class of anticancer agents with a unique mechanism of tubulin inhibition. |
| AID1435796 | Induction of mitochondrial membrane hyperpolarization in 3D culture of human Colo-357 cells at 1 uM measured after 48 hrs by DiOC6 dye based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID418790 | Growth inhibition of human HCT116 cells after 48 hrs | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Discovery and structure-activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers. |
| AID337651 | Cytotoxicity against human KBVIN cells after 3 days by SRB assay | 1994 | Journal of natural products, Oct, Volume: 57, Issue:10 | Cytotoxic diterpenoids from Isodon megathyrsus. |
| AID1153765 | Cytotoxicity against HEK293 cells after 48 hrs by MTS assay | 2014 | Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13 | Synthesis of a novel legumain-cleavable colchicine prodrug with cell-specific toxicity. |
| AID657610 | Inhibition of bovine tubulin polymerization after 20 mins by spectrophotometry | 2012 | Bioorganic & 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. |
| AID1785503 | Antiproliferative activity against human HeLa cells incubated for 72 hrs by MTT assay | |||
| AID758702 | Cell cycle arrest in human K562 cells assessed as accumulation at G0/G1 phase at 10 uM after 24 hrs by annexin V-FITC/PI staining-based FACS flow cytometric analysis (Rvb = 40 +/- 1.2%) | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID1586075 | Displacement of [3H]-colchicine from bovine brain tubulin at 1 uM by scintillation proximity assay relative to control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
| AID1756945 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | An insight into the anticancer potential of carbamates and thiocarbamates of 10-demethoxy-10-methylaminocolchicine. |
| AID1704309 | Induction of cell cycle arrest in human COLO357 cells assessed as accumulation at apoptotic phase at 5 nM incubated for 48 hrs by RNase/PI staining based flow cytometry analysis (Rvb = 1.3 %) | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1860217 | Apparent permeability across apical to basolateral side in human Caco-2 cells assessed as drug recovery at pH 6.5 to 7.4 | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of new quinoline derivatives as selective C-RAF kinase inhibitors with potent anticancer activity. |
| AID271653 | Cytotoxicity against human KB cell line by methylene blue dye assay | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents. |
| AID214730 | Inhibitory binding percentage of compound towards colchicine site in tubulin using tubulin-[3H]colchicine as radioligand at a concentration of 100 uM | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity. |
| AID1416437 | Anti-inflammatory activity in C57BL6 mouse model of CCl4-induced hepatic fibrosis assessed as reduction in hepatic fibrosis at 0.1 mg/kg, ig administered 2 times per week for 4 weeks by H and E staining based assay | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 18α-Glycyrrhetinic acid monoglucuronide as an anti-inflammatory agent through suppression of the NF-κB and MAPK signaling pathway. |
| AID1191355 | Cytotoxicity against human A549 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and structure-activity relationships of pyridinyl-1H-1,2,3-triazolyldihydroisoxazoles as potent inhibitors of tubulin polymerization. |
| AID1756948 | Cytotoxicity against mouse BALB/3T3 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | An insight into the anticancer potential of carbamates and thiocarbamates of 10-demethoxy-10-methylaminocolchicine. |
| AID1625716 | Solubility of the compound in 2.5% ethanol/2.5% Tween-80 at 1 mg | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID281503 | Inhibition of tubulin polymerization | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Arylthioindoles, potent inhibitors of tubulin polymerization. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1421774 | Selectivity index, ratio of IC50 for mouse L929 cells to IC50 for human A549 cells | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Conformation impacts on the bioactivities of SMART analogues. |
| AID150757 | P-gp activity was measured by a direct transport assay, using polarized LLC-MDR1 epithelial cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID1503402 | Cytotoxic activity in human MIAPaCa2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID711181 | Cytotoxicity against human HT-29 cells after 96 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID1771059 | Binding affinity to immobilized bovine brain tubulin by SPR assay | |||
| AID735021 | Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells in G2/M phase at 8 uM concentration after 24 hrs by propidium iodide staining based cytofluorimetric analysis (Rvb = 12.95%) | 2013 | European 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. |
| AID699541 | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID326375 | Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by SRB assay | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Docking and hydropathic scoring of polysubstituted pyrrole compounds with antitubulin activity. |
| AID1882732 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 24 hrs in presence of foetal bovine serum by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Recent advances of antitumor shikonin/alkannin derivatives: A comprehensive overview focusing on structural classification, synthetic approaches, and mechanisms of action. |
| AID348006 | Cell cycle arrest in human KB/HeLa cells assessed as G2/M phase accumulation at 316 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID383982 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of 4N cells at 2 uM after 24 hrs by flow cytometry | 2008 | Journal 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. |
| AID342594 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 2 times GI50 after 24 hrs by flow cytometry | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Selective alkylation of beta(II)-tubulin and thioredoxin-1 by structurally related subsets of aryl chloroethylureas leading to either anti-microtubules or redox modulating agents. |
| AID1435404 | Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and cytotoxic activity of certain novel chalcone analogous compounds. |
| AID422581 | Inhibition of tubulin polymerization | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and evaluation of 3-aroylindoles as anticancer agents: metabolite approach. |
| AID1562381 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin. |
| AID81367 | Inhibition of HeLa cell proliferation | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID262911 | Inhibition of tubulin polymerization | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Benzoylphenylurea sulfur analogues with potent antitumor activity. |
| AID636071 | Cell cycle arrest in mouse B16F10 cells assessed as accumulation at S phase at 1 ug/ml after 24 hrs by flow cytometry analysis (Rvb = 9.97 %) | 2012 | Bioorganic & 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. |
| AID1492843 | Antiproliferative activity against human DAN-G cells after 96 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. |
| AID1695285 | Toxicity in iv dosed C57BL/6 mouse assessed as lethal dose measured after 40 to 48 hrs | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
| AID348000 | Cell cycle arrest in human KB/HeLa cells assessed as G2/M phase accumulation at 31.6 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID101610 | Inhibition of MCF-7 cell proliferation | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID721880 | Cytotoxicity against human HT-29 cells assessed as growth inhibition after 48 hrs by MTT assay | 2013 | Journal 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. |
| AID1435788 | Induction of apoptosis in 3D culture of human Colo-357 cells assessed as accumulation at G2/M phase at 1 uM measured after 72 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1695283 | Induction of apoptosis in human L929 cells at 5 uM incubated for 72 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 1.2 %) | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
| AID303703 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at S phase at 3.16 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1221956 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID208873 | Cytotoxicity against human central nervous system carcinoma TE671 cell line | 1993 | Journal 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 |
| AID1428411 | Cytotoxicity against multidrug resistant human MCF7 cells cultured in vinblastine containing medium assessed as growth inhibition after 72 hrs by SRB assay | |||
| AID1183716 | Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy | 2014 | Journal 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. |
| AID612423 | Cell cycle arrest in mouse B16F10 cells assessed as accumulation at G0/G1 phase at 1 ug/ml after 24 hrs by flow cytometry analysis (Rvb = 48.57%) | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis, biological evaluation, and molecular modeling of cinnamic acyl sulfonamide derivatives as novel antitubulin agents. |
| AID719104 | Cytotoxicity against multidrug-resistant human A2780AD cells overexpressing p-gp assessed as growth inhibition | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation. |
| AID605765 | Antiproliferative activity against human DU145 cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID697553 | Antiproliferative activity against human WM164 cells after 48 hrs by SRB assay | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16 | Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents. |
| AID1821598 | Inhibition of tubulin polymerization in human KYSE-30 cells assessed as microtubule assembly at 0.01 uM measured after 48 hrs by immunofluorescence assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis and evaluation of novel bis-substituted aromatic amide dithiocarbamate derivatives as colchicine site tubulin polymerization inhibitors with potent anticancer activities. |
| AID1625739 | Cytotoxicity against P-gp overexpressing human MCF7/ADR cells assessed as reduction in cell growth after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID733783 | Cytotoxicity against human DU145 cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID331407 | Cell cycle arrest in human MCF7 cells assessed as increase in S phase accumulation at 0.1 uM after 16 hrs by FACS analysis | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Cycloalkyl-substituted aryl chloroethylureas inhibiting cell cycle progression in G0/G1 phase and thioredoxin-1 nuclear translocation. |
| AID553906 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. |
| AID1354605 | Inhibition of cell migration in human MDA-MB-231 cells at 2 uM incubated for 24 hrs by scratch wound healing assay relative to control | 2018 | Journal of natural products, 05-25, Volume: 81, Issue:5 | Inhibition of Breast Cancer Cell Migration by Cyclotides Isolated from Pombalia calceolaria. |
| AID716404 | Induction of morphological changes in human HaCaT cells assessed as cell rounding at 10 '-6 M by confocal microscopy | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4. |
| AID1566336 | Induction of cell cycle arrest in human ALL5 cells assessed as increase in 4 N DNA at 5 times of antiproliferative IC50 incubated for 48 hrs by propidium iodide based flow cytometry | |||
| AID620725 | Inhibition of bovine tubulin polymerization at 3 uM after 1 hr by fluorescence assay relative to control | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Design and synthesis of resveratrol-based nitrovinylstilbenes as antimitotic agents. |
| AID770272 | Induction of microtubule depolymerization in rat REF52 cells assessed as decrease in ratio of soluble to insoluble tubulin fraction at 0.1 uM after 30 mins by Western blot analysis | 2013 | Journal of natural products, Sep-27, Volume: 76, Issue:9 | Enantioselective effects of (+)- and (-)-citronellal on animal and plant microtubules. |
| AID228460 | Inhibition of tubulin polymerization activity using homogenous bovine brain tubulin at 45 degree C | 1999 | Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3 | The synthesis and evaluation of temperature sensitive tubulin toxins. |
| AID1527071 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
| AID695812 | Cytotoxicity against human HepG2 cells after 48 hrs | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis and biological evaluation of a series of podophyllotoxins derivatives as a class of potent antitubulin agents. |
| AID296584 | Effect on thrombin-induced human platelet aggregation at 0.1 uM | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16 | Characterization of the intracellular mechanisms involved in the antiaggregant properties of cinnamtannin B-1 from bay wood in human platelets. |
| AID1694410 | Antiproliferative activity against mouse BALB/3T3 cells incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
| AID1694414 | Cell cycle arrest in human ALL-5 cells assessed as accumulation at sub-G1 phase after 72 hrs at 5 times of IC50 by propidium iodide staining-based flow cytometric analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
| AID274802 | Displacement of [3H]colchicine from tubulin by SPA assay | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1771032 | Antiproliferative activity against human A549/Taxol cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID1700960 | Inhibition of N,N'-Ethylenebis(iodoacetamide) binding to beta-tubulin in human HepG2 cells assessed as reduction in EBI/beta-tubulin adduct formation at 5 uM preincubated for 2 hrs followed by EBI addition and measured after 1.5 hrs by Western blot analys | |||
| AID1058412 | Inhibition of CYP3A4 (unknown origin) at 3 uM | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation. |
| AID368408 | Cytotoxicity against human A549 cells after 24 hrs by propidium iodide assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Isolation, structure elucidation and cytotoxic evaluation of endiandrin B from the Australian rainforest plant Endiandra anthropophagorum. |
| AID87604 | In vitro inhibitory activity against HeLa/KB cells using XTT proliferation assay. | 2001 | Journal of medicinal chemistry, Dec-20, Volume: 44, Issue:26 | Synthetic 2-aroylindole derivatives as a new class of potent tubulin-inhibitory, antimitotic agents. |
| AID626623 | Ratio of IC50 for human multidrug-resistant CEM/VLB cells to IC50 for human CEM cells | 2011 | European 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. |
| AID658920 | Induction 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 %) | 2012 | Journal 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. |
| AID347997 | Cell cycle arrest in human KB/HeLa cells assessed as G2/M phase accumulation at 10 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID770279 | Induction of microtubule depolymerization in rat REF52 cells at 0.1 uM after 30 mins by fluorescence assay | 2013 | Journal of natural products, Sep-27, Volume: 76, Issue:9 | Enantioselective effects of (+)- and (-)-citronellal on animal and plant microtubules. |
| AID277280 | Cytotoxicity against HeLa cell line | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Highly potent triazole-based tubulin polymerization inhibitors. |
| AID1532042 | Inhibition of bovine brain tubulin polymerization after 20 mins in presence of GTP by spectrophotometric analysis | 2018 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24 | Optimization of substituted cinnamic acyl sulfonamide derivatives as tubulin polymerization inhibitors with anticancer activity. |
| AID1527073 | Antiproliferative activity against human LoVo cells assessed as reduction in cell viability | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
| AID1473701 | Cytotoxicity against human M14 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID1807388 | Cytotoxicity against paclitaxel resistant human M14 cells measured after 72 hrs by western blot | |||
| AID1628431 | Induction of apoptosis in human A549 cells assessed as early apoptotic cells level at 40 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FACS flow cytometry (Rvb = 0.65%) | 2016 | Journal 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. |
| AID95339 | Cytotoxicity was evaluated against KB CV-60 cells at 0.1 ug/mL; No cytotoxicity | 2000 | Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22 | Synthesis and evaluation of 4-deacetoxyagosterol A as an MDR-modulator. |
| AID422580 | Displacement of [3H]colchicine from tubulin after 1 hr by scintillation counter | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and evaluation of 3-aroylindoles as anticancer agents: metabolite approach. |
| AID342520 | Induction of morphological changes in human EA.hy 926 cells assessed as rounding up after 2 hrs | 2008 | Bioorganic & 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. |
| AID1414042 | Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1625735 | Cytotoxicity against beta-tubulin 3 overexpressing human A2780T cells assessed as reduction in cell growth after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
| AID1704320 | Inhibition of lamb brain tubulin polymerization assessed as reduction in microtubule assembly at 1 to 7 uM incubated for 40 mins at 4 degreeC by spectrophotometric analysis relative to control | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1905068 | Inhibition of [3H]colchicine binding to tubulin (unknown origin) by competitive binding assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Discovery of a Novel Stilbene Derivative as a Microtubule Targeting Agent Capable of Inducing Cell Ferroptosis. |
| AID711173 | Induction of ABCB1 mRNA expression in human HT-29 cells at 1/10 IC50 to IC50 after 96 hrs by RT-PCR analysis | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID1504731 | Cytotoxicity in human NCI-H157 cells assessed as reduction in cell viability after 4 days under dark condition by MTT assay | |||
| AID605763 | Antiproliferative activity against mouse P388D1 cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID733792 | Cytotoxicity against human H460 cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID1822505 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents. |
| AID2955 | Cytotoxicity against ovarian cancer cell line (1A-9) of humans was determined | 2002 | Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20 | Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids. |
| AID719102 | Cytotoxicity against human HeLa cells assessed as growth inhibition | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation. |
| AID1860528 | Inhibition of tubulin polymerization (unknown origin) by fluorescence based analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC. |
| AID1593960 | Cell cycle arrest in human PHK160b cells assessed as accumulation at G0/G1 phase at 50 uM incubated for 48 hrs by propidium iodide staining-based flow cytometry | |||
| AID716408 | Induction of microtubule depolymerization in human SKv-a cells at 10 '-6 M by confocal microscopy | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4. |
| AID1698824 | Antimitotic 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 analysis | 2020 | Bioorganic & 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. |
| AID637149 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2012 | Bioorganic & 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. |
| AID303685 | Inhibition of porcine brain tubulin polymerization | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID235405 | Therapeutic ratio was determined for peroral administration | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Synthesis and antiinflammatory activity of hexahydrothiopyrano[4,3-c]pyrazoles and related analogues. |
| AID1437254 | Inhibition of porcine tubulin assembly measured for 30 mins by UV/visible spectrophotometric method | 2017 | Bioorganic & 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. |
| AID1651323 | Inhibition of MSU-induced caspase-1 protein expression in synovial tissue of MSU-induced acute gout arthritis rat model at 10 mg/kg by western blot analysis | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Development of novel NLRP3-XOD dual inhibitors for the treatment of gout. |
| AID761195 | Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14 | Novel synthetic acridine derivatives as potent DNA-binding and apoptosis-inducing antitumor agents. |
| AID1333452 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1722124 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines. |
| AID336342 | Cytotoxicity against human A431 cells | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID355586 | Antiproliferative activity against mouse P388 cells at 0.01 ug after 48 hrs by two-layer agar-diffusion method | |||
| AID1736534 | Induction of apoptosis in human HT-29 cells assessed as viable cells at 1 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 98.3 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID331396 | Antiproliferative activity against human HT29 cells | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Cycloalkyl-substituted aryl chloroethylureas inhibiting cell cycle progression in G0/G1 phase and thioredoxin-1 nuclear translocation. |
| AID1198464 | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S phase after 24 hrs by flow cytometry (Rvb = 14.58%) | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents. |
| AID1625807 | Inhibition of microtubule polymerization in human HepG2 cells after 24 hrs by immunofluorescence staining-based confocal microscopy | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID612425 | Cell cycle arrest in mouse B16F10 cells assessed as accumulation at G2/M phase at 1 ug/ml after 24 hrs by flow cytometry analysis (Rvb = 17.03%) | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis, biological evaluation, and molecular modeling of cinnamic acyl sulfonamide derivatives as novel antitubulin agents. |
| AID657607 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2012 | Bioorganic & 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. |
| AID123252 | Toxicity found after a single intramuscular injection in mice | 1983 | Journal of medicinal chemistry, Oct, Volume: 26, Issue:10 | Biological effects of modified colchicines. 2. Evaluation of catecholic colchicines, colchifolines, colchicide, and novel N-acyl- and N-aroyldeacetylcolchicines. |
| AID1785460 | Antiproliferative activity against human A2780S cells incubated for 72 hrs by MTT assay | |||
| AID214008 | Inhibition of Tubulin polymerization by a 40 uM solution of compound; compound showed inhibition >50% at 40 uM | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Methoxy-substituted 3-formyl-2-phenylindoles inhibit tubulin polymerization. |
| AID1503405 | Induction of cell cycle arrest in human Colo-357 cells assessed as accumulation at G2/M phase at 5 uM incubated for 72 hrs by propidium iodide staining based flow cytometry (Rvb = 31%) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID1503417 | Gastrointestinal toxicity in human HT-29 cells assessed as increase in mitochondrial membrane potential at 5 uM incubated for 3 hrs by flow cytometry | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID1333455 | Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells at 5 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.6%) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID611267 | Antiproliferative activity against human K562 cells after 48 hrs by hemocytometer | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Phenylimino-10H-anthracen-9-ones as novel antimicrotubule agents-synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID377072 | Cytotoxicity against human MCF7 after 3 days by SRB assay | 2005 | Journal of natural products, Feb, Volume: 68, Issue:2 | New colchicinoids from a native Jordanian meadow saffron, colchicum brachyphyllum: isolation of the first naturally occurring dextrorotatory colchicinoid. |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID1771034 | Antiproliferative activity against human LCC6MDR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID1189603 | Inhibition of purified tubulin (unknown origin) assessed as critical concentration of tubulin required to produce assembly at 0.5 uM after 30 mins by spectrophotometry (Rvb = 3.3 +/- 0.1 uM) | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID1507351 | Cell cycle arrest in human HT-29 cells assessed as accumulation at S phase at 1.25 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 17.2 +/- 1.2%) | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Thiosemicarbazones and 4-thiazolidinones indole-based derivatives: Synthesis, evaluation of antiproliferative activity, cell death mechanisms and topoisomerase inhibition assay. |
| AID1700537 | Cell cycle arrest in mouse 518T2 cells assessed as increase in accumulation at G2/M-phase at 300 nM measured after 24 hrs by propidium iodide staining based flow cytometry | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | A Multipronged Approach Establishes Covalent Modification of β-Tubulin as the Mode of Action of Benzamide Anti-cancer Toxins. |
| AID1179661 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 1 ug/ml after 24 hrs by flow cytometry (Rvb = 24.61 %) | 2014 | Bioorganic & 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. |
| AID235165 | Selectivity ratio expressed as temperature dependence at 45 Degree C to that of 30 Degree C in bovine brain tubulin | 1999 | Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3 | The synthesis and evaluation of temperature sensitive tubulin toxins. |
| AID1395569 | Effect on VEGF gene expression in human HT-29 cells assessed as VEGF level at 25 nM after 48 hrs by RT-qPCR analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID123247 | Toxicity found after a single im injection. The total number of deaths were counted after 7 days and LD50 was determined by probit analysis; 2.5-4.0 | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Biological effects of modified colchicines. Improved preparation of 2-demethylcolchicine, 3-demethylcolchicine, and (+)-colchicine and reassignment of the position of the double bond in dehydro-7-deacetamidocolchicines. |
| AID1413546 | Selectivity index, ratio of CC50 for hTERT-RPE1 cells to GI50 for human MCF7 cells | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | Synthesis and biological evaluation of novel 5-chloro- |
| AID153197 | In vivo antitumor activity against P388 lymphocytic leukemia cells implanted intraperitoneally; reproducible significant activity. | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
| AID1850714 | Antiproliferative activity against human SH-SY5Y cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2022 | RSC medicinal chemistry, May-25, Volume: 13, Issue:5 | Morpholine substituted quinazoline derivatives as anticancer agents against MCF-7, A549 and SHSY-5Y cancer cell lines and mechanistic studies. |
| AID1883545 | Disruption of microtubule network in human HGC-27 cells assessed as incomplete mitosis at 25 nM measured after 48 hrs by DAPI staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID377079 | Antimicrobial activity against Aspergillus niger after 3 days | 2005 | Journal of natural products, Feb, Volume: 68, Issue:2 | New colchicinoids from a native Jordanian meadow saffron, colchicum brachyphyllum: isolation of the first naturally occurring dextrorotatory colchicinoid. |
| AID208695 | Tested for caspase activation activity in human breast cancer T47D cells | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | Discovery of substituted N-phenyl nicotinamides as potent inducers of apoptosis using a cell- and caspase-based high throughput screening assay. |
| AID274815 | Cell cycle arrest in KB/HeLa cells by accumulation at S phase at 100 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID780971 | Displacement of [3H]-colchicine from biotin-labeled tubulin (unknown origin) at 5 uM after 2 hrs by scintillation proximity assay relative to control | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Furanylazaindoles: potent anticancer agents in vitro and in vivo. |
| AID597796 | Cytotoxicity against human CEM cells after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Imidazolone-amide bridges and their effects on tubulin polymerization in cis-locked vinylogous combretastatin-A4 analogues: synthesis and biological evaluation. |
| AID658917 | Cytotoxicity against human HT-29 cells after 48 hrs using resazurin by microplate fluorometer analysis | 2012 | Journal 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. |
| AID152693 | The compound was tested for its potency against lymphocytic leukemia P388 screen in mice. | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Biological effects of modified colchicines. Improved preparation of 2-demethylcolchicine, 3-demethylcolchicine, and (+)-colchicine and reassignment of the position of the double bond in dehydro-7-deacetamidocolchicines. |
| AID540211 | Fraction unbound in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID302075 | Antiproliferative activity against human MCF7 cells after 5 days by microplate assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | [(2-Phenylindol-3-yl)methylene]propanedinitriles inhibit the growth of breast cancer cells by cell cycle arrest in G(2)/M phase and apoptosis. |
| AID670881 | Cytotoxicity against human HT-29 cells after 48 hrs by XTT assay | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14 | Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents. |
| AID1435803 | Disruption of preformed spheroids in human MIAPaCa2 cells at 1 uM measured after 48 hrs by propidium staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID596144 | Cell cycle arrest in human KB cells assessed as accumulation of cells at G2/M phase after 24 hrs by propidium iodide-based FACScan | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9 | Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors. |
| AID214006 | In vitro inhibitory activity against tubulin polymerization (10 uM) | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13 | Structure-activity requirements for flavone cytotoxicity and binding to tubulin. |
| AID214012 | Inhibition of tubulin polymerization | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and structure-activity profiles of A-homoestranes, the estratropones. |
| AID511364 | Cytotoxicity against human Jurkat cells assessed as dead cells at 5 uM after 48 hrs by propidium iodide-based FACS flow cytometry | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Glycopeptide dendrimer colchicine conjugates targeting cancer cells. |
| AID1905061 | Inhibition of tubulin polymerization (unknown origin) assessed as fluorescence intensity emission at 410 nm for 60 mins | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Discovery of a Novel Stilbene Derivative as a Microtubule Targeting Agent Capable of Inducing Cell Ferroptosis. |
| AID1296734 | Inhibition of porcine brain tubulin polymerization measured every 1 min for 60 mins by microplate reader analysis | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology. |
| AID264024 | Cytotoxicity against human PC3 cell line | 2006 | Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10 | Synthesis and biological evaluation of B-ring modified colchicine and isocolchicine analogs. |
| AID758703 | Cell cycle arrest in human K562 cells assessed as accumulation at subG1 phase at 10 uM after 24 hrs by annexin V-FITC/PI staining-based FACS flow cytometric analysis (Rvb = 7.1 +/- 1.1%) | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID1566324 | Cell cycle arrest in human MCF7 cells assessed as accumulation in S phase at 5 times of antiproliferative IC50 incubated for 48 hrs by propidium iodide based flow cytometry (Rvb = 34 %) | |||
| AID1773134 | Antiproliferative activity against human U-251 cells after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery 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. |
| AID1503421 | Gastrointestinal toxicity in human HT-29 cells assessed as lysosomal membrane potential at 5 uM incubated for 3 hrs by flow cytometry | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID404616 | Antiproliferative activity against human K562 cells after 72 hrs | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | New C5-alkylated indolobenzazepinones acting as inhibitors of tubulin polymerization: cytotoxic and antitumor activities. |
| AID1535573 | Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay | 2019 | Bioorganic & 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. |
| AID1402706 | Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design and characterization of α-lipoic acyl shikonin ester twin drugs as tubulin and PDK1 dual inhibitors. |
| AID54322 | Evaluated for the stimulation of GTP hydrolysis | 1993 | Journal 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 |
| AID409672 | Cytotoxicity against human HeLa cells after 48 hrs by luminescence cell viability assay | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 | Synthesis and characterization of BODIPY-labeled colchicine. |
| AID1186697 | Cytotoxicity against human COLO205 cells assessed as growth inhibition by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | New benzimidazole-2-urea derivates as tubulin inhibitors. |
| AID342499 | Inhibition of nuclear translocation of thioredoxin 1 in human M21 cells at 0.1 uM after 18 hrs by immunocytochemistry | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Aromatic 2-chloroethyl urea derivatives and bioisosteres. Part 2: Cytocidal activity and effects on the nuclear translocation of thioredoxin-1, and the cell cycle progression. |
| AID1773136 | Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery 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. |
| AID1402730 | Inhibition of microtubule polymerization in human HeLa cells at 0.5 uM after 24 hrs by rhodamine/DAPI staining-based confocal microscopic analysis | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design and characterization of α-lipoic acyl shikonin ester twin drugs as tubulin and PDK1 dual inhibitors. |
| AID101821 | Inhibition of MDA-MB-231 cell proliferation | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID526944 | Cytotoxicity against human multidrug-resistant MDA-MB-435/LCCMDR1 cells after 48 hrs by sulforhodamine B assay | 2010 | Journal 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. |
| AID1125811 | Displacement of [3H]colchicine from tubulin (unknown origin) at 5 uM after 2 hrs by scintillation counting analysis | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Antimitotic and vascular disrupting agents: 2-hydroxy-3,4,5-trimethoxybenzophenones. |
| AID256880 | Cell cycle arrest in A431 cells by accumulation at G2/M phase cell at 0.1uM | 2005 | Bioorganic & 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. |
| AID1186696 | Cytotoxicity against human NCI-H460 cells assessed as growth inhibition by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | New benzimidazole-2-urea derivates as tubulin inhibitors. |
| AID1821599 | Inhibition of tubulin polymerization in human KYSE-450 cells assessed as microtubule assembly at 0.01 uM measured after 48 hrs by immunofluorescence assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis and evaluation of novel bis-substituted aromatic amide dithiocarbamate derivatives as colchicine site tubulin polymerization inhibitors with potent anticancer activities. |
| AID1566325 | Cell cycle arrest in human MCF7 cells assessed as accumulation in S phase at 5 times of antiproliferative IC50 incubated for 72 hrs by propidium iodide based flow cytometry (Rvb = 19.8 %) | |||
| AID1870920 | Induction of microtubule depolymerization in human A549 cells assessed as occurence of cell shrinkage at 2.5 uM measured after 48 hrs by DAPI staining based immunofluorescence assay | |||
| AID605847 | Antiproliferative activity against human 451LU cells after 48 hrs by alamar blue assay | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID729108 | Cytotoxicity against human MDA-MB-435 cells assessed as growth inhibition after 48 hrs by SRB assay | 2013 | Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8 | Discovery of 4-Aryl-2-benzoyl-imidazoles as tubulin polymerization inhibitor with potent antiproliferative properties. |
| AID1566294 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay | |||
| AID587611 | Inhibition of spindle formation in human A549 cells after 24 hs by DAPI staining | 2011 | Journal 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. |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1414057 | Fungicidal activity against Aspergillus niger van Tiegen BAM4 ATCC 6275 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1431299 | Inhibition of lamb brain tubulin self assembly assessed as decrease in microtubule formation at 10 uM after 10 mins by turbidimetry/spectrometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID613262 | Antiproliferative activity against human H460 cells after 72 hrs by methylene blue assay | 2011 | European 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. |
| AID627403 | Antiproliferative activity against human SKOV3 after 48 hrs by SRB assay | 2011 | European 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. |
| AID761194 | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14 | Novel synthetic acridine derivatives as potent DNA-binding and apoptosis-inducing antitumor agents. |
| AID101630 | Anti tumor activity on human breast cancer cell line MDR-negative MDA-MB 231 after 72 hours of treatment | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | N-deacetyl-N-aminoacylthiocolchicine derivatives: synthesis and biological evaluation on MDR-positive and MDR-negative human cancer cell lines. |
| AID1075754 | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase after 24 hrs by propidium iodide staining-based FACS analysis | 2014 | Journal 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. |
| AID1883512 | Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID711171 | Induction of ABCB1 mRNA expression in human DLD1 cells at 1/10 IC50 to IC50 after 96 hrs by RT-PCR analysis | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID1333470 | Effect on cyclin D1 mRNA expression in human MDA-MB-231 cells assessed as ratio of cyclin D1 to GAPDH expression level at 5 uM after 24 hrs by RT-PCR method (Rvb = 0.71 No_unit) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID159536 | In vitro inhibitory concentration against tubulin assembly | 2003 | Journal 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. |
| AID780984 | Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Furanylazaindoles: potent anticancer agents in vitro and in vivo. |
| AID1736455 | Selectivity index, ratio of IC50 for drug resistant human K562 cells to IC50 for human K562 cells | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1395590 | Effect on VEGFR2 protein expression in human HT-29 cells assessed as secreted VEGFR2 level in culture media at 25 nM after 48 hrs by ELISA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID605774 | Antiproliferative activity against multidrug-resistant human CEM/VLB cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID1785444 | Non-covalent binding affinity to tubulin (unknown origin) assessed as compound detected in filtrate at 450 pmol incubated for 1 hr by UFLC-MS/MS analysis | |||
| AID553912 | Cell cycle arrest in human BxPC3 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. |
| AID732805 | Cytotoxicity against human HeLa cells assessed as growth inhibition | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Design, synthesis, biological evaluation and molecular modeling studies of 1-aryl-6-(3,4,5-trimethoxyphenyl)-3(Z)-hexen-1,5-diynes as a new class of potent antitumor agents. |
| AID1414061 | Fungicidal activity against Trichoderma viride Pers after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1822541 | Induction of microtubule depolymerization in human A2780S cells at 10 nM incubated for 24 hrs by immunofluorescence method | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents. |
| AID1492844 | Antiproliferative activity against human 5637 cells after 96 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. |
| AID336345 | Antimitotic activity against rat ASK cells assessed as reversal of astrocyte morphology at 0.032 ug/ml | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
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| AID1736445 | Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
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| AID201786 | In vitro growth inhibition of SK-MEL-2, malignant melanoma. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors. |
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| AID1389585 | Antiarthritic activity in MSU-induced acute gouty arthritis Sprague-Dawley rat model assessed as reduction in ankle swelling by measuring perimeter of ankle at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last do | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID428001 | Growth inhibition of human H1299 cells after 48 hrs | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents. |
| AID1569086 | Antiproliferative activity against human PC3-TxR cells | |||
| AID1736554 | Induction of microtubule disruption in human HT-29 cells at 0.5 uM incubated for 24 hrs by DAPI staining based confocal fluorescence microscopic analysis | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID678713 | Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID595055 | Cell cycle arrest in mouse B16F10 cells assessed as accumulation at G2/M phase at 1 ug/ml after 24 hrs by flow cytometry (Rbv = 12.27%) | 2011 | Bioorganic & 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. |
| AID340150 | Inhibition of microtubule associated protein rich tubulin polymerization | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors. |
| AID1566327 | Cell cycle arrest in human ALL5 cells assessed as accumulation in S phase at 5 times of antiproliferative IC50 incubated for 48 hrs by propidium iodide based flow cytometry (Rvb = 10.3 %) | |||
| AID1414055 | Antifungal activity against Aureobasidium pullulans BAM10 ATCC 9348 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1785506 | Antiproliferative activity against human Huh-7 cells incubated for 72 hrs by MTT assay | |||
| AID662405 | Cytotoxicity against mouse B16F10 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12 | Synthesis, characterization and in vitro anti-tumor activities of matrine derivatives. |
| AID214731 | Inhibitory binding percentage of compound towards colchicine site in tubulin using tubulin-[3H]colchicine as radioligand at a concentration of 200 uM | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity. |
| AID337652 | Cytotoxicity against human LNCAP cells after 3 days by SRB assay | 1994 | Journal of natural products, Oct, Volume: 57, Issue:10 | Cytotoxic diterpenoids from Isodon megathyrsus. |
| AID1333453 | Antiproliferative activity against human mammary epithelial cells after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID602115 | Antimitotic activity in human HeLa cells assessed as visible deffect in microtubule organization at 5 nM after 3 hrs by inverted microscopic analysis | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | Anticancer properties of an important drug lead podophyllotoxin can be efficiently mimicked by diverse heterocyclic scaffolds accessible via one-step synthesis. |
| AID355582 | Antiproliferative activity against human HT-29 cells at 0.01 ug after 48 hrs by two-layer agar-diffusion method | |||
| AID1736479 | Cell cycle arrest in human HT29 cells assessed as cell accumulation at G2 phase at 0.25 uM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 10.37 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID388963 | Toxicity in C57BL/J6 mouse assessed as creatinine level in serum | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis. |
| AID1077392 | Antiproliferative activity against human MDA-MB-431 cells by SRB assay | 2013 | MedChemComm, , Volume: 4, Issue:2 | Developing novel C-4 analogues of pyrrole-based antitubulin agents: weak but critical hydrogen bonding in the colchicine site. |
| AID1897648 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 12-15, Volume: 76 | Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID657579 | Cell cycle arrest in human MCF7 cells assessed as accumulation in S phase at 5 ug/ml after 24 hrs by flow cytometry (Rvb = 8.06%) | 2012 | Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10 | Design, synthesis and biological evaluation of novel chalcone derivatives as antitubulin agents. |
| AID721883 | Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by MTT assay | 2013 | Journal 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. |
| AID1163575 | Antiproliferative activity against human HCT15 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Synthesis and biological evaluation of novel millepachine derivatives as a new class of tubulin polymerization inhibitors. |
| AID1807385 | Cytotoxicity against paclitaxel resistant human MDA-MB-231/TxR cells measured after 72 hrs by western blot | |||
| AID1541696 | Antimigratory activity in human MDA-MB-231 cells assessed as inhibition of cell motility after 24 hrs by microscopic analysis | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis, and validation of novel nitrogen-based chalcone analogs against triple negative breast cancer. |
| AID536764 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis and cytotoxicity evaluation of novel 1,4-disubstituted 1,2,3-triazoles via CuI catalysed 1,3-dipolar cycloaddition. |
| AID1754733 | Antiproliferative activity against human A549 cells assessed as inhibition of proliferation after 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Synthesis and antiproliferative screening of novel doubly modified colchicines containing urea, thiourea and guanidine moieties. |
| AID328776 | Inhibition of pig brain tubulin polymerization at 3 uM | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Isoindolo[2,1-a]quinoxaline derivatives, novel potent antitumor agents with dual inhibition of tubulin polymerization and topoisomerase I. |
| AID8458 | In vitro growth inhibition of A549, lung carcinoma. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors. |
| AID605764 | Antiproliferative activity against mouse B16F0 cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID1201733 | Cytotoxicity against human PANC1 cells assessed as growth inhibition after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID274827 | Cell cycle arrest in KB/HeLa cells by accumulation at G1 phase at 1 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1625718 | Antiproliferative activity against human HCT8 cells after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID303690 | Cytotoxicity against human NCI-H460 cells after 48 hrs by XTT assay | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID375807 | Induction of apoptosis in human T47D cells assessed as caspase activation after 48 hrs by HTS assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylthieno[2,3-d]pyrimidines as potent apoptosis inducers. |
| AID1167532 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at S phase at 0.1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 24%) | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Synthesis and antiproliferative activity of 6-phenylaminopurines. |
| AID1110727 | Inhibition of Bos taurus (bovine) brain tubulin polymerization | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Structure-activity relationships of phenylcyclohexene and biphenyl antitubulin compounds against plant and mammalian cells. |
| AID274821 | Cell cycle arrest in KB/HeLa cells by accumulation at G2/M phase at 10 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1292354 | Antiproliferative activity against human A375 cells assessed as cell growth inhibition after 96 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11 | New imidazoquinoxaline derivatives: Synthesis, biological evaluation on melanoma, effect on tubulin polymerization and structure-activity relationships. |
| AID624628 | Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID75537 | Cytotoxic activity against cellular metabolic activity of Glioma SF-268 tumor cell line using XTT proliferation assay after incubation with the compound for 48 h | 2003 | Journal 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. |
| AID1639383 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4 | Parvifoline Derivatives as Tubulin Polymerization Inhibitors. |
| AID1198465 | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase after 24 hrs by flow cytometry (Rvb = 25.67%) | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents. |
| AID427909 | Induction of apoptosis in human H1299 cells assessed as caspase activation after 48 hrs | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents. |
| AID1585583 | Ratio of IC50 for human A2780AD cells to IC50 for human A2780 cells | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents. |
| AID1163571 | Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Synthesis and biological evaluation of novel millepachine derivatives as a new class of tubulin polymerization inhibitors. |
| AID1384286 | Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 50 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 15 +/- 6%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID730214 | Cytotoxicity against human HeLa cells after 72 hrs by CCK-8 assay | 2013 | Journal 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. |
| AID1465170 | Antiproliferative activity against human SKOV3 cells by SRB assay | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | Design, synthesis and biological evaluation of 2-phenylquinoline-4-carboxamide derivatives as a new class of tubulin polymerization inhibitors. |
| AID721884 | Cytotoxicity against human MCF7 cells assessed as growth inhibition by trypan blue exclusion assay | 2013 | Journal 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. |
| AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID235404 | Therapeutic ratio was determined for intraperitoneal administration | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Synthesis and antiinflammatory activity of hexahydrothiopyrano[4,3-c]pyrazoles and related analogues. |
| AID375809 | Inhibition of tubulin polymerization by high-throughput assay | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13 | Discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylthieno[2,3-d]pyrimidines as potent apoptosis inducers. |
| AID213853 | Binding constant at colchicine site of bovine brain tubulin | 2002 | Bioorganic & 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. |
| AID486604 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 25 nM after 24 hrs by flow cytometry | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | Synthesis, molecular modeling and biological evaluation of dithiocarbamates as novel antitubulin agents. |
| AID1771027 | Antiproliferative activity against human RPMI-7951 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID657575 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10 | Design, synthesis and biological evaluation of novel chalcone derivatives as antitubulin agents. |
| AID282689 | Cell cycle arrest in HEK293EBNA cells by accumulation at G2/M phase cell at 10 uM relative to DMSO | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Identification of novel and improved antimitotic agents derived from noscapine. |
| AID1674008 | Cytotoxicity against HEK293 cells incubated for 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1238307 | Inhibition of Myc mRNA expression in human HT-29 cells assessed as Myc mRNA level at at 10 uM incubated for 48 hrs by RT-PCR method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes. |
| AID412962 | Growth inhibition of human H460 cells after 72 hrs by methylene blue dye assay | 2008 | Journal 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. |
| AID637150 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2012 | Bioorganic & 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. |
| AID526950 | Cytotoxicity against human PC3 cells after 48 hrs by sulforhodamine B assay | 2010 | Journal 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. |
| AID1267534 | Antiproliferative activity against human MES-SA cells after 72 hrs by resazurin assay | 2016 | Bioorganic & 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. |
| AID214031 | Tested for inhibition against tubulin polymerization | 2000 | Journal 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. |
| AID102526 | Cytotoxic activity against cellular metabolic activity of Lung NCI-H460 tumor cell line using XTT proliferation assay after incubation with the compound for 48 h | 2003 | Journal 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. |
| AID1704321 | Acute toxicity in C57BL/6 mouse assessed as mouse death at 5 mg/kg, iv measured after 16 hrs | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID678943 | TP_TRANSPORTER: uptake in membranes from CEM/VLB100 cells | 1999 | Analytical biochemistry, Mar-15, Volume: 268, Issue:2 | A continuous fluorescence assay for the study of P-glycoprotein-mediated drug efflux using inside-out membrane vesicles. |
| AID1888930 | Antiproliferative activity against human HCT-116 cells after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Synthesis and biological evaluation of 3β-O-neoglycosides of caudatin and its analogues as potential anticancer agents. |
| AID605848 | Antiproliferative activity against human SW480 cells after 48 hrs by alamar blue assay | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1221977 | Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID342597 | Induction of beta2-tubulin alkylation in human M21 cells at 2 times GI50 by Western blot analysis | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Selective alkylation of beta(II)-tubulin and thioredoxin-1 by structurally related subsets of aryl chloroethylureas leading to either anti-microtubules or redox modulating agents. |
| AID1186701 | Cytotoxicity against human HeLa cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | New benzimidazole-2-urea derivates as tubulin inhibitors. |
| AID1651322 | Inhibition of MSU-induced ASC protein expression in synovial tissue of MSU-induced acute gout arthritis rat model at 10 mg/kg by western blot analysis | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Development of novel NLRP3-XOD dual inhibitors for the treatment of gout. |
| AID733795 | Cytotoxicity against mouse C26 cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID1421772 | Antiproliferative activity against mouse L929 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Conformation impacts on the bioactivities of SMART analogues. |
| AID624629 | Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID409956 | Inhibition of mouse brain MAOB | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
| AID1673966 | Antiproliferative activity against human A549 cells incubated for 72 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1870921 | Induction of microtubule depolymerization in human A549 cells assessed as occurence of rounded cells at 2.5 uM measured after 48 hrs by DAPI staining based immunofluorescence assay | |||
| AID1407723 | Induction of apoptosis in human A375 cells assessed as late apoptotic cells at 10 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 3.33%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID658919 | Inhibition of bovine brain tubulin polymerization by thermostatic spectrophotometer | 2012 | Journal 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. |
| AID1625737 | Cytotoxicity against vinblastine resistant/P-gp overexpressing human HCT8 cells assessed as reduction in cell growth after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1807396 | Induction of apoptosis in human A375/TxR cells assessed as apoptotic cells at 10 nM measured for 24 hrs by annexin VFITC /PI staining based analysis (Rvb = 8.8%) | |||
| AID1566299 | Selectivity index, ratio of IC50 of mouse BALB/3T3 cells to IC50 of human ALL5 cells | |||
| AID150756 | Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID1431308 | Binding affinity to lamb brain tubulin after 15 mins by fluorimetric titration method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID1882711 | Anticancer activity against human HeLa cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Recent advances of antitumor shikonin/alkannin derivatives: A comprehensive overview focusing on structural classification, synthetic approaches, and mechanisms of action. |
| AID1704324 | Acute toxicity in iv dosed A/Sn mouse assessed as mouse death at 5 mg/kg, iv measured after 16 hrs | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1399022 | Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18 | Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors. |
| AID1407738 | Induction of apoptosis in human A375 cells assessed as early apoptotic cells at 100 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.4%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
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| AID1732752 | Antiproliferative activity against multidrug-resistant human MES-SA/Dx5 cells assessed as reduction in cell viability incubated for 72 hrs by prestoblue dye based assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies. |
| AID336350 | Antimitotic activity against rat ASK cells assessed as reversal of astrocyte morphology at 100 ug/ml | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID780977 | Cytotoxicity against human KB-VIN10 cells overexpressing P-gp170/MDR assessed as growth inhibition after 72 hrs by methylene blue staining-based assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Furanylazaindoles: potent anticancer agents in vitro and in vivo. |
| AID1750231 | Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | |||
| AID1550789 | Binding affinity to calf brain tubulin assessed as binding constant | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop. |
| AID383965 | Cytotoxicity against human MDA-MB-435 cells | 2008 | Journal 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. |
| AID645073 | Antitumor activity against human HCT116 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 1 mg/kg, ip administered on 1, 3 and 5th day measured on day 21 relative to control | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Design, Synthesis, and Antitumor Activity of 4-Halocolchicines and Their Pro-drugs Activated by Cathepsin B. |
| AID1385700 | Cytotoxicity against human HeLa cells after 72 hrs by MTT assay | 2018 | Journal of natural products, 08-24, Volume: 81, Issue:8 | Structurally Diverse Highly Oxygenated Triterpenoids from the Roots of Ailanthus altissima and Their Cytotoxicity. |
| AID1507352 | Cell cycle arrest in human HT-29 cells assessed as accumulation at G2/M phase at 1.25 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 32.5 +/- 2.3%) | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Thiosemicarbazones and 4-thiazolidinones indole-based derivatives: Synthesis, evaluation of antiproliferative activity, cell death mechanisms and topoisomerase inhibition assay. |
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| AID1167523 | Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation after 4 days by Coulter counter based cell counting method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Synthesis and antiproliferative activity of 6-phenylaminopurines. |
| AID1541672 | Antimigratory activity in human MDA-MB-231 cells assessed as wound diameter at 5 uM measured after 24 hrs by microscopic analysis | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis, and validation of novel nitrogen-based chalcone analogs against triple negative breast cancer. |
| AID1221971 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID732802 | Cytotoxicity against human SKHEP1 cells assessed as growth inhibition | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Design, synthesis, biological evaluation and molecular modeling studies of 1-aryl-6-(3,4,5-trimethoxyphenyl)-3(Z)-hexen-1,5-diynes as a new class of potent antitumor agents. |
| AID758711 | Growth inhibition of human HT-29 cells at 10 uM after 72 hrs by MTT assay relative to control | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
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| AID1566314 | Cell cycle arrest in human MCF7 cells assessed as accumulation in G2 phase at 5 times of antiproliferative IC50 incubated for 24 hrs by propidium iodide based flow cytometry (Rvb = 22.4 %) | |||
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| AID1238303 | Inhibition of VEGF mRNA expression in human HT-29 cells assessed as VEGF mRNA level at at 10 uM incubated for 48 hrs by RT-PCR method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes. |
| AID511363 | Cytotoxicity against human Jurkat cells after 48 hrs | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Glycopeptide dendrimer colchicine conjugates targeting cancer cells. |
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| AID130472 | Carrageenan-induced edema was determined value for oral administration | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Synthesis and antiinflammatory activity of hexahydrothiopyrano[4,3-c]pyrazoles and related analogues. |
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| AID526953 | Resistance index, ratio of IC50 for human multidrug-resistant MDA-MB-435/LCCMDR1 cells to IC50 for human MDA-MB-435 cells | 2010 | Journal 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. |
| AID749383 | Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | The discovery of colchicine-SAHA hybrids as a new class of antitumor agents. |
| AID139239 | Logarithm of toxic activity (1/lethal dose) in mice bearing P388 leukemia on chronic regimen (Q 1-9) | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID1201725 | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID228428 | Compound was evaluated for its ability to affect topoisomerase II inhibition; inactive | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9 | The synthesis and evaluation of benzannelated-azatoxins: the benzazatoxins. |
| AID1628401 | Growth inhibition of human MCF7 cells incubated for 72 hrs by MTT assay | 2016 | Journal 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. |
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| AID1189188 | Induction of apoptosis in human A549 cells assessed as necrotic cells at 0.25 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.06%) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1566329 | Induction of apoptosis in human ALL5 cells assessed as reduction in 116 kDa PARP expression at 43 uM incubated for 24 and 48 hrs by immunoblot analysis | |||
| AID214033 | Inhibition of bovine tubulin polymerization | 1994 | Journal 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. |
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| AID458392 | Inhibition of bovine brain tubulin polymerization by turbidity assay | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | Synthesis and biological activities of 2-amino-1-arylidenamino imidazoles as orally active anticancer agents. |
| AID303710 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G2M phase at 0.3 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
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| AID1179654 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2014 | Bioorganic & 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. |
| AID679133 | TP_TRANSPORTER: drug resistance in KB-VIN10 cells | 2004 | Cancer research, Jul-01, Volume: 64, Issue:13 | BPR0L075, a novel synthetic indole compound with antimitotic activity in human cancer cells, exerts effective antitumoral activity in vivo. |
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| AID1754734 | Resistance index, ratio of IC50 for antiproliferative activity against human Lovo/DX cells to IC50 for antiproliferative activity against human LoVo cells | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Synthesis and antiproliferative screening of novel doubly modified colchicines containing urea, thiourea and guanidine moieties. |
| AID1333466 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 5 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 83.25%) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1593961 | Cell cycle arrest in human PHK160b cells assessed as accumulation at G2/M phase at 50 uM incubated for 48 hrs by propidium iodide staining-based flow cytometry | |||
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| AID1189588 | Cytotoxicity against human HEK293 cells after 3 days by MTT assay | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID120695 | Compound was evaluated for the antitumor activity against P388 lymphocytic leukemia in mice | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
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| AID596141 | Antiproliferative activity against human HT-29 cells after 72 hrs by sulforhodamine B assay | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9 | Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors. |
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| AID1882734 | Cytotoxicity against human HEK293T cells assessed as inhibition of cell growth incubated for 24 hrs in presence of foetal bovine serum by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Recent advances of antitumor shikonin/alkannin derivatives: A comprehensive overview focusing on structural classification, synthetic approaches, and mechanisms of action. |
| AID377077 | Antimicrobial activity against Mycobacterium smegmatis after 3 days | 2005 | Journal of natural products, Feb, Volume: 68, Issue:2 | New colchicinoids from a native Jordanian meadow saffron, colchicum brachyphyllum: isolation of the first naturally occurring dextrorotatory colchicinoid. |
| AID587610 | Inhibition of microtubule polymerization in human A549 cells after 24 hs by immunofluorescence staining | 2011 | Journal 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. |
| AID721881 | Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay | 2013 | Journal 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. |
| AID1492841 | Antiproliferative activity against human A427 cells after 96 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. |
| AID1395568 | Effect on hTERT gene expression in human HT-29 cells assessed as hTERT level at 25 nM after 48 hrs by RT-qPCR analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID1736533 | Induction of apoptosis in human HT-29 cells assessed as necrotic cells at 0.5 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.1 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID299429 | Cell cycle arrest in Jurkat cells assessed as accumulation at G2/M phase at 25 uM after 15 hrs relative to control | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Antiproliferative and apoptosis inducing properties of pyrano[3,2-c]pyridones accessible by a one-step multicomponent synthesis. |
| AID357845 | Binding affinity to calf thymus DNA assessed as reduction in DNA peak by pre-incubation method | |||
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| AID412968 | Inhibition of tubulin polymerization after 30 mins | 2008 | Journal 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. |
| AID1221980 | Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID409676 | Membrane permeability by PAMPA | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 | Synthesis and characterization of BODIPY-labeled colchicine. |
| AID1628400 | Growth inhibition of human PC3 cells incubated for 72 hrs by MTT assay | 2016 | Journal 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. |
| AID1189182 | Displacement of (E)-3-(4-(Dimethylamino)phenyl)-1-(4'-fluoro[1,1'-biphenyl]-2-yl)prop-2-en-1-one from tubulin (unknown origin) at 20 uM by fluorescence assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1167518 | Antiproliferative activity against human HMEC1 cells assessed as inhibition of cell proliferation after 4 days by Coulter counter based cell counting method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Synthesis and antiproliferative activity of 6-phenylaminopurines. |
| AID1736453 | Antiproliferative activity against human K562 cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID303723 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G1 phase at 31.6 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID41043 | Inhibition B16F1 cell proliferation (Not tested) | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID1673967 | Antiproliferative activity against human MCF7 cells incubated for 72 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1704328 | Acute toxicity in mouse assessed as lethal dose measured after 7 days | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1389601 | Inhibition of MSU-induced NLRP3 protein level in synovial homogenate of acute gouty arthritis Sprague-Dawley rat model at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last dose measured up to 24 hrs by Western bl | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID711166 | Resistance factor, ratio of IC50 for human HeLa cells expressing class 3 tubulin to IC50 for human HeLa cells | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID1897649 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 12-15, Volume: 76 | Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities. |
| AID721876 | Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay | 2013 | Journal 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. |
| AID1435785 | Cytotoxicity against 3D culture of human EAhy926 cells up to 10000 nM measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID595059 | Cell cycle arrest in mouse B16F10 cells assessed as accumulation at S phase at 1 ug/ml after 24 hrs by flow cytometry (Rbv = 14.96%) | 2011 | Bioorganic & 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. |
| AID1193498 | Thermodynamic equilibrium solubility, log S of the compound simulated gastric fluid at pH 1.2 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
| AID409671 | Inhibition of bovine tubulin polymerization at 5 uM | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 | Synthesis and characterization of BODIPY-labeled colchicine. |
| AID712842 | Inhibition of pig neuronal tubulin polymerization at 10 uM by fluorescence analysis | 2012 | ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12 | Synthesis and antiproliferative activities of ottelione a analogues. |
| AID1694413 | Cell cycle arrest in human ALL-5 cells assessed as accumulation at sub-G1 phase after 48 hrs at 5 times of IC50 by propidium iodide staining-based flow cytometric analysis relative to control | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
| AID347989 | Cell cycle arrest in human KB/HeLa cells assessed as G1 phase accumulation at 0.3 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1221960 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1899068 | Antiproliferative activity against human KB cells measured after 72 hrs by SRB assay | |||
| AID670879 | Cytotoxicity against human A549 cells after 48 hrs by WST-8 assay | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14 | Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents. |
| AID1703290 | Binding affinity to pig brain tubulin at 30 degree C without preincubation | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities. |
| AID681119 | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID1435799 | Induction of lysosomal membrane hyperpolarization in 3D culture of human MIAPaCa2 cells at 1 uM measured after 48 hrs by LysoTrackRed dye based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID612318 | Antiproliferative activity against human PC3 cells after 96 hrs by sulforhodamine B assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis and antiproliferative activity of novel 2-aryl-4-benzoyl-imidazole derivatives targeting tubulin polymerization. |
| AID1407711 | Antiproliferative activity against human A549 cells after 72 hrs by MTS assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1673971 | Antiproliferative activity against human KB-31 cells incubated for 96 hrs by spectrophotometric method | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1549907 | Antiproliferative activity against human H8 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain. |
| AID1465172 | Antiproliferative activity against human A549 cells by SRB assay | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | Design, synthesis and biological evaluation of 2-phenylquinoline-4-carboxamide derivatives as a new class of tubulin polymerization inhibitors. |
| AID1233600 | Induction of cell cycle arrest in human M21 cells assessed as cells accumulation at G0/G1 phase at 24 nM after 24 hrs by flow cytometry (Rvb = 54.5%) | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model. |
| AID1870923 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability at 0.01 to 100 uM measured after 24 to 72 hrs by MTT assay | |||
| AID1421769 | Antiproliferative activity against human SGC7901 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Conformation impacts on the bioactivities of SMART analogues. |
| AID1142137 | Cell cycle arrest in HMEC1 cells assessed as accumulation at G2/M phase at 0.03 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach. |
| AID303687 | Cytotoxicity against human KB/HeLa cells after 48 hrs by XTT assay | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1722133 | Induction of apoptosis in human HCT-116 cells assessed as necrotic cells at 5 uM measured after 24 hrs by annexin-V/FITC staining based flow cytometry analysis (Rvb = 0.2 %) | 2020 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20 | Anti-proliferative potential of triphenyl substituted pyrimidines against MDA-MB-231, HCT-116 and HT-29 cancer cell lines. |
| AID54102 | In vitro cytotoxicity against DMS114 cell line. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Antitumor agents. 141. Synthesis and biological evaluation of novel thiocolchicine analogs: N-acyl-, N-aroyl-, and N-(substituted benzyl)deacetylthiocolchicines as potent cytotoxic and antimitotic compounds. |
| AID598213 | Cytotoxicity against human OVCAR3 cells assessed as cell death after 24 hrs by trypan blue exclusion assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11 | Synthesis and characterisation of a novel tubulin-directed DO3A-colchicine conjugate with potential theranostic features. |
| AID1194693 | Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10 | Synthesis and evaluation of benzosuberone embedded with 1,3,4-oxadiazole, 1,3,4-thiadiazole and 1,2,4-triazole moieties as new potential anti proliferative agents. |
| AID1395535 | Induction of apoptosis in human HT-29 cells assessed as apoptotic cells at 40 nM after 48 hrs by Annexin V-FITC staining-based flow cytometric analysis (Rvb = 13 +/- 3%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID409678 | Induction of apoptosis in african green monkey Vero cells assessed as caspase 3/7 activity after 18 hrs by flow cytometry using propidium iodide staining | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 | Synthesis and characterization of BODIPY-labeled colchicine. |
| AID611266 | Cytotoxicity against human SKOV3 cells after 48 hrs by XTT assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Phenylimino-10H-anthracen-9-ones as novel antimicrotubule agents-synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID1163581 | Antiproliferative activity against human U251 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Synthesis and biological evaluation of novel millepachine derivatives as a new class of tubulin polymerization inhibitors. |
| AID1625729 | Binding affinity to tubulin in human HepG2 cells assessed as induction of abnormal chromosomal aggregation at 100 nM after 16 to 24 hrs by DAPI staining-based immunofluorescence microscopy | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1407740 | Induction of apoptosis in human A375 cells assessed as necrotic cells at 100 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.3%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1673973 | Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition and measured for 30 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1179657 | Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetric method | 2014 | Bioorganic & 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. |
| AID115600 | MED(minimum effective dose) against P388 lymphocytic leukemia in mice; this dose produced T/C greater than the threshold value of 125 | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
| AID1431303 | Binding affinity to lamb brain tubulin at 10 uM after 50 mins by fluorimetric titration method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID1407726 | Induction of apoptosis in human A375 cells assessed as early apoptotic cells at 100 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.35%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1221969 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID243422 | log (1/Km) value for human liver microsome cytochrome P450 3A4 | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18 | Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism. |
| AID492477 | Antitumor activity against human OVCAR-3 cells xenografted in mouse assessed as increase in mouse life span | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3 | Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach. |
| AID1395588 | Effect on c-MYC protein expression in human HT-29 cells assessed as c-MYC level at 25 nM after 48 hrs by ELISA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID1736448 | Antiproliferative activity against human HEK293T cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1736446 | Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1414054 | Antifungal activity against Penicillium cyclopium Westling after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1674002 | Cytotoxicity against human Mia PaCa-2 cells incubated for 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID627404 | Antiproliferative activity against human CEM after 48 hrs by SRB assay | 2011 | European 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. |
| AID1704311 | Induction of cell cycle arrest in human SW-620 cells assessed as accumulation at G1 phase at 5 nM incubated for 48 hrs by RNase/PI staining based flow cytometry analysis (Rvb = 65 %) | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID733785 | Cytotoxicity against human PC3 cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID1221958 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID697551 | Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16 | Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents. |
| AID348166 | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by alamar blue assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Design, synthesis and biological evaluation of novel stilbene-based antitumor agents. |
| AID1389602 | Inhibition of MSU-induced ASC protein level in synovial homogenate of acute gouty arthritis Sprague-Dawley rat model at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last dose measured up to 24 hrs by Western blot | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID303713 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G2M phase at 10 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID336338 | Cytotoxicity against multidrug-resistant human KBV1 cells | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID1407741 | Induction of apoptosis in human A375 cells assessed as live cells at 1000 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 92.3%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1194694 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10 | Synthesis and evaluation of benzosuberone embedded with 1,3,4-oxadiazole, 1,3,4-thiadiazole and 1,2,4-triazole moieties as new potential anti proliferative agents. |
| AID213862 | Inhibition activity of colchicine for tubuline polymerization to that of compound | 1997 | Journal of medicinal chemistry, Nov-07, Volume: 40, Issue:23 | Synthesis and structure-activity profiles of A-homoestranes, the estratropones. |
| AID347999 | Cell cycle arrest in human KB/HeLa cells assessed as S phase accumulation at 31.6 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID1245423 | Growth inhibition of human K562 cells incubated for 24 hrs by trypan blue dye exclusion assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality. |
| AID397414 | Cytotoxicity against Spodoptera frugiperda Sf9 cells assessed as chromatin condensation at 0.14 ppm after 48 hrs by fluorescence microscopy | 2009 | Bioorganic & medicinal chemistry, Jun-15, Volume: 17, Issue:12 | Insecticidal heterolignans--tubuline polymerization inhibitors with activity against chewing pests. |
| AID677620 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei 427 after 48 hrs by MTS assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17 | Identification of selective tubulin inhibitors as potential anti-trypanosomal agents. |
| AID1669121 | Induction of microtubule depolymerization in human HeLa cells at 100 nM incubated for 6 hrs by immunofluorescence microscopic method | |||
| AID221848 | Cytotoxic activity against mouse macrophage cell line J7.VBL-1 | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Fluorinated colchicinoids: antitubulin and cytotoxic properties. |
| AID214556 | Inhibition of tubulin polymerization (ITP) | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Antitumor Agents. 211. Fluorinated 2-phenyl-4-quinolone derivatives as antimitotic antitumor agents. |
| AID1407739 | Induction of apoptosis in human A375 cells assessed as late apoptotic cells at 100 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.96%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1651317 | Antiarthritic activity against MSU-induced acute gout arthritis rat model assessed as degree of ankle joint swelling after 48 hrs (Rvb = 3.4 +/- 0.5 No_unit) | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Development of novel NLRP3-XOD dual inhibitors for the treatment of gout. |
| AID1420817 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | |||
| AID270964 | Cytotoxicity against proliferating RKOp27 cells after 72 hrs by Alamar Blue assay | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19 | [4-(imidazol-1-yl)thiazol-2-yl]phenylamines. A novel class of highly potent colchicine site binding tubulin inhibitors: synthesis and cytotoxic activity on selected human cancer cell lines. |
| AID1628403 | Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay | 2016 | Journal 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. |
| AID1414047 | Cytotoxicity against human SKOV3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1198456 | Inhibition of bovine brain tubulin polymerization incubated for 20 mins by spectrophotometry | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents. |
| AID351577 | Inhibition of tubulin polymerization by DAPI staining method | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Discovery of N-aryl-9-oxo-9H-fluorene-1-carboxamides as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the carboxamide group. |
| AID612317 | Antiproliferative activity against human LNCAP cells after 96 hrs by sulforhodamine B assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis and antiproliferative activity of novel 2-aryl-4-benzoyl-imidazole derivatives targeting tubulin polymerization. |
| AID1235363 | Inhibition of bovine brain tubulin polymerization after 30 mins | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes. |
| AID536767 | Inhibition of tubulin polymerization at 3 uM | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Synthesis and cytotoxicity evaluation of novel 1,4-disubstituted 1,2,3-triazoles via CuI catalysed 1,3-dipolar cycloaddition. |
| AID1668047 | Inhibition of tubulin in human SK-MEL-28 cells assessed as disruption of microtubule network at 5 nM by Alexa Fluor 488 and DAPI staining based fluorescence microscopic method | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Drug repurposing and rediscovery: Design, synthesis and preliminary biological evaluation of 1-arylamino-3-aryloxypropan-2-ols as anti-melanoma agents. |
| AID461786 | Antiproliferative activity against P-gp170/MDR expressing human KBVIN cells after 72 hrs by methylene blue dye assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | 5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. |
| AID1378142 | Growth inhibition of human MDA-MB-231 cells up to 25 uM cotreated with camptothecin measured after 24 hrs by XTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma. |
| AID1704305 | Antiproliferative activity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1449628 | Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12 | Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification. |
| AID1807381 | Cytotoxicity against human A-375 cells measured after 72 hrs by western blot | |||
| AID291499 | Cell cycle arrest in HL60 cells assessed as accumulation in G0/G1 phase at 600 nM | 2007 | Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14 | Discovery of novel antitumor antimitotic agents that also reverse tumor resistance. |
| AID1333489 | Cell cycle arrest in human MDA-MB-231 cells assessed as increase in cell accumulation at G2/M phase at 5 uM after 24 hrs by propidium iodide staining based flow cytometry | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID299428 | Cell cycle arrest in Jurkat cells assessed as accumulation at S phase at 25 uM after 15 hrs relative to control | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Antiproliferative and apoptosis inducing properties of pyrano[3,2-c]pyridones accessible by a one-step multicomponent synthesis. |
| AID668143 | Antiproliferative activity against human LNCAP cells after 96 hrs by SRB assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | New substituted 4H-chromenes as anticancer agents. |
| AID1785448 | Refractive index, ratio of induction of irreversible mitotic block in human A2780S cells at 100 nM incubated for 12 hrs followed by compound elution and measured after 10 hrs to induction of mitotic block in human A2780S cells at 100 nM incubated for 12 h | |||
| AID1726339 | Induction of microtubule destabilization in human BT-549 cells assessed as loss of microtubule network at 100 nM incubated for 6 hrs by indirect immunofluorescence assay | 2020 | ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12 | Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides. |
| AID214376 | Percentage by which binding is reduced at 25 uM in rat brain microtubule protein | 1983 | Journal of medicinal chemistry, Oct, Volume: 26, Issue:10 | Biological effects of modified colchicines. 2. Evaluation of catecholic colchicines, colchifolines, colchicide, and novel N-acyl- and N-aroyldeacetylcolchicines. |
| AID94181 | Cytotoxicity was evaluated against KB-C2 cells at 0.1 ug/mL; No cytotoxicity | 2000 | Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22 | Synthesis and evaluation of 4-deacetoxyagosterol A as an MDR-modulator. |
| AID1566321 | Cell cycle arrest in human MCF7 cells assessed as accumulation in subG1 phase at 5 times of antiproliferative IC50 incubated for 48 hrs by propidium iodide based flow cytometry (Rvb = 9.19 %) | |||
| AID1566335 | Induction of cell cycle arrest in human ALL5 cells assessed as increase in 4 N DNA at 5 times of antiproliferative IC50 incubated for 24 hrs by propidium iodide based flow cytometry | |||
| AID1755839 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective. |
| AID394850 | Cytotoxicity against mouse B16-F1 cells after 48 hrs by SRB assay | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships. |
| AID1566311 | Cell cycle arrest in human ALL5 cells assessed as accumulation in subG1 phase at 5 times of antiproliferative IC50 incubated for 24 hrs by propidium iodide based flow cytometry (Rvb = 10.5 %) | |||
| AID1296733 | Cytotoxicity against human SKMES1 cells after 48 hrs by Celltiter-Glo luminescent cell viability assay | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology. |
| AID274829 | Cell cycle arrest in KB/HeLa cells by accumulation at G1 phase at 10 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID479367 | Cytotoxicity against vincristine-resistant human HL60 cells after 72 hrs MTS assay | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Phenylcinnamides as novel antimitotic agents. |
| AID1657526 | Cytotoxicity against human MCF7 cells after 68 hrs by MTT assay | 2020 | Journal of natural products, 05-22, Volume: 83, Issue:5 | Synthesis and Cytotoxicity Studies of Stilbene Long-Chain Fatty Acid Conjugates. |
| AID152691 | Potency against lymphocytic leukemia P388 screen in mice. | 1983 | Journal of medicinal chemistry, Oct, Volume: 26, Issue:10 | Biological effects of modified colchicines. 2. Evaluation of catecholic colchicines, colchifolines, colchicide, and novel N-acyl- and N-aroyldeacetylcolchicines. |
| AID120593 | Dose of compound which caused an average weight loss >3g in a set of mice or the death of one or more of the mice in the set in the P388 NCI screen. | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Biological effects of modified colchicines. Improved preparation of 2-demethylcolchicine, 3-demethylcolchicine, and (+)-colchicine and reassignment of the position of the double bond in dehydro-7-deacetamidocolchicines. |
| AID302074 | Antiproliferative activity against human MDA-MB-231 cells after 4 days by microplate assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | [(2-Phenylindol-3-yl)methylene]propanedinitriles inhibit the growth of breast cancer cells by cell cycle arrest in G(2)/M phase and apoptosis. |
| AID270729 | Inhibition of tubulin polymerization in porcine brain at 20 uM | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18 | Tubulin polymerization inhibitors with a fluorinated phthalimide skeleton derived from thalidomide. |
| AID1225534 | Toxicity in brine shrimp assessed as mortality | 2015 | Journal of natural products, Apr-24, Volume: 78, Issue:4 | Rubrumazines A-C, Indolediketopiperazines of the Isoechinulin Class from Eurotium rubrum MA-150, a Fungus Obtained from Marine Mangrove-Derived Rhizospheric Soil. |
| AID1238306 | Inhibition of hTERT mRNA expression in human HT-29 cells assessed as hTERT mRNA level at at 50 nM incubated for 48 hrs by RT-PCR method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes. |
| AID1569085 | Antiproliferative activity against human PC3 cells | |||
| AID1703298 | Induction of microtubule destabilization in mouse B16-F0 cells assessed as short and wrapped structure at 160 nM measured after 6 hrs by DAPI staining based immunofluorescent assay relative to control | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities. |
| AID1704310 | Induction of cell cycle arrest in human SW-620 cells assessed as accumulation at G2/M phase at 5 nM incubated for 48 hrs by RNase/PI staining based flow cytometry analysis (Rvb = 16 %) | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1736454 | Antiproliferative activity against drug resistant human K562 cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID459397 | Antiinvasive activity in human MDA-MB-231 cells assessed as cell invasion at 4 uM by BME cell invasion assay | 2010 | Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2 | Design and pharmacophore modeling of biaryl methyl eugenol analogs as breast cancer invasion inhibitors. |
| AID679099 | TP_TRANSPORTER: transepithelial transport of Colchicine at a concentration of 25 uM in Caco-2 cells | 2003 | Pharmaceutical research, Aug, Volume: 20, Issue:8 | Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. |
| AID1882903 | Inhibition of porcine brain tubulin polymerization measured at 1 min interval for 60 mins by fluorescence assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID397122 | Inhibition of HIV1 RT | |||
| AID553916 | Inhibition of tubulin polymerization after 60 mins | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. |
| AID1500600 | Antiproliferative activity against human A2780S cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents. |
| AID1740976 | Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Discovery of tertiary amide derivatives incorporating benzothiazole moiety as anti-gastric cancer agents in vitro via inhibiting tubulin polymerization and activating the Hippo signaling pathway. |
| AID1903067 | Antiproliferative activity against human HT-29 cells over expressing GLUT1 assessed as cell viability measured after 48 hrs by MTT assay relative to control | 2022 | Bioorganic & medicinal chemistry, 03-15, Volume: 58 | Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors. |
| AID1239200 | Inhibition of brain tubulin (unknown origin) polymerization measured up to 15 to 30 mins | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents. |
| AID214014 | Inhibition of tubulin polymerization | 1994 | Journal 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. |
| AID1431302 | Inhibition of lamb brain tubulin self assembly assessed as decrease in microtubule formation after 10 mins by turbidimetry/spectrometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID1167524 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at subG1 phase at 0.1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 1%) | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Synthesis and antiproliferative activity of 6-phenylaminopurines. |
| AID1233618 | Growth inhibition of human HepG2 cells assessed as inhibition of cell proliferation after 24 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jun-24, Volume: 99 | Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin polymerization inhibitors. |
| AID422577 | Cytotoxicity against human HT-29 cells after 72 hrs by methylene blue dye assay | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and evaluation of 3-aroylindoles as anticancer agents: metabolite approach. |
| AID514407 | Cytotoxicity against human HCT8 cells after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
| AID1549903 | Antiproliferative activity against human HL7702 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain. |
| AID1729584 | Inhibition of pig brain tubulin polymerization at 5 uM measured after 45 mins by turbidimetry based spectrophotometric method relative to control | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Imidazo[1,2-a]quinoxalines for melanoma treatment with original mechanism of action. |
| AID1809656 | Cytotoxicity against mouse BALB/3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Synthesis of thiocolchicine amine derivatives and evaluation of their antiproliferative activity. |
| AID303711 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G2M phase at 1 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1585585 | Cytotoxicity against mouse NIH/3T3 cells harboring MDR G185 after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents. |
| AID625294 | Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in O'Brien data | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID538697 | Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase after 24 hrs by flow cytometry relative to control | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Synthesis, molecular modeling and biological evaluation of guanidine derivatives as novel antitubulin agents. |
| AID724227 | Cytotoxicity against human MCF7 cells by SRB assay | 2013 | European journal of medicinal chemistry, Jan, Volume: 59 | Synthesis of novel chromene derivatives of expected antitumor activity. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID526949 | Cytotoxicity against human LNCAP cells after 48 hrs by sulforhodamine B assay | 2010 | Journal 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. |
| AID598212 | Cytotoxicity against human OVCAR3 cells assessed as reduction in viable cells after 24 hrs by trypan blue exclusion assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11 | Synthesis and characterisation of a novel tubulin-directed DO3A-colchicine conjugate with potential theranostic features. |
| AID1500599 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents. |
| AID1201728 | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID668214 | Antiproliferative activity against human WM164 cells after 48 hrs by SRB assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | New substituted 4H-chromenes as anticancer agents. |
| AID1420815 | Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay | |||
| AID303701 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at S phase at 0.3 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1414044 | Cytotoxicity against human DLD1 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1736449 | Antiproliferative activity against human LO2 cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1359658 | Resistance index, ratio of IC50 for human A2780T cells to IC50 for human A2780S cells | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Discovery of novel β-carboline/acylhydrazone hybrids as potent antitumor agents and overcome drug resistance. |
| AID1737802 | Inhibition of pig brain tubulin polymerization by absorbance based analysis | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Discovery of a chiral fluorinated azetidin-2-one as a tubulin polymerisation inhibitor with potent antitumour efficacy. |
| AID274819 | Cell cycle arrest in KB/HeLa cells by accumulation at G2/M phase at 1 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1636357 | Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID1221965 | Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID418791 | Growth inhibition of human SNU398 cells after 48 hrs | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Discovery and structure-activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers. |
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| AID1550797 | Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 0.016 uM measured after 24 hrs by DAPI staining based HCS analysis | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop. |
| AID23448 | Partition coefficient (logP) | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID1261387 | Cell cycle arrest in human 786-0 cells assessed as accumulation at G2/M phase at 1.25 nM after 24 hrs by propidium iodide based flow cytometric analysis (Rvb = 35.7 +/- 0.9%) | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Synthesis of thiophene-thiosemicarbazone derivatives and evaluation of their in vitro and in vivo antitumor activities. |
| AID721622 | Inhibition of bovine brain tubulin polymerization by fluorescence assay | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Design and synthesis of biaryl aryl stilbenes/ethylenes as antimicrotubule agents. |
| AID1503416 | Gastrointestinal toxicity in human HT-29 cells assessed as effect on membrane integrity at 5 uM incubated for 3 hrs by flow cytometry | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID1736529 | Induction of apoptosis in human HT-29 cells assessed as necrotic cells at 0.25 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.1 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1694408 | Antiproliferative activity against doxorubicin-resistant human LoVo/DX cells incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
| AID1863112 | Binding affinity to beta-tubulin colchicine binding site in human MGC-803 cells assessed as inhibition of EBI-beta-tubulin adduct band formation at 10 uM preincubated for 2 hrs followed by EBI addition and measured after 2 hrs by EBI competition based Wes | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway. |
| AID716407 | Induction of microtubule depolymerization in human HaCaT cells at 10 '-6 M by confocal microscopy | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4. |
| AID1899081 | Metabolic stability in human liver microsomes assessed as half-life at 1 uM in presence of NADPH measured by LC-MS/MS analysis | |||
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| AID658923 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at G0/G1 phase at 30 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 43.9 %) | 2012 | Journal 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. |
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| AID1426445 | Antiproliferative activity against human K562 cells after 48 hrs by Alamar blue dye based neubauer hemocytometer method | 2017 | Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2 | N-Heterocyclic (4-Phenylpiperazin-1-yl)methanones Derived from Phenoxazine and Phenothiazine as Highly Potent Inhibitors of Tubulin Polymerization. |
| AID1333474 | Effect on p21 mRNA expression in human MDA-MB-231 cells assessed as ratio of p21 to GAPDH expression level at 5 uM after 24 hrs by RT-PCR method (Rvb = 0.02 No_unit) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1414051 | Antifungal activity against Paecilomyces variotii BAM19 ATCC 18502 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1628433 | Induction of apoptosis in human A549 cells assessed as necrotic cells level at 40 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FACS flow cytometry (Rvb = 0.37%) | 2016 | Journal 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. |
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| AID1549911 | Antiproliferative activity against human HMEC cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain. |
| AID494502 | Inhibition of pig brain tubulin polymerization after 30 mins by turbidimetry | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis, antiproliferative activity and inhibition of tubulin polymerization by 1,5- and 1,8-disubstituted 10H-anthracen-9-ones bearing a 10-benzylidene or 10-(2-oxo-2-phenylethylidene) moiety. |
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| AID645072 | Cytotoxicity against human HCT116 cells after 96 hrs using tetracolor one | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Design, Synthesis, and Antitumor Activity of 4-Halocolchicines and Their Pro-drugs Activated by Cathepsin B. |
| AID383962 | Cytotoxicity against human UACC62 cells | 2008 | Journal 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. |
| AID732803 | Cytotoxicity against human CE81T cells assessed as growth inhibition | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Design, synthesis, biological evaluation and molecular modeling studies of 1-aryl-6-(3,4,5-trimethoxyphenyl)-3(Z)-hexen-1,5-diynes as a new class of potent antitumor agents. |
| AID1882733 | Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 24 hrs in presence of foetal bovine serum by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Recent advances of antitumor shikonin/alkannin derivatives: A comprehensive overview focusing on structural classification, synthetic approaches, and mechanisms of action. |
| AID1625728 | Binding affinity to tubulin in human HepG2 cells assessed as inhibition of microtubule network formation in cytosol at 100 nM after 16 to 24 hrs by DAPI staining-based immunofluorescence microscopy | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
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| AID1402708 | Antiproliferative activity against human LO2 cells after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design and characterization of α-lipoic acyl shikonin ester twin drugs as tubulin and PDK1 dual inhibitors. |
| AID1198453 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents. |
| AID1550796 | Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 0.08 uM measured after 24 hrs by DAPI staining based HCS analysis | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop. |
| AID1569053 | Antimigratory activity in human A375 cells assessed as wound closure at 5 nM after 22 hrs by scratch migration assay (Rvb = 60.7 +/- 3.5%) | |||
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| AID1142160 | Binding affinity to calf brain tubulin at 37 degC by fluorometric analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach. |
| AID756580 | Inhibition of tubulin polymerization in human DU145 cells after 24 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Design, synthesis, and biological evaluation of (E)-N-aryl-2-arylethenesulfonamide analogues as potent and orally bioavailable microtubule-targeted anticancer agents. |
| AID1695276 | Cytotoxicity against human HEK293 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
| AID1846761 | Inhibition of pig brain tubulin polymerization by spectrometric method | 2021 | European journal of medicinal chemistry, Oct-05, Volume: 221 | Isoxazole derivatives as anticancer agent: A review on synthetic strategies, mechanism of action and SAR studies. |
| AID1189602 | Inhibition of purified tubulin (unknown origin) assessed as critical concentration of tubulin required to produce assembly at 0.1 uM after 30 mins by spectrophotometry (Rvb = 3.3 +/- 0.1 uM) | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
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| AID342592 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 2 times GI50 after 24 hrs by flow cytometry | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Selective alkylation of beta(II)-tubulin and thioredoxin-1 by structurally related subsets of aryl chloroethylureas leading to either anti-microtubules or redox modulating agents. |
| AID1473708 | Antimigratory activity in human A375 cells assessed as wound closure at 5 nM after 22 hrs (Rvb = 60.7 +/- 3.5%) | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID1245422 | Growth inhibition of human K562 cells at 10 uM incubated for 24 hrs by trypan blue dye exclusion assay | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality. |
| AID721877 | Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition by trypan blue exclusion assay | 2013 | Journal 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. |
| AID1191358 | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and structure-activity relationships of pyridinyl-1H-1,2,3-triazolyldihydroisoxazoles as potent inhibitors of tubulin polymerization. |
| AID1229726 | Cytotoxicity in brine shrimp | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6 | Bisthiodiketopiperazines and Acorane Sesquiterpenes Produced by the Marine-Derived Fungus Penicillium adametzioides AS-53 on Different Culture Media. |
| AID697552 | Antiproliferative activity against human LNCAP cells after 48 hrs by SRB assay | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16 | Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents. |
| AID540235 | Phospholipidosis-negative literature compound | |||
| AID1189963 | Toxicity 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 fluorimetry | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Synthesis and biological evaluation of furanoallocolchicinoids. |
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| AID1593943 | Cytotoxicity against human PHK160b cells assessed as reduction in cell viability incubated for 48 hrs by LDH release assay | |||
| AID1428414 | Cytotoxicity against human HCT15 cells assessed as growth inhibition after 72 hrs by SRB assay | |||
| AID117073 | Lethal dose after the intraperitoneal injection in a group of 10 mice | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
| AID1763768 | Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by CCK8 assay | 2021 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 43 | Discovery of indoline derivatives as anticancer agents via inhibition of tubulin polymerization. |
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| AID1414058 | Fungicidal activity against Aspergillus versicolor BAM8 ATCC 11730 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
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| AID317728 | Inhibition of HIV1 reverse transcriptase | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
| AID98159 | Concentration required to inhibit proliferation of cultured lymphoid leukemia L1210 cells to 50% growth over 48 hours | 1992 | Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20 | Antimitotic agents: structure-activity studies with some pyridine derivatives. |
| AID1695277 | Cytotoxicity against human L929 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
| AID1473723 | Cytotoxicity against human PC3-TxR cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID524792 | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID1189607 | Inhibition of purified tubulin (unknown origin) assessed as critical concentration of tubulin required to produce assembly at 30 uM after 30 mins by spectrophotometry (Rvb = 3.3 +/- 0.1 uM) | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID397419 | Cytotoxicity against CHO cells assessed as chromatin condensation after 24 hrs by fluorescence microscopy | 2009 | Bioorganic & medicinal chemistry, Jun-15, Volume: 17, Issue:12 | Insecticidal heterolignans--tubuline polymerization inhibitors with activity against chewing pests. |
| AID1898101 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID1497175 | Inhibition of tubulin beta polymerization in human MCF7 cells after 18 to 24 hrs by ELISA based spectrophotometric analysis | |||
| AID1261386 | Cell cycle arrest in human 786-0 cells assessed as accumulation at S phase at 1.25 nM after 24 hrs by propidium iodide based flow cytometric analysis (Rvb = 14.6 +/- 1.3%) | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Synthesis of thiophene-thiosemicarbazone derivatives and evaluation of their in vitro and in vivo antitumor activities. |
| AID1500655 | Cell cycle arrest in human AGS cells assessed as accumulation at G0/G1 phase at 50 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 52.87%) | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of 9H-purins as potential tubulin polymerization inhibitors: Synthesis, biological evaluation and structure-activity relationships. |
| AID1500603 | Antiproliferative activity against HEK293 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents. |
| AID1785461 | Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by MTT assay | |||
| AID1503413 | Gastrointestinal toxicity in human HT-29 cells assessed as effect on EPR at 5 uM incubated for 3 hrs by flow cytometry | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID397291 | Cytotoxicity against human H1299 cells after 72 hrs | 2009 | Journal 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. |
| AID24566 | Retention time of the compound. | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Fluorinated colchicinoids: antitubulin and cytotoxic properties. |
| AID274791 | Antiproliferative activity against RKO cells by XTT assay after 48 hrs | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1883511 | Antiproliferative activity against human KYSE-450 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID1416435 | Anti-inflammatory activity in C57BL6 mouse model of CCl4-induced hepatic fibrosis assessed as reduction in inflammatory cell infiltration in hepatic tissue at 0.1 mg/kg, ig administered 2 times per week for 4 weeks by H and E staining based assay | 2017 | MedChemComm, Jul-01, Volume: 8, Issue:7 | 18α-Glycyrrhetinic acid monoglucuronide as an anti-inflammatory agent through suppression of the NF-κB and MAPK signaling pathway. |
| AID8461 | Cytotoxicity against human solid tumor lung carcinoma A549 cell line | 1993 | Journal 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 |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID342589 | Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B method | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Selective alkylation of beta(II)-tubulin and thioredoxin-1 by structurally related subsets of aryl chloroethylureas leading to either anti-microtubules or redox modulating agents. |
| AID1704308 | Induction of cell cycle arrest in human COLO357 cells assessed as accumulation at G1 phase at 5 nM incubated for 48 hrs by RNase/PI staining based flow cytometry analysis (Rvb = 72 %) | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1198454 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents. |
| AID1703287 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities. |
| AID780976 | Cytotoxicity against human KB-S15 cells overexpressing P-gp170/MDR assessed as growth inhibition after 72 hrs by methylene blue staining-based assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Furanylazaindoles: potent anticancer agents in vitro and in vivo. |
| AID335775 | Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 0.16 ug/mL | 1993 | Journal of natural products, Oct, Volume: 56, Issue:10 | Cytotoxic constituents from Hyptis verticillata. |
| AID486601 | Inhibition of bovine brain tubulin polymerization after 20 mins | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | Synthesis, molecular modeling and biological evaluation of dithiocarbamates as novel antitubulin agents. |
| AID1201727 | Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID132880 | Percent increase in life-span against in vivo P388 murine leukemia at a dose 0.5 mg/kg in trail 2 | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID1906176 | Antiproliferation activity against human MS751 cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay | |||
| AID540210 | Clearance in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1519676 | Retention time of compound at pH 7.4 by LC-UV analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies. |
| AID780985 | Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Furanylazaindoles: potent anticancer agents in vitro and in vivo. |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID1189148 | Antiproliferative activity against human HCT8 cells after 48 hrs by SRB method | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID613264 | Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue assay | 2011 | European 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. |
| AID1227902 | Inhibition of porcine tubulin polymerization at 100 uM incubated for 1 hr by turbidimetry | 2015 | Journal of natural products, Mar-27, Volume: 78, Issue:3 | Melampodium leucanthum, a source of cytotoxic sesquiterpenes with antimitotic activities. |
| AID78620 | Antiproliferative activity against the MDR positive human colon adenocarcinoma cell line HCT-15 | 2002 | Bioorganic & 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. |
| AID1703286 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities. |
| AID1703291 | Binding affinity to pig brain tubulin at 37 degree C without preincubation | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities. |
| AID670882 | Cytotoxicity against human HeLa cells after 48 hrs by WST-8 assay | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14 | Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents. |
| AID348169 | Cytotoxicity against human UCI101 cells after 48 hrs by alamar blue assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Design, synthesis and biological evaluation of novel stilbene-based antitumor agents. |
| AID1625736 | Resistance index, ratio of IC50 for beta-tubulin 3 overexpressing human A2780T cells to IC50 for human A2780S cells | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1435783 | Cytotoxicity against 2D culture of human HaCaT cells measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID19006 | Calculated membrane partition coefficient (Kmemb) | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 | Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability. |
| AID236904 | Partition coefficient (logP) | 2005 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13 | Synthesis of selective SRPK-1 inhibitors: novel tricyclic quinoxaline derivatives. |
| AID494515 | Cell cycle arrest in human KB/HeLa cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis, antiproliferative activity and inhibition of tubulin polymerization by 1,5- and 1,8-disubstituted 10H-anthracen-9-ones bearing a 10-benzylidene or 10-(2-oxo-2-phenylethylidene) moiety. |
| AID1163579 | Antiproliferative activity against human A2780S cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Synthesis and biological evaluation of novel millepachine derivatives as a new class of tubulin polymerization inhibitors. |
| AID1189144 | Antiproliferative activity against human MCF7 cells after 48 hrs by SRB method | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1261384 | Cell cycle arrest in human 786-0 cells assessed as accumulation at Sub G1 phase at 1.25 nM after 24 hrs by propidium iodide based flow cytometric analysis (Rvb = 3.0 +/- 0.7%) | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Synthesis of thiophene-thiosemicarbazone derivatives and evaluation of their in vitro and in vivo antitumor activities. |
| AID1758695 | Selectivity ratio of IC50 for human BEAS-2B cells to IC50 for human A549 cells | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Synthesis and structure-activity relationships of 5-phenyloxazole-2-carboxylic acid derivatives as novel inhibitors of tubulin polymerization. |
| AID1535571 | Antiproliferative activity against human A549 cells after 24 hrs by MTT assay | 2019 | Bioorganic & 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. |
| AID1846985 | Inhibition of pig brain tubulin polymerization at 10 uM measured after 20 mins by spectrometric method relative to control | |||
| AID1189604 | Inhibition of purified tubulin (unknown origin) assessed as critical concentration of tubulin required to produce assembly at 1 uM after 30 mins by spectrophotometry (Rvb = 3.3 +/- 0.1 uM) | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID719100 | Resistance factor, ratio of IC50 for human HeLa cells harboring class 3 beta tubulin mutant to IC50 for human HeLa cells | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation. |
| AID1582225 | Inhibition of porcine brain tubulin polymerization at 10 uM measured at 30 secs interval for 65 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties. |
| AID1267532 | Inhibition of Tubulin polymerization in human HeLa cells assessed as decrease in dynamic tyrosinated microtubules after 2 hrs by microplate reader analysis | 2016 | Bioorganic & 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. |
| AID1492839 | Antiproliferative activity against human CCRF-CEM cells after 96 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. |
| AID281698 | Induction of apoptosis in human T47D cells assessed as caspase activation after 24 hrs | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group. |
| AID461785 | Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue dye assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | 5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. |
| AID1882709 | Anticancer activity against human A875 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Recent advances of antitumor shikonin/alkannin derivatives: A comprehensive overview focusing on structural classification, synthetic approaches, and mechanisms of action. |
| AID347974 | Antiproliferative activity against human NCI-H460 cells by XTT assay | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1189586 | Cytotoxicity against human HT-29 cells after 3 days by MTT assay | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID317730 | Antiviral activity against HIV13B infected in human MT4 cells | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
| AID697853 | Inhibition of horse BChE at 2 mg/ml by Ellman's method | 2012 | Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22 | Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine. |
| AID1407721 | Induction of apoptosis in human A375 cells assessed as live cells at 10 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 94.2%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID347987 | Cell cycle arrest in human KB/HeLa cells assessed as S phase accumulation at 0.3 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID620717 | Inhibition of bovine tubulin assembly after 1 hr by fluorescence assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Design and synthesis of resveratrol-based nitrovinylstilbenes as antimitotic agents. |
| AID1238300 | Inhibition of VEGF mRNA expression in human HT-29 cells assessed as VEGF mRNA level at 5 ug/ml incubated for 48 hrs by RT-PCR method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes. |
| AID1817855 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and bioevaluation of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d]imidazoles as tubulin polymerization inhibitors. |
| AID1736483 | Cell cycle arrest in human HT29 cells assessed as cell accumulation at S phase at 0.5 uM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 20.44 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1221961 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1406861 | Antiproliferative activity against human EC109 cells after 48 hrs by MTT assay | |||
| AID636394 | Cell cycle arrest in mouse B16F10 cells assessed as accumulation at S phase at 1 ug/ml after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 12 %) | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis, biological evaluation and molecular docking studies of resveratrol derivatives possessing curcumin moiety as potent antitubulin agents. |
| AID1413547 | Inhibition of tubulin beta polymerization in human Caco2 cells after 48 hrs by ELISA | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | Synthesis and biological evaluation of novel 5-chloro- |
| AID347998 | Cell cycle arrest in human KB/HeLa cells assessed as G1 phase accumulation at 10 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID310119 | Cytotoxicity against human A2780 cells after 72 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | New functional assay of P-glycoprotein activity using Hoechst 33342. |
| AID744715 | Cytotoxicity against human HUVEC cells after 24 hrs by MTT assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID744706 | Antimitotic activity in human HeLa cells assessed as tubulin staining intensity at 1 nM after 24 hrs by Hoechst 33342 staining | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID537734 | Antifungal activity against yeast AD1-8u expressing Candida albicans CaMdr1p by agar disk diffusion assay | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans. |
| AID1694906 | Inhibition of tubulin polymerization (unknown origin) incubated for 1 hr by fluorescence based assay | 2020 | RSC medicinal chemistry, Mar-01, Volume: 11, Issue:3 | Application of triazoles as bioisosteres and linkers in the development of microtubule targeting agents. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1785090 | Cytotoxicity against paclitaxel-resistant human SW620/AD300 cells measured after 72 hrs by MTT assay | |||
| AID524794 | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID511362 | Cytotoxicity against MEF cells assessed as dead cells at 5 uM after 48 hrs by propidium iodide-based FACS flow cytometry | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17 | Glycopeptide dendrimer colchicine conjugates targeting cancer cells. |
| AID1527067 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
| AID1785511 | Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay | |||
| AID150343 | Cytotoxic activity against P388 mouse lymphocytic leukemia cell line | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Fluorinated colchicinoids: antitubulin and cytotoxic properties. |
| AID1492840 | Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. |
| AID98510 | In vitro cytotoxicity against L1210 (murine leukemia) cells. | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Antitubulin effects of derivatives of 3-demethylthiocolchicine, methylthio ethers of natural colchicinoids, and thioketones derived from thiocolchicine. Comparison with colchicinoids. |
| AID383960 | Cytotoxicity against human HCT15 cells | 2008 | Journal 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. |
| AID401022 | Toxicity in intramuscular dosed mouse | |||
| AID1863088 | Antiproliferative activity against human KYSE-450 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway. |
| AID1773139 | Inhibition of pig brain tubulin polymerization at 10 uM by spectrometric method relative to control | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery 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. |
| AID774671 | Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18 | New phenstatin-fatty acid conjugates: synthesis and evaluation. |
| AID29423 | HPLC capacity factor (k') | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID1167522 | Antiproliferative activity against human CEM cells assessed as inhibition of cell proliferation after 96 hrs by Coulter counter based cell counting method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Synthesis and antiproliferative activity of 6-phenylaminopurines. |
| AID404618 | Antiproliferative activity against human HCT116 cells after 72 hrs | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | New C5-alkylated indolobenzazepinones acting as inhibitors of tubulin polymerization: cytotoxic and antitumor activities. |
| AID256881 | Cell cycle arrest in A431 cells by accumulation at G2/M phase cell | 2005 | Bioorganic & 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. |
| AID75546 | Ability to inhibit the dibutyryl-cAMP-induced change of an immature glioma cell to a mature, differentiated astrocyte by in vitro astrocytoma assay at 10 ug/mL dose (Experiment #1); value may range from 91 to up | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | In vivo antitumor activity of 6-benzyl-1,3-benzodioxole derivatives against the P388, L1210, B16, and M5076 murine models. |
| AID331397 | Antiproliferative activity against human M21 cells | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Cycloalkyl-substituted aryl chloroethylureas inhibiting cell cycle progression in G0/G1 phase and thioredoxin-1 nuclear translocation. |
| AID1872836 | Cytotoxicity against human SK-BR-3 cells treated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Tandem construction of biological relevant aliphatic 5-membered N-heterocycles. |
| AID1586074 | Inhibition of bovine brain tubulin polymerization measured every 30 secs for 30 mins by turbidimetric assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
| AID1566312 | Cell cycle arrest in human ALL5 cells assessed as accumulation in subG1 phase at 5 times of antiproliferative IC50 incubated for 48 hrs by propidium iodide based flow cytometry (Rvb = 11 %) | |||
| AID383959 | Cytotoxicity against human K562 cells | 2008 | Journal 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. |
| AID627397 | Antiproliferative activity against mouse L1210 after 48 hrs by SRB assay | 2011 | European 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. |
| AID1389579 | Antiarthritic activity in MSU-induced acute gouty arthritis Sprague-Dawley rat model assessed as reduction in ankle swelling by measuring perimeter of ankle at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last do | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID605766 | Antiproliferative activity against human HT1080 cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID1296731 | Cytotoxicity against human HeLa cells after 48 hrs by Celltiter-Glo luminescent cell viability assay | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology. |
| AID401548 | Cytotoxicity against human HL60 cells after 48 hrs by MTT assay | 2004 | Journal of natural products, May, Volume: 67, Issue:5 | Chemical constituents from the mangrove plant, Aegiceras corniculatum. |
| AID1142135 | Antiproliferative activity against human HeLa cells after 4 days by coulter counter analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach. |
| AID1414045 | Cytotoxicity against human LoVo cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1382725 | Disruption of microtubule network in human A498 cells at 5 times antiproliferative IC50 after 1 to 12 hrs by immunofluorescence assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Enediynes bearing polyfluoroaryl sulfoxide as new antiproliferative agents with dual targeting of microtubules and DNA. |
| AID1903074 | Cytotoxicity against HUVEC measured after 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 03-15, Volume: 58 | Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors. |
| AID1807448 | Inhibition of microtubule (unknown origin) polymerization at 5 uM | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Design, structure-activity relationship study and biological evaluation of the thieno[3,2-c]isoquinoline scaffold as a potential anti-cancer agent. |
| AID1179660 | Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 1 ug/ml after 24 hrs by flow cytometry (Rvb = 13.05 %) | 2014 | Bioorganic & 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. |
| AID461782 | Antiproliferative activity against human KB cells after 72 hrs by methylene blue dye assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | 5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. |
| AID1582227 | Binding affinity to porcine brain tubulin polymerization by surface plasmon analysis analysis | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties. |
| AID735029 | Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells in S phase at 2uM concentration after 24 hrs by propidium iodide staining based cytofluorimetric analysis (Rvb = 26.17%) | 2013 | European 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. |
| AID1437255 | Cytotoxicity against human K562 cells assessed as growth inhibition after 5 days by MTT assay | 2017 | Bioorganic & 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. |
| AID1755838 | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective. |
| AID348168 | Cytotoxicity against human SNU423 cells after 48 hrs by alamar blue assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Design, synthesis and biological evaluation of novel stilbene-based antitumor agents. |
| AID1233620 | Inhibition of bovine brain tubulin polymerization extent after 20 mins by turbidimetrically | 2015 | European journal of medicinal chemistry, Jun-24, Volume: 99 | Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin polymerization inhibitors. |
| AID1378143 | Growth inhibition of human WM266.4 cells up to 25 uM cotreated with camptothecin measured after 24 hrs by XTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma. |
| AID298660 | Increase in caspase 3 activation in Jurkat cells at 5 uM | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Discovery and investigation of antiproliferative and apoptosis-inducing properties of new heterocyclic podophyllotoxin analogues accessible by a one-step multicomponent synthesis. |
| AID596140 | Antiproliferative activity against human SKOV3 cells after 72 hrs by sulforhodamine B assay | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9 | Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors. |
| AID1407724 | Induction of apoptosis in human A375 cells assessed as necrotic cells at 10 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.13%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1628410 | Displacement of [3H]colchicine from biotinylated porcine tubulin at 1 uM incubated for 2 hrs by competition scintillation proximity | 2016 | Journal 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. |
| AID605768 | Antiproliferative activity against human SKOV3 cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID302076 | Inhibition of cell growth in human A431 cells after 3 days by microplate assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | [(2-Phenylindol-3-yl)methylene]propanedinitriles inhibit the growth of breast cancer cells by cell cycle arrest in G(2)/M phase and apoptosis. |
| AID1594093 | Inhibition of goat brain tubulin polymerization | |||
| AID1566297 | Antiproliferative activity against human LoVo/DX cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay | |||
| AID605773 | Resistant ratio of IC50 for paclitaxel-resistant CHO-VV 3-2 cells to IC50 for CHO cells | 2011 | Journal 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. |
| AID368327 | Cytotoxicity against human A549 cells after 24 hrs by YO-PRO-1 assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Isolation, structure elucidation and cytotoxic evaluation of endiandrin B from the Australian rainforest plant Endiandra anthropophagorum. |
| AID1316905 | Inhibition of microtubule associated proteins free porcine brain alpha/beta-tubulin polymerization measured after 10 mins by thermostatic spectrophotometric method | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Discovery of O |
| AID274812 | Cell cycle arrest in KB/HeLa cells by accumulation at S phase at 3.16 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID733791 | Cytotoxicity against human SPC-A1 cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID303707 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at S phase at 316 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
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| AID1755840 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective. |
| AID679691 | TP_TRANSPORTER: slot-blot analysis in vivo CF I mouse, liver | 1994 | Journal of hepatology, Nov, Volume: 21, Issue:5 | Effect of colchicine and heat shock on multidrug resistance gene and P-glycoprotein expression in rat liver. |
| AID1237707 | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay | 2015 | Journal 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. |
| AID700073 | Immunosuppressant activity in mouse splenocytes by mixed-leukocyte reaction assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21 | Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties. |
| AID1189601 | Resistance factor, ratio of IC50 for human A2780AD cells to IC50 for human A2780 cells | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID150759 | P-gp activity was measured by a direct transport assay, using polarized LLC-mdr1a epithelial cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
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| AID303689 | Cytotoxicity against human SF268 cells after 48 hrs by XTT assay | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID428054 | Immunosuppressive activity in LPS-activated B lymphocyte assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Design, synthesis and identification of novel colchicine-derived immunosuppressant. |
| AID732804 | Cytotoxicity against human SAS cells assessed as growth inhibition | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Design, synthesis, biological evaluation and molecular modeling studies of 1-aryl-6-(3,4,5-trimethoxyphenyl)-3(Z)-hexen-1,5-diynes as a new class of potent antitumor agents. |
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| AID424441 | Inhibition of tubulin polymerization | 2009 | Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10 | Discovery of substituted N'-(2-oxoindolin-3-ylidene)benzohydrazides as new apoptosis inducers using a cell- and caspase-based HTS assay. |
| AID679469 | TP_TRANSPORTER: ATP hydrolysis in reconstituted proteoliposomes | 1992 | Proceedings of the National Academy of Sciences of the United States of America, Sep-15, Volume: 89, Issue:18 | Partial purification and reconstitution of the human multidrug-resistance pump: characterization of the drug-stimulatable ATP hydrolysis. |
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| AID1189143 | Antiproliferative activity against human SW480 cells after 48 hrs by SRB method | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1167519 | Antiproliferative activity against mouse MBEC assessed as inhibition of cell proliferation after 3 days by Coulter counter based cell counting method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Synthesis and antiproliferative activity of 6-phenylaminopurines. |
| AID1882893 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1736537 | Induction of apoptosis in human HT-29 cells assessed as necrotic cells at 1 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.1 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
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| AID1850715 | Cytotoxicity against human HEK293 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2022 | RSC medicinal chemistry, May-25, Volume: 13, Issue:5 | Morpholine substituted quinazoline derivatives as anticancer agents against MCF-7, A549 and SHSY-5Y cancer cell lines and mechanistic studies. |
| AID1420816 | Antiproliferative activity against mouse B16F10 cells after 72 hrs by MTT assay | |||
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| AID1750230 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | |||
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| AID1435786 | Induction of apoptosis in 2D culture of human Colo-357 cells assessed as accumulation at G2/M phase at 1 uM measured after 72 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1185444 | Displacement of [3H]colchicine from long-chain biotin-labeled tubulin (unknown origin) at 1 uM after 2 hrs by competition-binding scintillation proximity assay | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Concise syntheses of 7-anilino-indoline-N-benzenesulfonamides as antimitotic and vascular disrupting agents. |
| AID1832149 | Inhibition 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 assay | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors. |
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| AID1669118 | Inhibition of porcine brain tubulin polymerization assessed as residual tubulin polymerization at 10 uM in presence of 0.8 M glutamate incubated for 30 mins by SDS-PAGE analysis (Rvb = 84.8 +/- 9.9 %) | |||
| AID1237725 | Cytotoxicity against human MESSA cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2015 | Journal 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. |
| AID1695281 | Induction of cell cycle arrest in human L929 cells assessed as G2/M phase at 5 uM incubated for 72 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 8 %) | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
| AID1694406 | Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
| AID1899069 | Antiproliferative activity against human KB/VCR cells measured after 72 hrs by SRB assay | |||
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| AID1406895 | Inhibition of EBI binding to beta-tubulin colchicine binding site in human MGC803 cells at 5 uM preincubated for 2 hrs followed by EBI addition and measured after 2 hrs by Western blot analysis | |||
| AID744717 | Cytotoxicity against human REH cells after 48 hrs by MTT assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID749384 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | The discovery of colchicine-SAHA hybrids as a new class of antitumor agents. |
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| AID1785504 | Antiproliferative activity against human HepG2 cells incubated for 72 hrs by MTT assay | |||
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| AID1428413 | Cytotoxicity against human HeLa cells assessed as growth inhibition after 72 hrs by SRB assay | |||
| AID1897656 | Induction of cell cycle arrest in human HCT-116 cells assessed as S phase cells at 20 nM measured after 48 hrs by propidium iodide/RNase staining based flow cytometry analysis (Rvb = 61.51 %) | 2022 | Bioorganic & medicinal chemistry, 12-15, Volume: 76 | Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities. |
| AID1694404 | Antiproliferative activity against human ALL5 cells incubated for 120 hrs followed by MTT addition further incubated for 48 hrs | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
| AID1077391 | Inhibition of microtubule depolymerization in rat A10 cells after 18 hrs by immunofluorescence assay | 2013 | MedChemComm, , Volume: 4, Issue:2 | Developing novel C-4 analogues of pyrrole-based antitubulin agents: weak but critical hydrogen bonding in the colchicine site. |
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| AID1272832 | Inhibition of N-terminal MKLP2 (56 to 505 residues) ATPase basal activity isolated from human hepatocellular carcinoma cells by pyruvate kinase/lactate dehydrogenase enzyme linked assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | New MKLP-2 inhibitors in the paprotrain series: Design, synthesis and biological evaluations. |
| AID1431304 | Induction of abnormal lamb brain tubulin polymer formation at 50 uM after 10 mins by turbidimetry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID1566331 | Induction of apoptosis in human ALL5 cells assessed as increase in 85 kDa PARP expression at 43 uM incubated for 48 hrs by immunoblot analysis | |||
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| AID1492842 | Antiproliferative activity against human LCLC-103H cells after 96 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. |
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| AID312974 | Growth inhibition of human T47D cells after 48 hrs | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions. |
| AID1221972 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1807383 | Resistance index, ratio of IC50 for cytotoxicity against paclitaxel resistant human A-375/TxR cells to IC50 cytotoxicity against human A-375 cells | |||
| AID355584 | Antiproliferative activity against mouse P388 cells at 1 ug after 48 hrs by two-layer agar-diffusion method | |||
| AID614580 | Effect on microtubule network in human A549 cells assessed as microtubule depolymerization at 1 uM after 8 hrs by immunofluorescence microscopic analysis | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | Synthesis and SAR requirements of adamantane-colchicine conjugates with both microtubule depolymerizing and tubulin clustering activities. |
| AID90441 | Cytotoxic activity against human colon adenocarcinoma RKO cells with ectopic inducible expression of cyclin-dependent kinase inhibitor p27kip1 | 2003 | Journal 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. |
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| AID636395 | Cell cycle arrest in mouse B16F10 cells assessed as accumulation at G2/M phase at 1 ug/ml after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 18 %) | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis, biological evaluation and molecular docking studies of resveratrol derivatives possessing curcumin moiety as potent antitubulin agents. |
| AID1382775 | Antiproliferative activity against human CEM cells after 96 hrs by coulter counting method | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity. |
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| AID1822546 | Disruption of microtubule network in human A2780S cells assessed as bundling of microtubule fibers in cytosol at 100 nM for 24 hrs | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents. |
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| AID288695 | Growth inhibition of human M21 cells after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Alkylation potency and protein specificity of aromatic urea derivatives and bioisosteres as potential irreversible antagonists of the colchicine-binding site. |
| AID125974 | Inhibition of bovine brain microtubule polymerization; No data | 2002 | Bioorganic & 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. |
| AID1110725 | Antitumor activity against Homo sapiens (human) HCT116 cells | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Structure-activity relationships of phenylcyclohexene and biphenyl antitubulin compounds against plant and mammalian cells. |
| AID374355 | Selectivity index, ratio of CC50 for human WI38 cells preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay to EC50 for BKV Gardner ATCC VR837 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12 | BK Virus replication in vitro: limited effect of drugs interfering with viral uptake and intracellular transport. |
| AID721878 | Cytotoxicity against human HCT116 assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay | 2013 | Journal 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. |
| AID297420 | Growth inhibition of human KB-vin10 cells after 72 hrs by methylene blue dye assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | 4- and 5-aroylindoles as novel classes of potent antitubulin agents. |
| AID213841 | Compound was evaluated for its ability to inhibit polymerization of tubulin | 2000 | Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5 | Antimitotic activity of moroidin, a bicyclic peptide from the seeds of Celosia argentea. |
| AID404608 | Cytotoxicity against human KB cells after 72 hrs | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | New C5-alkylated indolobenzazepinones acting as inhibitors of tubulin polymerization: cytotoxic and antitumor activities. |
| AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID355578 | Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay | |||
| AID249641 | Effect to arrest G2/M-phase on HEK 293 cells at 10 uM was determined | 2005 | Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8 | Discovery of S-phase arresting agents derived from noscapine. |
| AID1657525 | Cytotoxicity against HEK293 cells after 68 hrs by MTT assay | 2020 | Journal of natural products, 05-22, Volume: 83, Issue:5 | Synthesis and Cytotoxicity Studies of Stilbene Long-Chain Fatty Acid Conjugates. |
| AID1193497 | Thermodynamic equilibrium solubility, log S of the compound PBS at pH 7.4 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
| AID75556 | Ability to inhibit the dibutyryl-cAMP-induced change of an immature glioma cell to a mature, differentiated astrocyte by in vitro astrocytoma assay at 1 ug/mL dose (Experiment #2); value may range from 51 to 70 | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | In vivo antitumor activity of 6-benzyl-1,3-benzodioxole derivatives against the P388, L1210, B16, and M5076 murine models. |
| AID596139 | Antiproliferative activity against human A431 cells after 72 hrs by sulforhodamine B assay | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9 | Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors. |
| AID711182 | Cytotoxicity against human MDA-MB-231 cells after 96 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID1185195 | Binding affinity to bovine brain tubulin assessed as half life of compound-tubulin complex | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Novel 9'-substituted-noscapines: synthesis with Suzuki cross-coupling, structure elucidation and biological evaluation. |
| AID23476 | Partition coefficient (logP) | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Fluorinated colchicinoids: antitubulin and cytotoxic properties. |
| AID1507349 | Cell cycle arrest in human HT-29 cells assessed as accumulation at sub-G1 phase at 1.25 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 3.5 +/- 0.7%) | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Thiosemicarbazones and 4-thiazolidinones indole-based derivatives: Synthesis, evaluation of antiproliferative activity, cell death mechanisms and topoisomerase inhibition assay. |
| AID1704307 | Induction of cell cycle arrest in human COLO357 cells assessed as accumulation at G2/M phase at 5 nM incubated for 48 hrs by RNase/PI staining based flow cytometry analysis (Rvb = 13 %) | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1569055 | Antimigratory activity in human RPMI7951 cells assessed as wound closure at 25 nM after 18 hrs by scratch migration assay (Rvb = 71.8 +/- 1.8%) | |||
| AID1201731 | Cytotoxicity against human SNU16 cells assessed as growth inhibition after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID1407722 | Induction of apoptosis in human A375 cells assessed as early apoptotic cells at 10 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.35%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID333741 | Cytotoxicity against human MDA-MB-423 cells after 48 hrs by MTT assay | 2004 | Journal of natural products, Dec, Volume: 67, Issue:12 | Isomalabaricane-type compounds from the marine sponge Rhabdastrella aff. distincta. |
| AID274790 | Antiproliferative activity against RKO cells with ectopic-induced p27kip1-expression by XTT assay after 48 hrs | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID627400 | Antiproliferative activity against human DU145 after 48 hrs by SRB assay | 2011 | European 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. |
| AID1424776 | Inhibition of tubulin polymerization (unknown origin) preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric method | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors. |
| AID1566319 | Cell cycle arrest in human MCF7 cells assessed as accumulation in G1 phase at 5 times of antiproliferative IC50 incubated for 72 hrs by propidium iodide based flow cytometry (Rvb = 58 %) | |||
| AID379862 | Inhibition of tubulin polymerization at 1 ug/mL by tubulin assembly assay | 1999 | Journal of natural products, Jun, Volume: 62, Issue:6 | Six triterpenoid saponins from Mmaesa laxiflora. |
| AID1817856 | Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and bioevaluation of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d]imidazoles as tubulin polymerization inhibitors. |
| AID1628402 | Growth inhibition of human A549 cells incubated for 48 hrs by MTT assay | 2016 | Journal 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. |
| AID312972 | Induction of apoptosis in human HCT116 cells assessed as caspase activation after 24 hrs by HTS assay | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions. |
| AID1402788 | Inhibition of microtubule polymerization (unknown origin) at 0.5 uM after 24 hrs by immunoblot | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design and characterization of α-lipoic acyl shikonin ester twin drugs as tubulin and PDK1 dual inhibitors. |
| AID1407713 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1226626 | Inhibition of tubulin polymerization in human HeLa cells assessed as reduction of microtubule formation at 100 nM after 6 hrs by DAPI staining-based immunofluorescence assay | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10 | Methyl 3-((6-methoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)amino)benzoate (GN39482) as a tubulin polymerization inhibitor identified by MorphoBase and ChemProteoBase profiling methods. |
| AID758701 | Cell cycle arrest in human K562 cells assessed as accumulation at S phase at 10 uM after 24 hrs by annexin V-FITC/PI staining-based FACS flow cytometric analysis (Rvb = 24 +/- 0.8%) | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID492476 | Inhibition of tubulin polymerization | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3 | Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach. |
| AID342593 | Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 2 times GI50 after 24 hrs by flow cytometry | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Selective alkylation of beta(II)-tubulin and thioredoxin-1 by structurally related subsets of aryl chloroethylureas leading to either anti-microtubules or redox modulating agents. |
| AID1407743 | Induction of apoptosis in human A375 cells assessed as late apoptotic cells at 1000 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.96%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID605957 | Inhibition of tubulin polymerization in Potorous tridactylus Ptk2 cells assessed as destruction of microtubule network at 5 uM after 1 hr by immunofluorescence assay | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID394852 | Cytotoxicity against human DU145 cells after 48 hrs by SRB assay | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships. |
| AID1903073 | Selectivity ratio of IC50 for human Hep3B cells to IC50 for human HT-29 cells | 2022 | Bioorganic & medicinal chemistry, 03-15, Volume: 58 | Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors. |
| AID1189594 | Depolymerization of microtubule cytoskeleton in human A549 cells assessed as DNA forming a ball without microtubules at 50 nM after 24 hrs by hoechst 33342-based fluorescence microscopy | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID1384334 | Inhibition of VEGF protein secretion in human HT-29 cells assessed as VEGF protein level at 10 nM after 48 hrs by ELISA (Rvb = 100%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID348011 | Displacement of [3H]Colchicine from pig biotinylated tubulin after 2 hrs by SPA | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1569087 | Resistance index, ratio of IC50 for human PC3-TxR cells to IC50 for human PC3 cells | |||
| AID588210 | Human drug-induced liver injury (DILI) modelling dataset from Ekins et al | 2010 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12 | A predictive ligand-based Bayesian model for human drug-induced liver injury. |
| AID354543 | Cytotoxicity against rat C6 cells assessed as cell release at 50 ug/mL to 2.5 mg/mL after 5 hrs by MTT assay in absence of db-cAMP | 1996 | Journal of natural products, Dec, Volume: 59, Issue:12 | Cell-based screen for identification of inhibitors of tubulin polymerization. |
| AID75538 | Ability to inhibit the dibutyryl-cAMP-induced change of an immature glioma cell to a mature, differentiated astrocyte by in vitro astrocytoma assay at 0.1 ug/mL dose (Experiment #1); value may range from 0 to 5 | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | In vivo antitumor activity of 6-benzyl-1,3-benzodioxole derivatives against the P388, L1210, B16, and M5076 murine models. |
| AID331404 | Cell cycle arrest in human MCF7 cells assessed as increase in G0/G1 phase accumulation at 0.1 uM after 16 hrs by FACS analysis | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Cycloalkyl-substituted aryl chloroethylureas inhibiting cell cycle progression in G0/G1 phase and thioredoxin-1 nuclear translocation. |
| AID274822 | Cell cycle arrest in KB/HeLa cells by accumulation at G2/M phase at 31.6 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID409674 | Cytotoxicity against human Raji cells after 48 hrs by luminescence cell viability assay | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 | Synthesis and characterization of BODIPY-labeled colchicine. |
| AID1421770 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Conformation impacts on the bioactivities of SMART analogues. |
| AID538696 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase after 24 hrs by flow cytometry relative to control | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Synthesis, molecular modeling and biological evaluation of guanidine derivatives as novel antitubulin agents. |
| AID744707 | Antimitotic activity in human HeLa cells assessed as tubulin staining intensity at 5 nM after 24 hrs by Hoechst 33342 staining | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID303714 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G2M phase at 31.6 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1407742 | Induction of apoptosis in human A375 cells assessed as early apoptotic cells at 1000 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.4%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1703284 | Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities. |
| AID1785508 | Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay | |||
| AID1636440 | Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID603022 | Inhibition of purified bovine brain tubulin microtubule assembly at 5 to 10 uM | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis, antiproliferative activity, and mechanism of action of a series of 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID1898098 | Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID214361 | Tested for the inhibition of polymerization rate of tubulin microtubule assembly. | 1980 | Journal of medicinal chemistry, May, Volume: 23, Issue:5 | Structure--antitubulin activity relationship in steganacin congeners and analogues. Inhibition of tubulin polymerization in vitro by (+/-)-isodeoxypodophyllotoxin. |
| AID155864 | In vitro cytotoxic activity (growth inhibition) of compound against PC-12 human cancer cell line was determined | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity. |
| AID716405 | Induction of morphological changes in human SKv-a cells assessed as cell detachment at 10 '-6 M by confocal microscopy | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4. |
| AID1473724 | Resistance index, ratio of IC50 for human PC3-TxR cells to IC50 for human PC3 cells | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID1582223 | Resistance index, ratio of IC50 for antiproliferative activity against human M14/LCC6MDR1 cells to IC50 for antiproliferative activity against human M14 cells | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties. |
| AID1875313 | Cytotoxicity in human MCF7 cells assessed as growth inhibition level after 48 hrs by SRB assay | 2022 | Journal of natural products, 10-28, Volume: 85, Issue:10 | Resin Glycosides from |
| AID427907 | Induction of apoptosis in human T47D cells assessed as caspase activation after 48 hrs | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents. |
| AID390905 | Inhibition of tubulin polymerization | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Novel microtubule-interacting phenoxy pyridine and phenyl sulfanyl pyridine analogues for cancer therapy. |
| AID659042 | Induction of cell cycle arrest in human HeLa cells assessed as accumulation at S phase at 30 nM after 18 hrs by propidium iodide based flow cytometric analysis (Rvb = 39.9 %) | 2012 | Journal 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. |
| AID663036 | Antiproliferative activity against human MDA-MB-435 cells by sulforhodamine B assay | 2012 | ACS medicinal chemistry letters, Jan-12, Volume: 3, Issue:1 | Pyrrole-Based Antitubulin Agents: Two Distinct Binding Modalities are Predicted for C-2 Analogs in the Colchicine Site. |
| AID657609 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2012 | Bioorganic & 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. |
| AID401551 | Cytotoxicity against human U937 cells after 48 hrs by MTT assay | 2004 | Journal of natural products, May, Volume: 67, Issue:5 | Chemical constituents from the mangrove plant, Aegiceras corniculatum. |
| AID611270 | Cytotoxicity against human SF268 cells after 48 hrs by XTT assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Phenylimino-10H-anthracen-9-ones as novel antimicrotubule agents-synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID735505 | Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells in G0/G1 phase at 8 uM concentration after 24 hrs by propidium iodide staining based cytofluorimetric analysis (Rvb = 39.55%) | 2013 | European 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. |
| AID1142133 | Antiproliferative activity against mouse L1210 cells after 48 to 96 hrs by coulter counter analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach. |
| AID1657523 | Cytotoxicity against human KB3-1 cells after 68 hrs by MTT assay | 2020 | Journal of natural products, 05-22, Volume: 83, Issue:5 | Synthesis and Cytotoxicity Studies of Stilbene Long-Chain Fatty Acid Conjugates. |
| AID662406 | Cytotoxicity against human A549 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12 | Synthesis, characterization and in vitro anti-tumor activities of matrine derivatives. |
| AID1503404 | Induction of cell cycle arrest in human Colo-357 cells assessed as accumulation at G phase at 5 uM incubated for 72 hrs by propidium iodide staining based flow cytometry (Rvb = 56.6%) | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID612257 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Exploration of acridine scaffold as a potentially interesting scaffold for discovering novel multi-target VEGFR-2 and Src kinase inhibitors. |
| AID1191357 | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and structure-activity relationships of pyridinyl-1H-1,2,3-triazolyldihydroisoxazoles as potent inhibitors of tubulin polymerization. |
| AID1183706 | Cytotoxicity against human MCF7 cells after 96 hrs by Giemsa staining-based light microscopy | 2014 | Journal 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. |
| AID412960 | Growth inhibition of human KB cells after 72 hrs by methylene blue dye assay | 2008 | Journal 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. |
| AID1882894 | Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID335778 | Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 0.00128 ug/mL | 1993 | Journal of natural products, Oct, Volume: 56, Issue:10 | Cytotoxic constituents from Hyptis verticillata. |
| AID1453485 | Induction of microtubule disruption in human HeLa cells assessed as short microtubule at 1 uM after 6 hrs by DAPI staining based immunofluorescence microscopic analysis | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | One-pot synthesis and biological evaluation of N-(aminosulfonyl)-4-podophyllotoxin carbamates as potential anticancer agents. |
| AID288668 | Growth inhibition of human MCF7 cells after 48 hrs | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies. |
| AID336347 | Antimitotic activity against rat ASK cells assessed as reversal of astrocyte morphology at 0.8 ug/ml | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID1504736 | Solubility of the compound in water irradiated with UV light | |||
| AID1756944 | Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | An insight into the anticancer potential of carbamates and thiocarbamates of 10-demethoxy-10-methylaminocolchicine. |
| AID1566298 | Antiproliferative activity against mouse BALB/3T3 cells assessed as reduction in cell viability incubated for 120 hrs by MTT assay | |||
| AID383963 | Cytotoxicity against human OVCAR-3 cells | 2008 | Journal 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. |
| AID1110731 | Mitotic arrest in Nicotiana tabacum (tobacco) root suspension-cultured cells assessed as accumulation of cells in metaphase by cytological staining assay | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Structure-activity relationships of phenylcyclohexene and biphenyl antitubulin compounds against plant and mammalian cells. |
| AID394853 | Cytotoxicity against human PC3 cells after 48 hrs by SRB assay | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships. |
| AID401549 | Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay | 2004 | Journal of natural products, May, Volume: 67, Issue:5 | Chemical constituents from the mangrove plant, Aegiceras corniculatum. |
| AID524795 | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | 2009 | Nature chemical biology, Oct, Volume: 5, Issue:10 | Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. |
| AID1384325 | Downregulation of VEGF gene expression in human HT-29 cells assessed as VEGF mRNA level at 10 nM after 48 hrs by RT-PCR method (Rvb = 100%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID1872835 | Cytotoxicity against human PC-3 cells treated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Tandem construction of biological relevant aliphatic 5-membered N-heterocycles. |
| AID1519674 | Chromatographic hydrophobicity index of compound at 250 uM at pH 7.4 by HPLC analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies. |
| AID2968 | Inhibitory activity against Taxol resistant 1A9 cell lines | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | Stabilization of microtubules by Combretastatin D derivatives. |
| AID1582221 | Resistance index, ratio of IC50 for antiproliferative activity against human DU145-TxR cells to IC50 for antiproliferative activity against human DU145 cells | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties. |
| AID342503 | Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 2 times GI50 after 24 hrs by flow cytometry | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Aromatic 2-chloroethyl urea derivatives and bioisosteres. Part 2: Cytocidal activity and effects on the nuclear translocation of thioredoxin-1, and the cell cycle progression. |
| AID157341 | Inhibitory activity against Taxol resistant PTX10 cell lines | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | Stabilization of microtubules by Combretastatin D derivatives. |
| AID658922 | Induction 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 %) | 2012 | Journal 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. |
| AID756578 | Inhibition of tubulin polymerization in human DU145 cells at 10 nM pretreated with paclitaxel for 24 hrs followed by compound treatment for 4 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Design, synthesis, and biological evaluation of (E)-N-aryl-2-arylethenesulfonamide analogues as potent and orally bioavailable microtubule-targeted anticancer agents. |
| AID1316907 | Inhibition of [3H]vinblastine binding to microtubule associated proteins free porcine brain alpha/beta-tubulin assessed as remaining radiolabeled binding at 100 uM measured after 5 mins by centrifugal gel filtration method relative to control | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Discovery of O |
| AID1384306 | Downregulation of c-Myc gene expression in human HT-29 cells assessed as c-Myc mRNA level at 40 nM after 48 hrs by RT-PCR method (Rvb = 100%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID1628420 | Induction of apoptosis in human A549 cells assessed as induction of nucleus fragmentation at 40 nM incubated for 24 hrs microscopy | 2016 | Journal 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. |
| AID711187 | Resistance factor, ratio of IC50 for human SW780AD cells expressing p-gp to IC50 for human SW780 cells | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID1305705 | Permeability across apical side at pH 6.5 to basolateral side at pH 7.4 in human Caco2 cells at 10 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Coumarin carboxylic acids as monocarboxylate transporter 1 inhibitors: In vitro and in vivo studies as potential anticancer agents. |
| AID486602 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 25 nM after 24 hrs by flow cytometry | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | Synthesis, molecular modeling and biological evaluation of dithiocarbamates as novel antitubulin agents. |
| AID1473725 | Cytotoxicity against human DU145 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID1693026 | Induction of apoptosis in human K562 cells at 30 nM measured after 48 hrs by Annexin V-FITC/7-AAD staining based flow cytometric analysis | 2021 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 32 | 10-(4-Phenylpiperazine-1-carbonyl)acridin-9(10H)-ones and related compounds: Synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID202313 | In vitro cytotoxicity against SK-MEL-5 cell line. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Antitumor agents. 141. Synthesis and biological evaluation of novel thiocolchicine analogs: N-acyl-, N-aroyl-, and N-(substituted benzyl)deacetylthiocolchicines as potent cytotoxic and antimitotic compounds. |
| AID303712 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G2M phase at 3.16 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID680331 | TP_TRANSPORTER: inhibition of MPP+ uptake in OCT3-expressing HEK293 cells | 1998 | Nature neuroscience, Sep, Volume: 1, Issue:5 | Molecular identification of the corticosterone-sensitive extraneuronal catecholamine transporter. |
| AID1407737 | Induction of apoptosis in human A375 cells assessed as live cells at 100 nM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 92.3%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1389594 | Inhibition of MSU-induced IL-1beta level in serum of acute gouty arthritis Sprague-Dawley rat model at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last dose measured up to 24 hrs by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID1503418 | Gastrointestinal toxicity in human HT-29 cells assessed as increase in mitochondrial number at 5 uM incubated for 3 hrs by flow cytometry | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID624623 | Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID1333465 | Cell cycle arrest in human MCF7 cells assessed as accumulation at sub-G1 phase at 5 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 3.58%) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID333739 | Cytotoxicity against human PC-3MIE8 cells after 48 hrs by MTT assay | 2004 | Journal of natural products, Dec, Volume: 67, Issue:12 | Isomalabaricane-type compounds from the marine sponge Rhabdastrella aff. distincta. |
| AID274832 | Cell cycle arrest in KB/HeLa cells by accumulation at G1 phase at 316 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID537735 | Binding affinity to Candida albicans CaMdr1p expressed in yeast AD1-8u | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 | Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans. |
| AID483368 | Cytotoxicity against human MCF7 cells after 72 hrs by crystal violet staining | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Syntheses and biological evaluation of ring-C modified colchicine analogs. |
| AID733796 | Cytotoxicity against human HCT15 cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID1750239 | Binding affinity to immobilized pig brain tubulin assessed as equilibrium dissociation constant by SPR assay | |||
| AID452614 | Inhibition of tubulin assembly by immunofluorescence assay | 2009 | Bioorganic & 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. |
| AID612339 | Inhibition of bovine brain tubulin polymerization at 20 uM after 15 mins by spectrophotometric analysis | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis and antiproliferative activity of novel 2-aryl-4-benzoyl-imidazole derivatives targeting tubulin polymerization. |
| AID214010 | Inhibition of tubulin polymerization using isolated calf brain at 26 degrees C | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22 | Inhibition of tubulin polymerization by 5,6-dihydroindolo[2,1-alpha]isoquinoline derivatives. |
| AID1562378 | Antiproliferative activity against human A2780 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin. |
| AID1771490 | Inhibition of tubulin polymerization in human MGC-803 cells | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency. |
| AID1142131 | Antiproliferative activity against MBEC after 3 days by coulter counter analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach. |
| AID612315 | Antiproliferative activity against human A375 cells after 48 hrs by sulforhodamine B assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis and antiproliferative activity of novel 2-aryl-4-benzoyl-imidazole derivatives targeting tubulin polymerization. |
| AID213858 | Percentage by which the binding of [3H]colchicine (2.5 uM) to tubulin from calf brain is reduced by 25 uM concentration of compound | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | A novel synthesis of colchicide and analogues from thiocolchicine and congeners: reevaluation of colchicide as a potential antitumor agent. |
| AID214180 | Inhibition of tubulin polymerisation in calf brain | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22 | Inhibition of tubulin polymerization by 5,6-dihydroindolo[2,1-alpha]isoquinoline derivatives. |
| AID220415 | Tested for caspase activation activity in human breast cancer ZR-75-1 cells | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | Discovery of substituted N-phenyl nicotinamides as potent inducers of apoptosis using a cell- and caspase-based high throughput screening assay. |
| AID1763770 | Antiproliferative activity against human KYSE-30 cells incubated for 48 hrs by CCK8 assay | 2021 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 43 | Discovery of indoline derivatives as anticancer agents via inhibition of tubulin polymerization. |
| AID1549908 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain. |
| AID342519 | Cytotoxicity against mouse B16 cells assessed as cell viability after 48 hrs by MTT test | 2008 | Bioorganic & 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. |
| AID377074 | Cytotoxicity against human SF-268 after 3 days by SRB assay | 2005 | Journal of natural products, Feb, Volume: 68, Issue:2 | New colchicinoids from a native Jordanian meadow saffron, colchicum brachyphyllum: isolation of the first naturally occurring dextrorotatory colchicinoid. |
| AID1382491 | Apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM after 60 mins by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA). |
| AID1549910 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain. |
| AID336349 | Antimitotic activity against rat ASK cells assessed as reversal of astrocyte morphology at 20 ug/ml | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID681132 | TP_TRANSPORTER: ATP hydrolysis in MDR1-expressing Sf9 cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID348171 | Inhibition of tubulin without microtubule associated protein polymerization at 5 uM after 60 mins | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Design, synthesis and biological evaluation of novel stilbene-based antitumor agents. |
| AID472410 | Cytotoxicity against human multidrug-resistant KB-C2 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8 | Papyriferic acid derivatives as reversal agents of multidrug resistance in cancer cells. |
| AID605767 | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID1473702 | Cytotoxicity against human RPMI7951 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID1384283 | Induction of morphological changes in human A549 cells assessed as cell rounding after 24 hrs | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID140029 | Acute toxicity after intramuscular injection in mice. | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2 | Antitubulin effects of derivatives of 3-demethylthiocolchicine, methylthio ethers of natural colchicinoids, and thioketones derived from thiocolchicine. Comparison with colchicinoids. |
| AID1189598 | Inhibition of purified tubulin (unknown origin) assessed as critical concentration of tubulin required to produce assembly at 25 uM after 30 mins by spectrophotometry (Rvb = 3.3 +/- 0.1 uM) | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID1221964 | Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1771029 | Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID274824 | Cell cycle arrest in KB/HeLa cells by accumulation at G2/M phase at 316 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID102187 | Inhibition of LOVO cell proliferation | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID342600 | Inhibition of nuclear translocation of thioredoxin-1 from cytosol in human M21 cells at 50 nM after 16 hrs by immunocytofluorescence | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Selective alkylation of beta(II)-tubulin and thioredoxin-1 by structurally related subsets of aryl chloroethylureas leading to either anti-microtubules or redox modulating agents. |
| AID1503414 | Gastrointestinal toxicity in human HT-29 cells assessed as effect on golgi apparatus at 5 uM incubated for 3 hrs by flow cytometry | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID1698823 | Antimitotic activity against sea urchin embryo assessed as cleavage arrest measured 2.5 to 6 hrs post-fertilization by light microscopy analysis | 2020 | Bioorganic & 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. |
| AID303721 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G1 phase at 3.16 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID394851 | Cytotoxicity against human A375 cells after 48 hrs by SRB assay | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships. |
| AID1413539 | Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | Synthesis and biological evaluation of novel 5-chloro- |
| AID274810 | Cell cycle arrest in KB/HeLa cells by accumulation at S phase at 0.3 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID1906182 | Binding affinity to beta-tubulin colchicine binding site in human HeLa cells assessed as decrease of adduct formation by measuring gray value measured at 2 uM incubated for 2 hrs followed by addition of EBI measured after 1.5 hrs by EBI competition based | |||
| AID95876 | Inhibition of KB cell proliferation | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID678775 | TP_TRANSPORTER: increase in brain concentration in mdr1a(-/-) mouse | 2000 | Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, Feb, Volume: 20, Issue:2 | Development of an in situ mouse brain perfusion model and its application to mdr1a P-glycoprotein-deficient mice. |
| AID355581 | Antiproliferative activity against human HT-29 cells at 0.1 ug after 48 hrs by two-layer agar-diffusion method | |||
| AID1058413 | Inhibition of CYP2D6 (unknown origin) at 3 uM | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation. |
| AID1736531 | Induction of apoptosis in human HT-29 cells assessed as early apoptotic cells at 0.5 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.6 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1333451 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1110732 | Inhibition of Nicotiana tabacum (tobacco) root growth assessed as inhibition of root elongation | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Structure-activity relationships of phenylcyclohexene and biphenyl antitubulin compounds against plant and mammalian cells. |
| AID1695274 | Cytotoxicity against human BxPC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
| AID280074 | Antiproliferative activity against drug resistant HCT15 cell line expressing MDR1 by Alamar Blue assay | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5 | Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles. |
| AID1378144 | Growth inhibition of human A172 cells up to 25 uM cotreated with camptothecin measured after 24 hrs by XTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma. |
| AID526947 | Cytotoxicity against mouse B16-F1 cells after 48 hrs by sulforhodamine B assay | 2010 | Journal 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. |
| AID1566328 | Cell cycle arrest in human ALL5 cells assessed as accumulation in S phase at 5 times of antiproliferative IC50 incubated for 72 hrs by propidium iodide based flow cytometry (Rvb = 13.5 %) | |||
| AID169086 | The ability to displace [3H]colchicine binding to rat brain tubulin protein | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Synthesis and binding to tubulin of colchicine spin probes. |
| AID281700 | Induction of apoptosis in human DLD1 cells assessed as caspase activation after 24 hrs | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group. |
| AID553910 | Cell cycle arrest in human SW620 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. |
| AID1500601 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents. |
| AID1549904 | Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain. |
| AID94435 | Inhibition of L1210 cell proliferation | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID1704302 | Cytotoxicity against human HEK293 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1198463 | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase after 24 hrs by flow cytometry (Rvb = 59.75%) | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Synthesis, biological evaluation and 3D-QSAR studies of novel 5-phenyl-1H-pyrazol cinnamamide derivatives as novel antitubulin agents. |
| AID1333456 | Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells at 5 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.3%) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1636356 | Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID151506 | Cytotoxic activity against cellular metabolic activity of Ovary SKOV3 tumor cell line using XTT proliferation assay after incubation with the compound for 48 h | 2003 | Journal 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. |
| AID132743 | Percent increase in life-span against in vivo P388 murine leukemia at a dose 0.12 mg/kg in trail 1 | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID642051 | Inhibition of tubulin polymerization after 15 mins preincubation measured after 20 mins by spectrophotometry | 2011 | Journal 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. |
| AID1771030 | Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID612421 | Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT based ELISA assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis, biological evaluation, and molecular modeling of cinnamic acyl sulfonamide derivatives as novel antitubulin agents. |
| AID1236601 | Binding affinity to tubulin in human HepG2 cells at 5 uM after 4 hrs by EBI competition assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Synthesis and biological evaluation of diarylthiazole derivatives as antimitotic and antivascular agents with potent antitumor activity. |
| AID1566307 | Cell cycle arrest in human ALL5 cells assessed as accumulation in G2 phase at 5 times of antiproliferative IC50 incubated for 72 hrs by propidium iodide based flow cytometry (Rvb = 11.3 %) | |||
| AID1435784 | Cytotoxicity against 3D culture of human Colo-357 cells up to 10000 nM measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID697550 | Antiproliferative activity against human DU145 cells after 48 hrs by SRB assay | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16 | Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents. |
| AID711184 | Binding affinity to pig brain tubulin polymerization measured every 1 mins of 60 mins by fluorescence assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID92127 | in vitro antitumor activity against NCI 's human tumor cell lines | 1997 | Journal 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. |
| AID645070 | Cytotoxicity against human HT-29 cells after 96 hrs using tetracolor one | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Design, Synthesis, and Antitumor Activity of 4-Halocolchicines and Their Pro-drugs Activated by Cathepsin B. |
| AID1535578 | Cytotoxicity against HEK293T cells after 24 hrs by MTT assay | 2019 | Bioorganic & 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. |
| AID1389573 | Antiarthritic activity in MSU-induced acute gouty arthritis Sprague-Dawley rat model assessed as reduction in ankle swelling by measuring perimeter of ankle at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last do | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID1872845 | Cytotoxicity against human MCF7 cells treated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Tandem construction of biological relevant aliphatic 5-membered N-heterocycles. |
| AID1582219 | Antiproliferative activity against human DU145 cells measured after 72 hrs by MTS assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties. |
| AID1646367 | Inhibition of tubulin polymerization (unknown origin) at 10 uM relative to control | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 | Design, synthesis and biological evaluation of novel indole-based oxalamide and aminoacetamide derivatives as tubulin polymerization inhibitors. |
| AID1550794 | Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 2 uM measured after 24 hrs by DAPI staining based HCS analysis | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop. |
| AID1754377 | Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay | 2021 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 45 | WITHDRAWN: Discovery of indoline derivatives as anticancer agents via inhibition of tubulin polymerization. |
| AID1736482 | Cell cycle arrest in human HT29 cells assessed as cell accumulation at G2 phase at 0.5 uM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 10.37 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1638301 | Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Molecular diversity of trimethoxyphenyl-1,2,3-triazole hybrids as novel colchicine site tubulin polymerization inhibitors. |
| AID274823 | Cell cycle arrest in KB/HeLa cells by accumulation at G2/M phase at 100 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1233601 | Induction of cell cycle arrest in human M21 cells assessed as cells accumulation at S phase at 24 nM after 24 hrs by flow cytometry (Rvb = 22.2%) | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model. |
| AID1402709 | Antiproliferative activity against human 293T cells after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design and characterization of α-lipoic acyl shikonin ester twin drugs as tubulin and PDK1 dual inhibitors. |
| AID612316 | Antiproliferative activity against human WM164 cells after 48 hrs by sulforhodamine B assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis and antiproliferative activity of novel 2-aryl-4-benzoyl-imidazole derivatives targeting tubulin polymerization. |
| AID526945 | Cytotoxicity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay | 2010 | Journal 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. |
| AID1809654 | Antiproliferative activity against human LoVo cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Synthesis of thiocolchicine amine derivatives and evaluation of their antiproliferative activity. |
| AID327206 | Inhibition of tubulin polymerization in presence of microtubule-associated proteins | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8 | Synthesis and structure-activity relationship studies on tryprostatin A, an inhibitor of breast cancer resistance protein. |
| AID1385698 | Cytotoxicity against human 786-O cells after 72 hrs by MTT assay | 2018 | Journal of natural products, 08-24, Volume: 81, Issue:8 | Structurally Diverse Highly Oxygenated Triterpenoids from the Roots of Ailanthus altissima and Their Cytotoxicity. |
| AID605769 | Antiproliferative activity against human CEM cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID29925 | Volume of distribution in man (IV dose) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID1428409 | Cytotoxicity against vinblastine-sensitive human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay | |||
| AID1426446 | Inhibition of porcine tubulin polymerization after 45 mins by turbidometric method | 2017 | Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2 | N-Heterocyclic (4-Phenylpiperazin-1-yl)methanones Derived from Phenoxazine and Phenothiazine as Highly Potent Inhibitors of Tubulin Polymerization. |
| AID1500656 | Cell cycle arrest in human AGS cells assessed as accumulation at S phase at 50 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 37.94%) | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of 9H-purins as potential tubulin polymerization inhibitors: Synthesis, biological evaluation and structure-activity relationships. |
| AID1384284 | Cell cycle arrest in human A549 cells assessed as accumulation at sub-G0 phase at 50 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 2 +/- 1%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID312971 | Induction of apoptosis in human T47D cells assessed as caspase activation after 24 hrs by HTS assay | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions. |
| AID1740986 | Inhibition of pig brain tubulin polymerization in presence of GTP by spectrophotometric method | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Discovery of tertiary amide derivatives incorporating benzothiazole moiety as anti-gastric cancer agents in vitro via inhibiting tubulin polymerization and activating the Hippo signaling pathway. |
| AID668215 | Antiproliferative activity against human A375 cells after 48 hrs by SRB assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | New substituted 4H-chromenes as anticancer agents. |
| AID730216 | Cytotoxicity against human HepG2 cells after 72 hrs by CCK-8 assay | 2013 | Journal 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. |
| AID317731 | Antiviral activity against HIV2ROD infected in human MT4 cells | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
| AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
| AID1625808 | Binding affinity to microtubule in human HepG2 cells assessed as inhibition of spindle formation after 24 hrs by immunofluorescence staining-based confocal microscopy | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1692983 | Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 32 | 10-(4-Phenylpiperazine-1-carbonyl)acridin-9(10H)-ones and related compounds: Synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID225200 | Percent inhibition of [3H]-colchicine binding to tubulin with molar ratio of 1:1 (inhibitor: [3H]-colchicine) | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | Synthesis and tubulin binding of novel C-10 analogues of colchicine. |
| AID271657 | Cytotoxicity against KB-VIN 10 cell line by methylene blue dye assay | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents. |
| AID383970 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of 2N cells at 2 uM after 24 hrs by flow cytometry | 2008 | Journal 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. |
| AID461787 | Inhibition of tubulin polymerization by turbidimetric assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | 5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. |
| AID1646370 | Antiproliferative activity against human HeLa cells assessed as reduction in cell growth after 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 | Design, synthesis and biological evaluation of novel indole-based oxalamide and aminoacetamide derivatives as tubulin polymerization inhibitors. |
| AID214373 | In vitro inhibitory concentration required to displace [3H]colchicine from its binding site on tubulin | 2003 | Journal 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. |
| AID735507 | Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells in G0/G1 phase at 2uM concentration after 24 hrs by propidium iodide staining based cytofluorimetric analysis (Rvb = 39.55%) | 2013 | European 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. |
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| AID1414043 | Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID384000 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at sub-G1 phase at 2 uM after 72 hrs by flow cytometry | 2008 | Journal 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. |
| AID1674014 | Cytotoxicity against human HeLa cells after 24 to 72 hrs by Cell Titer Blue assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1677848 | Inhibition of tubulin polymerization (unknown origin) relative to control | 2020 | Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21 | New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation. |
| AID1736530 | Induction of apoptosis in human HT-29 cells assessed as viable cells at 0.5 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 98.3 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1399018 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18 | Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors. |
| AID1535579 | Cytotoxicity against mouse primary hepatocytes after 24 hrs by MTT assay | 2019 | Bioorganic & 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. |
| AID1459300 | Induction of reactive oxygen species generation in human MCF7 cells assessed as decrease in cell viability at 1 to 10 uM in presence of N-acetyl cysteine after 48 hrs by alamarBlue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
| AID612422 | Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetric analysis | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis, biological evaluation, and molecular modeling of cinnamic acyl sulfonamide derivatives as novel antitubulin agents. |
| AID605958 | Cell cycle arrest in human K562 cells assessed as accumulation at G2/M phase at 0.003 to. 1 ug/ml after 24 hrs by flow cytometric analysis | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1236573 | Cytotoxicity against human NCI/ADR cells | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | Progress Toward the Development of Noscapine and Derivatives as Anticancer Agents. |
| AID1785505 | Antiproliferative activity against human 786-O cells incubated for 72 hrs by MTT assay | |||
| AID340147 | Growth inhibition of human H460 cells after 72 hrs by methylene blue dye assay | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors. |
| AID302077 | Inhibition of temperature-induced tubulin polymerization of calf brain at 40 uM | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | [(2-Phenylindol-3-yl)methylene]propanedinitriles inhibit the growth of breast cancer cells by cell cycle arrest in G(2)/M phase and apoptosis. |
| AID1384275 | Antiproliferative activity against human MCF7 cells after 2 days by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID1566300 | Selectivity index, ratio of IC50 of mouse BALB/3T3 cells to IC50 of human A549 cells | |||
| AID342591 | Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B method | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Selective alkylation of beta(II)-tubulin and thioredoxin-1 by structurally related subsets of aryl chloroethylureas leading to either anti-microtubules or redox modulating agents. |
| AID486603 | Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 25 nM after 24 hrs by flow cytometry | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12 | Synthesis, molecular modeling and biological evaluation of dithiocarbamates as novel antitubulin agents. |
| AID1562387 | Antiproliferative activity against human A549 cells harboring control siRNA after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin. |
| AID1435777 | Cytotoxicity against 2D culture of human PANC1 cells measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1628411 | Displacement of [3H]colchicine from biotinylated porcine tubulin at 5 uM incubated for 2 hrs by competition scintillation proximity | 2016 | Journal 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. |
| AID366389 | Inhibition of tubulin polymerization | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a potent inducer of apoptosis with high in vivo activity. |
| AID618908 | Anticancer activity against human OVCAR8 cells after 96 hrs by SRB assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Design, synthesis, and SAR studies of 4-substituted methoxylbenzoyl-aryl-thiazoles analogues as potent and orally bioavailable anticancer agents. |
| AID342590 | Antiproliferative activity against human M21 cells after 48 hrs by sulforhodamine B method | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Selective alkylation of beta(II)-tubulin and thioredoxin-1 by structurally related subsets of aryl chloroethylureas leading to either anti-microtubules or redox modulating agents. |
| AID1237726 | Cytotoxicity against human MESSA/DX5 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2015 | Journal 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. |
| AID1203383 | Antiproliferative activity in sea urchin embryo assessed as antimitotic activity by measuring cleavage alteration exposed for 8 to 20 mins after fertilization and 45 to 55 mins before first mitotic cycle completion measured 2.5 to 5.5 hrs after fertilizat | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines. |
| AID627405 | Antiproliferative activity against paclitaxel-resistant CHO-TAX 5-6 cells after 48 hrs by SRB assay | 2011 | European 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. |
| AID1221957 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID681120 | TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID26380 | Dissociation constant (pKa) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
| AID1501687 | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel chemotypes targeting tubulin at the colchicine binding site and unbiasing P-glycoprotein. |
| AID342501 | Cell cycle arrest in human MCF7 cells assessed as MG0/G1 phase accumulation at 2 times GI50 after 24 hrs by flow cytometry | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Aromatic 2-chloroethyl urea derivatives and bioisosteres. Part 2: Cytocidal activity and effects on the nuclear translocation of thioredoxin-1, and the cell cycle progression. |
| AID1272837 | Growth inhibition of human KB cells after 72 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | New MKLP-2 inhibitors in the paprotrain series: Design, synthesis and biological evaluations. |
| AID256879 | Inhibition of tubulin polymerization in bovine brain at 10 uM | 2005 | Bioorganic & 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. |
| AID595054 | Inhibition of bovine brain tubulin polymerization after 20 mins by turbidimetry | 2011 | Bioorganic & 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. |
| AID733788 | Cytotoxicity against human SKHEP1 cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID1566306 | Cell cycle arrest in human ALL5 cells assessed as accumulation in G2 phase at 5 times of antiproliferative IC50 incubated for 48 hrs by propidium iodide based flow cytometry (Rvb = 11.2 %) | |||
| AID1882727 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 24 hrs in presence of foetal bovine serum by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Recent advances of antitumor shikonin/alkannin derivatives: A comprehensive overview focusing on structural classification, synthetic approaches, and mechanisms of action. |
| AID1519871 | Inhibition of tubulin polymerization (unknown origin) incubated for 15 mins followed by GTP addition and measured for 20 mins by spectrophotometry | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structure-activity relationship studies and in vitro and in vivo anticancer activity of novel 3-aroyl-1,4-diarylpyrroles against solid tumors and hematological malignancies. |
| AID744709 | Antimitotic activity in human HeLa cells assessed as tubulin intensity after 24 hrs by Hoechst 33342 staining | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID1771035 | Antiproliferative activity against human MDA-MB-231/TxR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID1672883 | Antiproliferative activity against D4-9-31 resistance human A2780 cells incubated for 72 hrs by ATPlite reagent based assay | 2019 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13 | Resistance mechanisms and cross-resistance for a pyridine-pyrimidine amide inhibitor of microtubule polymerization. |
| AID494520 | Cell growth inhibition of human K562 cells after 48 hrs | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis, antiproliferative activity and inhibition of tubulin polymerization by anthracenone-based oxime derivatives. |
| AID342502 | Cell cycle arrest in human MCF7 cells assessed as S phase accumulation at 2 times GI50 after 24 hrs by flow cytometry | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Aromatic 2-chloroethyl urea derivatives and bioisosteres. Part 2: Cytocidal activity and effects on the nuclear translocation of thioredoxin-1, and the cell cycle progression. |
| AID1566308 | Cell cycle arrest in human ALL5 cells assessed as accumulation in G1 phase at 5 times of antiproliferative IC50 incubated for 24 hrs by propidium iodide based flow cytometry (Rvb = 68.1 %) | |||
| AID1201720 | Inhibition of recombinant human HDAC2 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID9014 | Cytotoxicity against human lung carcinoma cells (A-549) using SRB assay. | 1998 | Journal 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. |
| AID1287982 | Inhibition of porcine tubulin polymerization by UV-Vis microplate reader analysis | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Discovery of novel 2-phenyl-imidazo[1,2-a]pyridine analogues targeting tubulin polymerization as antiproliferative agents. |
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| AID54923 | Inhibition of human cytochrome P450 3A4 | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID627398 | Antiproliferative activity against human P388D1 after 48 hrs by SRB assay | 2011 | European 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. |
| AID1384279 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for human MCF7 cells | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID526946 | Cytotoxicity against human A375 cells after 48 hrs by sulforhodamine B assay | 2010 | Journal 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. |
| AID514408 | Cytotoxicity against human A549 cells after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
| AID1860525 | Antiproliferative activity against human CAL-27 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC. |
| AID1203387 | Cytotoxicity against human NCI60 cells | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines. |
| AID297424 | Growth inhibition of human MKN45 cells after 72 hrs by methylene blue dye assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | 4- and 5-aroylindoles as novel classes of potent antitubulin agents. |
| AID150344 | Cytotoxic activity against P388 mouse lymphocytic leukemia cell line (doxorubicin resistant). | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Fluorinated colchicinoids: antitubulin and cytotoxic properties. |
| AID494503 | Antiproliferative activity against human KB/HeLa cells after 48 hrs by XTT assay | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis, antiproliferative activity and inhibition of tubulin polymerization by 1,5- and 1,8-disubstituted 10H-anthracen-9-ones bearing a 10-benzylidene or 10-(2-oxo-2-phenylethylidene) moiety. |
| AID1736457 | Inhibition of tubulin polymerization (unknown origin) measured every 2 mins for 60 mins by spectrophotometric method | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID494505 | Antiproliferative activity against human SF268 cells after 48 hrs by XTT assay | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis, antiproliferative activity and inhibition of tubulin polymerization by 1,5- and 1,8-disubstituted 10H-anthracen-9-ones bearing a 10-benzylidene or 10-(2-oxo-2-phenylethylidene) moiety. |
| AID340149 | Growth inhibition of P-gp 170/MDR overexpressing human KB-vin10 cells after 72 hrs by methylene blue dye assay | 2008 | Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14 | Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors. |
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| AID1628399 | Growth inhibition of human HeLa cells incubated for 72 hrs by MTT assay | 2016 | Journal 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. |
| AID397292 | Cytotoxicity against human MDA-MB-231 cells after 72 hrs | 2009 | Journal 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. |
| AID1367982 | Inhibition of pig brain tubulin polymerization measured every 1 min for 20 mins by spectrophotometric analysis | |||
| AID335776 | Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 0.032 ug/mL | 1993 | Journal of natural products, Oct, Volume: 56, Issue:10 | Cytotoxic constituents from Hyptis verticillata. |
| AID1875315 | Cytotoxicity in human HeLa cells assessed as growth inhibition level after 48 hrs by SRB assay | 2022 | Journal of natural products, 10-28, Volume: 85, Issue:10 | Resin Glycosides from |
| AID780983 | Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Furanylazaindoles: potent anticancer agents in vitro and in vivo. |
| AID1628415 | Induction of cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 40 nM incubated for 24 hrs by propidium iodide staining based FACS flow cytometry | 2016 | Journal 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. |
| AID1704314 | Inhibition of tubulin assembly in human COLO357 cells assessed as induction of tubulin dissipation at 5 nM incubated for 24 hrs by Hoechst 33342 staining based confocal microscopic analysis | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID228464 | Inhibition of tubulin polymerization, induced by 10 mM taxol at a concentration of 5 uM. | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Fluorinated colchicinoids: antitubulin and cytotoxic properties. |
| AID665239 | Induction of mitotic arrest in human HeLa cells assessed as nuclear condensation by Hoechst 33342 staining | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | N⁴-Phenyl-substituted 2-acetylpyridine thiosemicarbazones: cytotoxicity against human tumor cells, structure-activity relationship studies and investigation on the mechanism of action. |
| AID1638299 | Antiproliferative activity against human PC3 cells measured after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Molecular diversity of trimethoxyphenyl-1,2,3-triazole hybrids as novel colchicine site tubulin polymerization inhibitors. |
| AID1668779 | Effect on alpha-tublin parameters in Parkinson's disease patient derived human ONS cells at 10 uM after 24 hrs by anti-alphatubulin staining based fluorescence assay | 2020 | Journal of natural products, 05-22, Volume: 83, Issue:5 | A Grand Challenge. 3. Unbiased Phenotypic Function of Metabolites from Australia Plants |
| AID28233 | Fraction ionized (pH 7.4) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
| AID719103 | Resistance factor, ratio of IC50 for multidrug-resistant human A2780AD cells overexpressing p-gp to IC50 for human A2780 cells | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation. |
| AID735022 | Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells in G2/M phase at 4 uM concentration after 24 hrs by propidium iodide staining based cytofluorimetric analysis (Rvb = 12.95%) | 2013 | European 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. |
| AID1142141 | Competitive binding affinity to beta-tubulin in human MDA-MB-231 cells assessed as inhibition of protein-N/N'-ethylene-bis(iodoacetamide) adduct formation at 0.5 uM preincubated for 16 hrs followed by N/N'-ethylene-bis(iodoacetamide) formation measured af | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach. |
| AID711175 | Cytotoxicity against human SW780 cells after 96 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID200619 | Inhibition of SCL-1 cell proliferation (Not tested) | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID1221970 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1384277 | Antiproliferative activity against HEK293 cells after 2 days by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID514409 | Cytotoxicity against human DU145 cells after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
| AID611268 | Cytotoxicity against non induced human RKOp27 cells after 48 hrs by XTT assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Phenylimino-10H-anthracen-9-ones as novel antimicrotubule agents-synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID695932 | Cytotoxicity against human SGC7901 cells after 48 hrs | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis and biological evaluation of a series of podophyllotoxins derivatives as a class of potent antitubulin agents. |
| AID152356 | Inhibition of P388 cell proliferation | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID1407728 | Induction of apoptosis in human A375 cells assessed as necrotic cells at 100 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.13%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1186700 | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17 | New benzimidazole-2-urea derivates as tubulin inhibitors. |
| AID1898099 | Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID1518073 | Inhibition of pig brain tubulin polymerization in presence of GTP by spectrophotometric analysis | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents. |
| AID299427 | Cell cycle arrest in Jurkat cells assessed as accumulation at G0/G1 phase at 25 uM after 15 hrs relative to control | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Antiproliferative and apoptosis inducing properties of pyrano[3,2-c]pyridones accessible by a one-step multicomponent synthesis. |
| AID427913 | Growth inhibition of human T47D cells after 48 hrs | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents. |
| AID228458 | Inhibition of tubulin polymerization activity using homogenous bovine brain tubulin at 30 degree C | 1999 | Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3 | The synthesis and evaluation of temperature sensitive tubulin toxins. |
| AID657608 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2012 | Bioorganic & 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. |
| AID1750238 | Inhibition of pig brain tubulin polymerization by spectrophotometric method | |||
| AID1628421 | Induction of apoptosis in human A549 cells assessed as induction of chromatin condensation at 40 nM incubated for 24 hrs microscopy | 2016 | Journal 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. |
| AID1378141 | Growth inhibition of human PC3 cells up to 25 uM cotreated with camptothecin measured after 24 hrs by XTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma. |
| AID1406436 | Inhibition of tubulin polymerization in human HepG2 cells assessed as abnormal microtubule network formation at 0.04 uM after 12 hrs by DAPI staining based immunofluorescence confocal laser scanning microscopic analysis | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation. |
| AID44202 | Effect on cross resistance of CCRF-CEM cells resistant to vincristine. | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Structure-activity relationships of antineoplastic agents in multidrug resistance. |
| AID1189152 | Drug resistance index, ratio of IC50 for taxol-resistant human A2780 cells to IC50 for human A2780 cells | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID428055 | Immunosuppressive activity in concanavalin A-activated T cell assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Design, synthesis and identification of novel colchicine-derived immunosuppressant. |
| AID538692 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23 | Synthesis, molecular modeling and biological evaluation of guanidine derivatives as novel antitubulin agents. |
| AID1384316 | Downregulation of hTERT gene expression in human HT-29 cells assessed as hTERT mRNA level at 10 nM after 48 hrs by RT-PCR method (Rvb = 100%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID136915 | In vivo antitumor activity against P388 mouse leukemia expressed as T/C (median survival time of treated animals / median survival time of untreated controls x 100) at a dose of 0.5 mg/kg | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | A novel synthesis of colchicide and analogues from thiocolchicine and congeners: reevaluation of colchicide as a potential antitumor agent. |
| AID1674004 | Cytotoxicity against human A549 cells incubated for 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1435801 | Induction of cell membrane permeability in 3D culture of human MIAPaCa2 cells at 1 uM measured after 48 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1221982 | Fraction absorbed in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID780982 | Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Furanylazaindoles: potent anticancer agents in vitro and in vivo. |
| AID1673972 | Antiproliferative activity against human KB-8511 cells incubated for 96 hrs by spectrophotometric method | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID303691 | Cytotoxicity against human RKO cells after 48 hrs by XTT assay | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1704300 | Antiproliferative activity against human COLO357 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID274830 | Cell cycle arrest in KB/HeLa cells by accumulation at G1 phase at 31.6 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID348001 | Cell cycle arrest in human KB/HeLa cells assessed as G1 phase accumulation at 31.6 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1233617 | Growth inhibition of human A549 cells assessed as inhibition of cell proliferation after 24 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Jun-24, Volume: 99 | Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin polymerization inhibitors. |
| AID1541705 | Inhibition of anchorage-independent colony formation in human MDA-MB-468 cells at 5 uM measured upto 21 days by soft agar colony formation assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis, and validation of novel nitrogen-based chalcone analogs against triple negative breast cancer. |
| AID1811842 | Induction of mitotic block in human SK-OV-3 cells at 10 to 30 nM in absence of colchicine measured immediately by flow cytometry analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Design, Synthesis, and Bioactivity Evaluation of Dual-Target Inhibitors of Tubulin and Src Kinase Guided by Crystal Structure. |
| AID553917 | Displacement of [3H]colchicine from tubulin at 30 uM | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. |
| AID337653 | Cytotoxicity against human ZR-75-1 cells after 3 days by SRB assay | 1994 | Journal of natural products, Oct, Volume: 57, Issue:10 | Cytotoxic diterpenoids from Isodon megathyrsus. |
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| AID317733 | Cytotoxicity against mock-infected human MT4 cells by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
| AID1142150 | Antiinvasive activity against human MDA-MB-231 cells at 0.08 uM after 17 hrs by Transwell assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach. |
| AID1261385 | Cell cycle arrest in human 786-0 cells assessed as reduction in G1 phase at 1.25 nM after 24 hrs by propidium iodide based flow cytometric analysis (Rvb = 46.7 +/- 0.8%) | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Synthesis of thiophene-thiosemicarbazone derivatives and evaluation of their in vitro and in vivo antitumor activities. |
| AID1333462 | Effect on p53 gene expression in human MDA-MB-231 cells assessed as ratio of p53 to beta-actin expression level at 5 uM after 24 hrs by RT-PCR method (Rvb = 0.22 No_unit) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1888929 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Synthesis and biological evaluation of 3β-O-neoglycosides of caudatin and its analogues as potential anticancer agents. |
| AID1883539 | Disruption of microtubule network in human MGC-803 cells assessed as incomplete mitosis at 25 nM measured after 48 hrs by DAPI staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID98163 | Concentration that inhibits proliferation of cultured lymphoid leukemia L1210 cells to 50% control growth during 48 h | 1992 | Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26 | Antimitotic agents: ring analogues and derivatives of ethyl [(S)-5-amino-1,2-dihydro-2-methyl-3-phenylpyrido[3,4-b]pyrazin-7- yl]carbamate. |
| AID1639384 | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4 | Parvifoline Derivatives as Tubulin Polymerization Inhibitors. |
| AID1703285 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK-8 assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities. |
| AID296580 | Effect on rate of thrombin-induced human platelet aggregation at 0.1 uM | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16 | Characterization of the intracellular mechanisms involved in the antiaggregant properties of cinnamtannin B-1 from bay wood in human platelets. |
| AID1717032 | Inhibition of porcine tubulin polymerization at 16 uM preincubated for 10 mins followed by GTP addition by turbidimetric method | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Isoquinoline-based biaryls as a robust scaffold for microtubule inhibitors. |
| AID1431296 | Cytotoxicity against HEK293 cells assessed as growth inhibition after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID1110729 | Inhibition of Bos taurus (bovine) brain tubulin polymerization at 2 uM | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Structure-activity relationships of phenylcyclohexene and biphenyl antitubulin compounds against plant and mammalian cells. |
| AID78790 | In vitro cytotoxicity against HCT-15 cell line. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Antitumor agents. 141. Synthesis and biological evaluation of novel thiocolchicine analogs: N-acyl-, N-aroyl-, and N-(substituted benzyl)deacetylthiocolchicines as potent cytotoxic and antimitotic compounds. |
| AID1233609 | Induction of microtubule depolymerization and cytoskeleton disruption in human M21 cells at 24 nM after 24 hrs by immunofluorescence assay | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model. |
| AID393415 | Cell cycle arrest in human K562 cells assessed as accumulation in Sub-G1 phase at 10 uM after 24 hrs by flow cytometry analysis | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis and biological evaluation of novel symmetry bis-enediynes. |
| AID749385 | Cytotoxicity against human A431 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | The discovery of colchicine-SAHA hybrids as a new class of antitumor agents. |
| AID214714 | Inhibitory activity against tubulin polymerization at 0.25 mM concentration | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | Stabilization of microtubules by Combretastatin D derivatives. |
| AID711170 | Induction of ABCG2 mRNA expression in human DLD1 cells at 1/10 IC50 to IC50 after 96 hrs by RT-PCR analysis | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID134556 | Compound was tested for toxicity in non tumored mice | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID1582217 | Antiproliferative activity against human PC3/TxR cells measured after 72 hrs by MTS assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties. |
| AID1333468 | Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 9.29%) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1406860 | Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay | |||
| AID678714 | Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1625738 | Resistance index, ratio of IC50 for vinblastine resistant/P-gp overexpressing human HCT8 cells to IC50 for human HCT8 cells | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1414053 | Antifungal activity against Trichoderma viride Pers after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1750228 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | |||
| AID333842 | Cytotoxicity against human KB cells | |||
| AID357846 | Binding affinity to yeast tRNA assessed as reduction in tRNA peak by pre-incubation method | |||
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID130471 | Carrageenan-induced edema was determined value for intraperitoneal administration | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Synthesis and antiinflammatory activity of hexahydrothiopyrano[4,3-c]pyrazoles and related analogues. |
| AID409673 | Cytotoxicity against human HepG2 cells after 48 hrs by luminescence cell viability assay | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 | Synthesis and characterization of BODIPY-labeled colchicine. |
| AID1239260 | Displacement of [3H]-colchicine from tubulin (unknown origin) preincubated with protein for 1 hr followed by [3H]-colchicine addition measured after 3 hrs by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling. |
| AID1453486 | Induction of microtubule disruption in human HeLa cells assessed as dense microtubule at 1 uM after 6 hrs by DAPI staining based immunofluorescence microscopic analysis | 2017 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 27, Issue:13 | One-pot synthesis and biological evaluation of N-(aminosulfonyl)-4-podophyllotoxin carbamates as potential anticancer agents. |
| AID1403595 | Inhibition of pig brain tubulin polymerization measured every 1 min for 20 mins by spectrophotometric method | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design, synthesis, biological evaluation and cocrystal structures with tubulin of chiral β-lactam bridged combretastatin A-4 analogues as potent antitumor agents. |
| AID472409 | Cytotoxicity against human KB cells after 48 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8 | Papyriferic acid derivatives as reversal agents of multidrug resistance in cancer cells. |
| AID1526482 | Competitive inhibition of porcine tubulin alpha/beta at 10 to 100 uM preincubated 30 mins followed by addition of N-(2-(3-(But-3-yn-1-yl)-3H-diazirin-3-yl)ethyl)-5-(2-(phenoxymethyl)-3H-imidazo[4,5-b]pyridin-6-yl)thiophene-3-carboxamide and measured after | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Identification of 2,6-Disubstituted 3 |
| AID1541706 | Inhibition of anchorage-independent colony formation in human MCF7 cells at 5 uM measured upto 21 days by soft agar colony formation assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis, and validation of novel nitrogen-based chalcone analogs against triple negative breast cancer. |
| AID596136 | Inhibition of pig brain tubulin polymerization by spectrophotometry | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9 | Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors. |
| AID157344 | Inhibitory activity against Taxol resistant PTX22 cell lines | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | Stabilization of microtubules by Combretastatin D derivatives. |
| AID296594 | Effect on thrombin-induced microtubular reorganization at 10 uM after 30 mins | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16 | Characterization of the intracellular mechanisms involved in the antiaggregant properties of cinnamtannin B-1 from bay wood in human platelets. |
| AID1413540 | Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | Synthesis and biological evaluation of novel 5-chloro- |
| AID1414064 | Fungicidal activity against Chaetomium globosum BAM12 ATCC 6205 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1771028 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID355585 | Antiproliferative activity against mouse P388 cells at 0.1 ug after 48 hrs by two-layer agar-diffusion method | |||
| AID1189589 | Selectivity ratio of IC50 for human HEK293 cells to IC50 for human HT29 cells | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID221845 | Cytotoxic activity against mouse macrophage cell line J7.COL-100. | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Fluorinated colchicinoids: antitubulin and cytotoxic properties. |
| AID658916 | Binding affinity to bovine tubulin after 1 hr by spectrofluorometric analysis | 2012 | Journal 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. |
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| AID514410 | Cytotoxicity against human SKBR3 cells after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
| AID1535572 | Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay | 2019 | Bioorganic & 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. |
| AID1205821 | Induction of microtubule destabilization in human A549 cells at 45 nM by DAPI-staining-based fluorescence microscopic analysis | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3 | Synthesis and Structure-Activity Relationship Study of 1-Phenyl-1-(quinazolin-4-yl)ethanols as Anticancer Agents. |
| AID214891 | beta-Tubulin GTPase activity at 10 uM concentration. | 2001 | Journal of medicinal chemistry, Dec-20, Volume: 44, Issue:26 | Synthetic 2-aroylindole derivatives as a new class of potent tubulin-inhibitory, antimitotic agents. |
| AID1389610 | Inhibition of MSU-induced phosphorylated IkappaB protein level in synovial homogenate of acute gouty arthritis Sprague-Dawley rat model at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last dose measured up to 24 | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID228457 | Inhibition of tubulin polymerization | 1993 | Journal 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. |
| AID274818 | Cell cycle arrest in KB/HeLa cells by accumulation at G2/M phase at 0.3 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1378145 | Growth inhibition of human NCI-H1299 cells up to 25 uM cotreated with camptothecin measured after 24 hrs by XTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma. |
| AID333740 | Cytotoxicity against human BGC823 cells after 48 hrs by MTT assay | 2004 | Journal of natural products, Dec, Volume: 67, Issue:12 | Isomalabaricane-type compounds from the marine sponge Rhabdastrella aff. distincta. |
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| AID336346 | Antimitotic activity against rat ASK cells assessed as reversal of astrocyte morphology at 0.16 ug/ml | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID1695275 | Cytotoxicity against human HaCaT cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
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| AID1201732 | Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID1406437 | Inhibition of tubulin polymerization in human HeLa cells assessed as abnormal microtubule network formation at 0.04 uM after 12 hrs by DAPI staining based immunofluorescence confocal laser scanning microscopic analysis | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation. |
| AID605845 | Antiproliferative activity against human SKOV3 cells after 48 hrs by alamar blue assay | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12 | N-benzoylated phenoxazines and phenothiazines: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1776204 | Inhibition of tubulin polymerization in asexual blood stage Plasmodium falciparum NF54 | |||
| AID597798 | Cytotoxicity against human LoVo cells after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Imidazolone-amide bridges and their effects on tubulin polymerization in cis-locked vinylogous combretastatin-A4 analogues: synthesis and biological evaluation. |
| AID1877706 | Cell cycle arrest in human A549 cells assessed as accumulation at G2 phase at 4 uM measured after 36 hrs by flow cytometry (Rvb = 10.02%) | 2022 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 57 | Shikonin N-benzyl matrinic acid ester derivatives as novel telomerase inhibitors with potent activity against lung cancer cell lines. |
| AID1058420 | Cytotoxicity against HUVEC assessed as cell viability after 4 days by MTS assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation. |
| AID143209 | Compound was evaluated for growth inhibition against NCI-H520 cells using cellular assay | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9 | The synthesis and evaluation of benzannelated-azatoxins: the benzazatoxins. |
| AID167041 | Cytotoxicity against human melanoma RPMI-7951 cell line | 1993 | Journal 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 |
| AID274798 | Cell cycle arrest in KB/HeLa cells by accumulation at G2/M phase | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID336336 | Cytotoxicity against human LNCAP cells | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID1704306 | Antiproliferative activity against human PANC-1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID102444 | Compound was evaluated for growth inhibition against MCF-7 cells using cellular assay | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9 | The synthesis and evaluation of benzannelated-azatoxins: the benzazatoxins. |
| AID1189142 | Antiproliferative activity against human CNE2 cells after 48 hrs by SRB method | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1809653 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Synthesis of thiocolchicine amine derivatives and evaluation of their antiproliferative activity. |
| AID1333471 | Effect on cyclin E mRNA expression in human MDA-MB-231 cells assessed as ratio of cyclin E to GAPDH expression level at 5 uM after 24 hrs by RT-PCR method (Rvb = 0.13 No_unit) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID711179 | Cell cycle arrest in human HT-29 cells assessed as accumulation at G2/M phase at 40 nM after 24 hrs by FACS analysis | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID116722 | Acute toxicity as LD50 value was determined in mice administered intraperitoneally | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Synthesis and antiinflammatory activity of hexahydrothiopyrano[4,3-c]pyrazoles and related analogues. |
| AID1549909 | Antiproliferative activity against human MRC5 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain. |
| AID274828 | Cell cycle arrest in KB/HeLa cells by accumulation at G1 phase at 3.16 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1673968 | Antiproliferative activity against human LoVo cells incubated for 72 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1503401 | Cytotoxic activity in human Colo-357 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID42572 | Cytotoxicity against human renal cancer cells (CAKI-1) using SRB assay. | 1998 | Journal 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. |
| AID461784 | Antiproliferative activity against human HT-29 cells after 72 hrs by methylene blue dye assay | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | 5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors. |
| AID103890 | Anti tumor activity on human breast cancer cell line MDR-positive MCF-7 ADRr after 72 hours of treatment | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | N-deacetyl-N-aminoacylthiocolchicine derivatives: synthesis and biological evaluation on MDR-positive and MDR-negative human cancer cell lines. |
| AID214039 | Inhibition of bovine brain tubulin polymerization (ITP). | 1998 | Journal 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. |
| AID116723 | Acute toxicity as LD50 value was determined in mice administered orally | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Synthesis and antiinflammatory activity of hexahydrothiopyrano[4,3-c]pyrazoles and related analogues. |
| AID681122 | TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID1420820 | Antiproliferative activity against human HCT8/T cells after 72 hrs by MTT assay | |||
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| AID1562395 | Inhibition of pig brain tubulin polymerization measured every 1 min for 25 mins by spectrophotometric method | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin. |
| AID1191360 | Inhibition of bovine brain tubulin polymerization measured for 1 hr by fluorescence assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and structure-activity relationships of pyridinyl-1H-1,2,3-triazolyldihydroisoxazoles as potent inhibitors of tubulin polymerization. |
| AID1413541 | Cytotoxicity against hTERT-RPE1 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay | 2018 | MedChemComm, Sep-01, Volume: 9, Issue:9 | Synthesis and biological evaluation of novel 5-chloro- |
| AID673731 | Inhibition of microtubule polymerization in human HT1080 cells at 50 nM for 4 hrs by immunocytochemistry analysis | 2012 | ACS medicinal chemistry letters, Jan-12, Volume: 3, Issue:1 | Identification of Simple Compounds with Microtubule-Binding Activity That Inhibit Cancer Cell Growth with High Potency. |
| AID1473722 | Cytotoxicity against human PC3 cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID1566318 | Cell cycle arrest in human MCF7 cells assessed as accumulation in G1 phase at 5 times of antiproliferative IC50 incubated for 48 hrs by propidium iodide based flow cytometry (Rvb = 40.8 %) | |||
| AID1785484 | Inhibition of EBI binding to beta tubulin in human A2780S cells at 5 uM preincubated for 2 hrs followed by addition of EBI and measured after 2 hrs by western blot assay | |||
| AID1809276 | Induction of microtubule damage in human MCF7 cells incubated for 48 hrs by DAPI staining based immunofluorescence assay | |||
| AID1075752 | Inhibition of tubulin polymerization in human A549 cells assessed as disappearance of microtubule network at 100 nM after 24 hrs by Hoechst 33342 staining-based immunocytochemistry relative to control | 2014 | Journal 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. |
| AID1883538 | Disruption of microtubule network in human MGC-803 cells assessed as irregular form of filamentous microtubule structures at 25 nM measured after 48 hrs by DAPI staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID328771 | Cell cycle arrest in human Jurkat cells at mitosis at 0.5 uM after 24 hrs | 2008 | Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8 | Isoindolo[2,1-a]quinoxaline derivatives, novel potent antitumor agents with dual inhibition of tubulin polymerization and topoisomerase I. |
| AID1785507 | Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs by MTT assay | |||
| AID744703 | Antimigratory activity against human MDA-MB-231 cells at 0.5 to 5 uM after 22 hrs by scratch wound healing assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID1272834 | Inhibition of microtubule-stimulated N-terminal MKLP-2 (56 to 505 residues) ATPase activity isolated from human hepatocellular carcinoma cells by pyruvate kinase/lactate dehydrogenase enzyme linked assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | New MKLP-2 inhibitors in the paprotrain series: Design, synthesis and biological evaluations. |
| AID214066 | Inhibition of U937 cell proliferation | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID105060 | Inhibition of MDA-MB-468 cell proliferation | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID261688 | Activity against NCI60 cell line xenograft in nude mouse by HF assay | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Assessment of in vitro and in vivo activities in the National Cancer Institute's anticancer screen with respect to chemical structure, target specificity, and mechanism of action. |
| AID670888 | Cytotoxicity against human HT-29 cells after 48 hrs by resazurin assay | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14 | Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents. |
| AID1407727 | Induction of apoptosis in human A375 cells assessed as late apoptotic cells at 100 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 3.33%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID518931 | Inhibition of tubulin in Acanthamoeba polyphaga by alamar blue assay | 2008 | Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3 | Molecular basis for resistance of acanthamoeba tubulins to all major classes of antitubulin compounds. |
| AID668144 | Antiproliferative activity against human paclitaxel-resistant PC3-TxR cells after 96 hrs by SRB assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | New substituted 4H-chromenes as anticancer agents. |
| AID1189605 | Inhibition of purified tubulin (unknown origin) assessed as critical concentration of tubulin required to produce assembly at 5 uM after 30 mins by spectrophotometry (Rvb = 3.3 +/- 0.1 uM) | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID1639378 | Inhibition of porcine brain tubulin alpha/beta polymerization at 50 uM measured every minute for 30 mins | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4 | Parvifoline Derivatives as Tubulin Polymerization Inhibitors. |
| AID271658 | Inhibition of tubulin polymerization | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents. |
| AID749382 | Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | The discovery of colchicine-SAHA hybrids as a new class of antitumor agents. |
| AID347582 | Inhibition of pig brain tubulin polymerization after 30 mins by turbidimetric assay | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID251661 | Inhibitory activity against tubulin polymerization at 20 uM | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Tubulin-polymerization inhibitors derived from thalidomide. |
| AID1058416 | Inhibition of CYP2C8 (unknown origin) at 3 uM | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24 | New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation. |
| AID1918330 | Anti-allodynic activity in MSU-induced Wistar rat gouty arthritis model assessed as mechanical allodynia at 0.5 mg/kg, iv administered once daily for 7 days and measured on day 2 | 2022 | Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21 | Overcoming Preclinical Safety Obstacles to Discover ( |
| AID311138 | Antitrypanosomal activity against Trypanosoma brucei brucei bloodstream trypomastigotes by alamar blue assay | 2007 | Journal of natural products, Aug, Volume: 70, Issue:8 | Antitrypanosomal activity of triterpenoids and sterols from the leaves of Strychnos spinosa and related compounds. |
| AID52380 | Cytotoxic activity against cellular metabolic activity of Cervix KB/HeLa tumor cell line using XTT proliferation assay after incubation with the compound for 48 h | 2003 | Journal 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. |
| AID678717 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID281699 | Induction of apoptosis in human H1299 cells assessed as caspase activation after 24 hrs | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group. |
| AID1201724 | Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID1754730 | Antiproliferative activity against human LoVo cells assessed as inhibition of proliferation after 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Synthesis and antiproliferative screening of novel doubly modified colchicines containing urea, thiourea and guanidine moieties. |
| AID1704318 | Inhibition of tubulin assembly in human SW-620 cells assessed as induction of chromosome disturbance at 5 nM incubated for 24 hrs by Hoechst 33342 staining based confocal microscopic analysis | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1473727 | Resistance index, ratio of IC50 for human DU145-TxR cells to IC50 for human DU145 cells | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID418789 | Growth inhibition of human T47D cells after 48 hrs | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Discovery and structure-activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers. |
| AID1238305 | Inhibition of hTERT mRNA expression in human HT-29 cells assessed as hTERT mRNA level at at 10 uM incubated for 48 hrs by RT-PCR method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes. |
| AID1906186 | Inhibition of pig brain tubulin polymerization at 6 uM by spectrophotometer analysis | |||
| AID1414059 | Fungicidal activity against Paecilomyces variotii BAM19 ATCC 18502 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID657576 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10 | Design, synthesis and biological evaluation of novel chalcone derivatives as antitubulin agents. |
| AID132745 | Percent increase in life-span against in vivo P388 murine leukemia at a dose 0.25 mg/kg in trail 1 | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID681130 | TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID1428412 | Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by SRB assay | |||
| AID1550795 | Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 0.4 uM measured after 24 hrs by DAPI staining based HCS analysis | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop. |
| AID1785510 | Antiproliferative activity against human THP-1 cells incubated for 72 hrs by MTT assay | |||
| AID394854 | Cytotoxicity against human LNCAP cells after 48 hrs by SRB assay | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships. |
| AID1194049 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8 | Synthesis and biological evaluation of benzimidazole acridine derivatives as potential DNA-binding and apoptosis-inducing agents. |
| AID93939 | The compound was tested in vitro for growth of inhibitory activity against lymphoid leukemia L1210 cells | 1989 | Journal of medicinal chemistry, Oct, Volume: 32, Issue:10 | New anticancer agents: alterations of the carbamate group of ethyl (5-amino-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-yl)car bamates. |
| AID1807436 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Design, structure-activity relationship study and biological evaluation of the thieno[3,2-c]isoquinoline scaffold as a potential anti-cancer agent. |
| AID143034 | Antiproliferative activity against the human non small cell lung carcinoma cell line NCI-H460 | 2002 | Bioorganic & 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. |
| AID1550785 | Antiproliferative activity against human HeLa cells measured after 3 days by Coulter counter method | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop. |
| AID611269 | Cytotoxicity against human NCI-H460 cells after 48 hrs by XTT assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Phenylimino-10H-anthracen-9-ones as novel antimicrotubule agents-synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID101632 | Inhibition of the growth of MDA-MB 231 human breast cancer cells | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22 | Inhibition of tubulin polymerization by 5,6-dihydroindolo[2,1-alpha]isoquinoline derivatives. |
| AID1320574 | Destabilization of rhodamine labeled porcine microtubule assessed as appearance of short strands microtubules at 10 uM after 5 mins by upright fluorescence microscopic analysis | 2016 | Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20 | Antitumor Activity of Lankacidin Group Antibiotics Is Due to Microtubule Stabilization via a Paclitaxel-like Mechanism. |
| AID1492876 | Inhibition of tubulin polymerization (unknown origin) preincubated for 10 mins followed by GTP addition measured after 20 mins by Coomassie blue staining based SDS-PAGE analysis | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. |
| AID1736528 | Induction of apoptosis in human HT-29 cells assessed as late apoptotic cells at 0.25 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.0 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID1917311 | Inhibition of pig brain tubulin polymerization by spectrometric method | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors. |
| AID1189166 | Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 0.25 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.10%) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID96598 | Concentration that causes a mitotic index (number of cells in mitosis divided by total cells) of 0.5 for cultured lymphoid leukemia L1210 cells during an exposure period of 12 h | 1992 | Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26 | Antimitotic agents: ring analogues and derivatives of ethyl [(S)-5-amino-1,2-dihydro-2-methyl-3-phenylpyrido[3,4-b]pyrazin-7- yl]carbamate. |
| AID700072 | Solubility of the compound in presence of 20% serum | 2012 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21 | Part II. Development of novel colchicine-derived immunosuppressants with improved pharmacokinetic properties. |
| AID1856348 | Inhibition of tubulin polymerization in human MCF7 cells by ELISA | |||
| AID588208 | Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset | 2010 | Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5 | Predicting phospholipidosis using machine learning. |
| AID1338403 | Cell cycle arrest in human 786-0 cells assessed as accumulation at G1 phase at 1.25 uM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb=47.1+/-1%) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and evaluation of novel hybrids β-carboline-4-thiazolidinones as potential antitumor and antiviral agents. |
| AID274816 | Cell cycle arrest in KB/HeLa cells by accumulation at S phase at 316 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID401021 | Displacement of [3H]colchicine from rat brain tubulin at 25 uM | |||
| AID665236 | Inhibition of bovine brain tubulin at 2.5 uM after 10 mins by spectrophotometry | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | N⁴-Phenyl-substituted 2-acetylpyridine thiosemicarbazones: cytotoxicity against human tumor cells, structure-activity relationship studies and investigation on the mechanism of action. |
| AID642052 | Growth inhibition of human MCF7 cells after 96 hrs | 2011 | Journal 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. |
| AID1503407 | Inhibition of beta tubulin assembly in human Colo-357 cells at 5 uM incubated for 24 hrs by anti-tubulin antibody based confocal microscopy | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID390908 | Inhibition of tubulin polymerization assessed as effect on maximum propogation rate | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Novel microtubule-interacting phenoxy pyridine and phenyl sulfanyl pyridine analogues for cancer therapy. |
| AID1736447 | Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID214350 | Binding affinity against tubulin usingf [3H]-colchicine as radioligand | 1980 | Journal of medicinal chemistry, May, Volume: 23, Issue:5 | Structure--antitubulin activity relationship in steganacin congeners and analogues. Inhibition of tubulin polymerization in vitro by (+/-)-isodeoxypodophyllotoxin. |
| AID137225 | In vivo antitumor activity was measured in mice (P388 leukemia) at dose 1 mg/kg after intraperitoneal administration | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Synthesis and antitumor activity of tropolone derivatives. |
| AID1755837 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective. |
| AID1638336 | Inhibition of EBI binding to beta-tubulin colchicine binding site in human MGC803 cells at 10 uM preincubated for 2 hrs followed by EBI addition and measured after 2 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Mar-01, Volume: 165 | Molecular diversity of trimethoxyphenyl-1,2,3-triazole hybrids as novel colchicine site tubulin polymerization inhibitors. |
| AID1320559 | Destabilization of microtubule network in human T47D cells at 0.5 uM after 2 hrs by DAPI staining-based immunofluorescence assay | 2016 | Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20 | Antitumor Activity of Lankacidin Group Antibiotics Is Due to Microtubule Stabilization via a Paclitaxel-like Mechanism. |
| AID1492845 | Antiproliferative activity against human HL60 cells after 96 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. |
| AID1550784 | Antiproliferative activity against human CEM cells measured after 96 hrs by Coulter counter method | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop. |
| AID1898103 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID719105 | Cytotoxicity against human A2780 cells assessed as growth inhibition | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation. |
| AID428053 | Immunosuppressive activity in mouse splenocytes assessed as inhibition of allogenic mixed lymphocyte reaction | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Design, synthesis and identification of novel colchicine-derived immunosuppressant. |
| AID1566320 | Cell cycle arrest in human MCF7 cells assessed as accumulation in subG1 phase at 5 times of antiproliferative IC50 incubated for 24 hrs by propidium iodide based flow cytometry (Rvb = 7.79 %) | |||
| AID774674 | Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18 | New phenstatin-fatty acid conjugates: synthesis and evaluation. |
| AID1673970 | Cytotoxicity against mouse BALB/3T3 cells incubated for 72 hrs by sulforhodamine B assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID637197 | Inhibition of bovine brain tubulin polymerization preincubated for 10 mins measured after 20 mins | 2012 | Bioorganic & 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. |
| AID1628419 | Induction of apoptosis in human A549 cells assessed as induction of cell shrinkage at 40 nM incubated for 24 hrs microscopy | 2016 | Journal 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. |
| AID337171 | Antiviral activity against HIV1 HTLV-3B in human H9 cells after 3 days by p24 antigen capture assay | |||
| AID1704325 | Acute toxicity in iv dosed CD-1 mouse assessed as mouse death at 5 mg/kg, iv measured after 16 hrs | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID758712 | Growth inhibition of human MCF7 cells at 10 uM after 72 hrs by MTT assay relative to control | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID1625713 | Antiproliferative activity against human SKOV3 cells after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1167521 | Antiproliferative activity against mouse L1210 assessed as inhibition of cell proliferation after 48 hrs by Coulter counter based cell counting method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Synthesis and antiproliferative activity of 6-phenylaminopurines. |
| AID697554 | Antiproliferative activity against human A375 cells after 48 hrs by SRB assay | 2012 | Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16 | Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents. |
| AID1695278 | Induction of cell cycle arrest in human COLO357 cells assessed as G2/M phase at 5 uM incubated for 72 hrs by propidium iodide staining based flow cytometry analysis (Rvb = 7.2 %) | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
| AID404615 | Antiproliferative activity against mouse L1210 cells after 72 hrs | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | New C5-alkylated indolobenzazepinones acting as inhibitors of tubulin polymerization: cytotoxic and antitumor activities. |
| AID721873 | Cytotoxicity against human MESSA/DX5 cells assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay | 2013 | Journal 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. |
| AID1527068 | Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability incubated for 24 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
| AID91688 | In vitro inhibition of tubulin polymerization. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Antitumor agents. 141. Synthesis and biological evaluation of novel thiocolchicine analogs: N-acyl-, N-aroyl-, and N-(substituted benzyl)deacetylthiocolchicines as potent cytotoxic and antimitotic compounds. |
| AID1883550 | Binding affinity to beta-tubulin colchicine binding site in human HGC-27 cells assessed as decrease in beta-tubulin adduct band at 10 uM incubated for 2 hrs by EBI alkylate competition assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID1883544 | Disruption of microtubule network in human HGC-27 cells assessed as irregular form of filamentous microtubule structures at 25 nM measured after 48 hrs by DAPI staining based fluorescence microscopic analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID1238304 | Inhibition of VEGF mRNA expression in human HT-29 cells assessed as VEGF mRNA level at at 50 nM incubated for 48 hrs by RT-PCR method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes. |
| AID1473711 | Antimigratory activity in human RPMI7951 cells assessed as wound closure at 25 nM after 18 hrs (Rvb = 71.8 +/- 1.8%) | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID351385 | Cell cycle arrest in human leukemic cells assessed as mitotic block by cytometry | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Novel carbazole and acyl-indole antimitotics. |
| AID75539 | Ability to inhibit the dibutyryl-cAMP-induced change of an immature glioma cell to a mature, differentiated astrocyte by in vitro astrocytoma assay at 0.1 ug/mL dose (Experiment #2); value may range from 0 to 5 | 1987 | Journal of medicinal chemistry, Oct, Volume: 30, Issue:10 | In vivo antitumor activity of 6-benzyl-1,3-benzodioxole derivatives against the P388, L1210, B16, and M5076 murine models. |
| AID1357214 | Inhibition of bovine brain tubulin polymerization at 10 uM measured every 1 min for 20 mins by spectrophotometry | 2018 | Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17 | Structural Modification of the 3,4,5-Trimethoxyphenyl Moiety in the Tubulin Inhibitor VERU-111 Leads to Improved Antiproliferative Activities. |
| AID383988 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of >4N cells at 2 uM after 24 hrs by flow cytometry | 2008 | Journal 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. |
| AID1882895 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID662407 | Cytotoxicity against human TW03 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12 | Synthesis, characterization and in vitro anti-tumor activities of matrine derivatives. |
| AID605772 | Antiproliferative activity against paclitaxel-resistant CHO-VV 3-2 cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID1235364 | Displacement of 1 uM of [3H]colchicine from biotin-labeled tubulin (unknown origin) after 2 hrs by scintillation proximity assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes. |
| AID1124107 | Mitotic arrest in CHO cells assessed as increase in cell accumulation at 0.02 ug/ml | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Structure-activity relationships of dimeric Catharanthus alkaloids. 2. Experimental antitumor activities of N-substituted deacetylvinblastine amide (vindesine) sulfates. |
| AID657577 | Inhibition of bovine tubulin polymerization after 20 mins by spectrophotometry | 2012 | Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10 | Design, synthesis and biological evaluation of novel chalcone derivatives as antitubulin agents. |
| AID595052 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2011 | Bioorganic & 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. |
| AID1870922 | Induction of microtubule depolymerization in human A549 cells assessed as reduction in tubulin protein level at 2.5 uM by Western blot analysis | |||
| AID540213 | Half life in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1384285 | Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 50 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 73 +/- 3%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID1435798 | Induction of lysosomal membrane hyperpolarization in 3D culture of human Colo-357 cells at 1 uM measured after 48 hrs by LysoTrackRed dye based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1672882 | Antiproliferative activity against human A2780 cells incubated for 72 hrs by ATPlite reagent based assay | 2019 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13 | Resistance mechanisms and cross-resistance for a pyridine-pyrimidine amide inhibitor of microtubule polymerization. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID730215 | Cytotoxicity against human HT1080 cells after 72 hrs by CCK-8 assay | 2013 | Journal 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. |
| AID1821558 | Antiproliferative activity against human MGC-803 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Design, synthesis and evaluation of novel bis-substituted aromatic amide dithiocarbamate derivatives as colchicine site tubulin polymerization inhibitors with potent anticancer activities. |
| AID483367 | Inhibition of microtubule polymerization at 10 uM after 10 mins | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Syntheses and biological evaluation of ring-C modified colchicine analogs. |
| AID1756951 | Selectivity index, ratio of IC50 for cytotoxicity against mouse BALB/3T3 cells to IC50 for antiproliferative activity against human MCF7 cells | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | An insight into the anticancer potential of carbamates and thiocarbamates of 10-demethoxy-10-methylaminocolchicine. |
| AID1807384 | Cytotoxicity against human MDA-MB-231 cells measured after 72 hrs by western blot | |||
| AID1267182 | Inhibition of porcine brain tubulin polymerization assessed as reduction in GTP-induced microtubule assembly after 60 mins by OD340 method | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer. |
| AID1550787 | Antiproliferative activity against human HMEC1 cells measured after 4 days by Coulter counter method | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop. |
| AID1333464 | Ratio of Bcl-2 to Bax gene expression in human MDA-MB-231 cells at 5 uM after 24 hrs by RT-PCR method (Rvb = 0.03 No_unit) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID214716 | Inhibitory activity against tubulin polymerization at 1.0 mM concentration | 1999 | Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20 | Stabilization of microtubules by Combretastatin D derivatives. |
| AID473622 | Antiproliferative activity against human MCF7 cells after 72 hrs by crystal violet biomass reduction assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8 | N-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)arylamide as a new scaffold that provides rapid access to antimicrotubule agents: synthesis and evaluation of antiproliferative activity against select cancer cell lines. |
| AID1569090 | Resistance index, ratio of IC50 for human DU145-TxR cells to IC50 for human DU145 cells | |||
| AID1431298 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for human MCF7 cells | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID7783 | Unbound fraction (plasma) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
| AID80380 | Cytotoxicity against human solid tumor Colon carcinoma HCT-8 cell line | 1993 | Journal 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 |
| AID1320433 | Disruption of interphase microtubule in HUVEC assessed as change in cell morphology at 1 uM after 90 mins by DAPI staining-based immunofluorescence assay | 2016 | Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20 | Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4. |
| AID418797 | Inhibition of tubulin polymerization by DAPI fluorescence method | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7 | Discovery and structure-activity relationships of (2-(arylthio)benzylideneamino)guanidines as a novel series of potent apoptosis inducers. |
| AID1566337 | Induction of cell death in human ALL5 cells assessed as decrease in 4 N DNA at 5 times of antiproliferative IC50 incubated for 72 hrs by propidium iodide based flow cytometry | |||
| AID1527064 | Induction of P-gp in human LS180 cells assessed as increase in intracellular accumulation of Rh123 at 100 nM using Rho123 as substrate preincubated for 48 hrs followed by addition of Rh123 and measured after 90 mins by fluorescence based assay relative to | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
| AID526952 | Cytotoxicity against human PPC1 cells after 48 hrs by sulforhodamine B assay | 2010 | Journal 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. |
| AID134555 | Compound was tested for toxicity in P388 tumored mice | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID42750 | In vitro growth inhibition of CAKI-1, Kidney carcinoma | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors. |
| AID1201719 | Inhibition of recombinant human HDAC1 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID645071 | Cytotoxicity against human A549 cells after 96 hrs using tetracolor one | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Design, Synthesis, and Antitumor Activity of 4-Halocolchicines and Their Pro-drugs Activated by Cathepsin B. |
| AID627402 | Antiproliferative activity against human MDA-MB-231 after 48 hrs by SRB assay | 2011 | European 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. |
| AID719106 | Cytotoxicity against human DLD1 cells assessed as growth inhibition | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation. |
| AID1500597 | Antiproliferative activity against human HCT8 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents. |
| AID1189167 | Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 0.25 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometry (Rvb = 0.47%) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID605716 | Antiproliferative activity against human K562 cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID1435789 | Induction of apoptosis in 3D culture of human MIAPaCa2 cells assessed as accumulation at G2/M phase at 1 uM measured after 72 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1503415 | Gastrointestinal toxicity in human HT-29 cells assessed as effect on endosomes at 5 uM incubated for 3 hrs by flow cytometry | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID347983 | Cell cycle arrest in human KB/HeLa cells assessed as G2/M phase accumulation after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1272839 | Growth inhibition of human KB cells at 10 uM after 72 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | New MKLP-2 inhibitors in the paprotrain series: Design, synthesis and biological evaluations. |
| AID1903069 | Antiproliferative activity against human MCF7 cells over expressing GLUT1 measured after 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 03-15, Volume: 58 | Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors. |
| AID1503419 | Gastrointestinal toxicity in human HT-29 cells assessed as relocation from perinuclear position to cytoplasm at 5 uM incubated for 3 hrs by flow cytometry | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID1075755 | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 300 nM after 24 hrs by propidium iodide staining-based FACS analysis | 2014 | Journal 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. |
| AID1549997 | Binding affinity to alpha/beta tubulin complex (unknown origin) | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain. |
| AID1384281 | Inhibition of tubulin polymerization (unknown origin) in glycerol-assembly buffer assessed as critical concentration of tubulin required for assembly at 27.5 uM measured every 30 secs for 2 hrs in presence of GTP (Rvb = 9 +/- 2 uM) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID1625812 | Competitive binding affinity to beta-tubulin in human HepG2 cells assessed as disappearance of EBI-protein adducts at 5 uM preincubated for 2 hrs followed by EBI addition measured after 1.5 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID303702 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at S phase at 1 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1124106 | Mitotic arrest in CHO cells assessed as increase in cell accumulation at 0.2 ug/ml | 1979 | Journal of medicinal chemistry, Apr, Volume: 22, Issue:4 | Structure-activity relationships of dimeric Catharanthus alkaloids. 2. Experimental antitumor activities of N-substituted deacetylvinblastine amide (vindesine) sulfates. |
| AID422576 | Cytotoxicity against human H460 cells after 72 hrs by methylene blue dye assay | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and evaluation of 3-aroylindoles as anticancer agents: metabolite approach. |
| AID642530 | Growth inhibition of human MKN45 cells after 72 hrs by methylene blue assay | 2011 | Journal 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. |
| AID1566323 | Cell cycle arrest in human MCF7 cells assessed as accumulation in S phase at 5 times of antiproliferative IC50 incubated for 24 hrs by propidium iodide based flow cytometry (Rvb = 19.9 %) | |||
| AID317729 | Antiviral activity against HIV1RF infected in human CEM-SS cells | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
| AID1489119 | Induction of tubulin depolymerization in human MCF7 cells at 1 uM after 12 hrs by DAPI staining based confocal microscopic analysis | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 | Design and synthesis of piperazine acetate podophyllotoxin ester derivatives targeting tubulin depolymerization as new anticancer agents. |
| AID1414048 | Cytotoxicity against arrested non-proliferative human SKOV3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID1758694 | Cytotoxicity against human BEAS-2B cells assessed as reduction in cell growth by CCK8 assay | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Synthesis and structure-activity relationships of 5-phenyloxazole-2-carboxylic acid derivatives as novel inhibitors of tubulin polymerization. |
| AID494509 | Antiproliferative activity against human RKO cells expressing p27Kip1 after 48 hrs by XTT assay | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis, antiproliferative activity and inhibition of tubulin polymerization by 1,5- and 1,8-disubstituted 10H-anthracen-9-ones bearing a 10-benzylidene or 10-(2-oxo-2-phenylethylidene) moiety. |
| AID348005 | Cell cycle arrest in human KB/HeLa cells assessed as S phase accumulation at 316 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID277282 | Cytotoxicity against P-glycoprotein-overexpressing KB-V1 cell line | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Highly potent triazole-based tubulin polymerization inhibitors. |
| AID274787 | Antiproliferative activity against SKOV3 cells by XTT assay after 48 hrs | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID8002 | Observed volume of distribution | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
| AID1179656 | Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay | 2014 | Bioorganic & 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. |
| AID1384333 | Inhibition of VEGF protein secretion in human HT-29 cells assessed as VEGF protein level at 40 nM after 48 hrs by ELISA (Rvb = 100%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID150753 | Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID281505 | Growth inhibition of human MCF7 cells assessed as G2/M DNA content after 48 hrs | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Arylthioindoles, potent inhibitors of tubulin polymerization. |
| AID1897657 | Induction of cell cycle arrest in human HCT-116 cells assessed as increase in G2/M phase cells at 20 nM measured after 48 hrs by propidium iodide/RNase staining based flow cytometry analysis (Rvb = 61.51 %) | 2022 | Bioorganic & medicinal chemistry, 12-15, Volume: 76 | Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities. |
| AID1316908 | Binding affinity to porcine alpha/beta tubulin assessed as decrease in tryptophan fluorescence measured after 30 mins by tryptophan fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Discovery of O |
| AID1368405 | Inhibition of beta-tubulin polymerization in human A549 cells at 1 uM after 12 to 24 hrs by DAPI staining based confocal microscopic method | 2018 | Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1 | N-Arylsulfonylsubstituted-1H indole derivatives as small molecule dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and tubulin. |
| AID1625740 | Resistance index, ratio of IC50 for P-gp overexpressing human MCF7/ADR cells to IC50 for human MCF7 cells | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors. |
| AID1435800 | Induction of cell membrane permeability in 3D culture of human Colo-357 cells at 1 uM measured after 48 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID494501 | Antiproliferative activity against human K562 cells after 48 hrs | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis, antiproliferative activity and inhibition of tubulin polymerization by 1,5- and 1,8-disubstituted 10H-anthracen-9-ones bearing a 10-benzylidene or 10-(2-oxo-2-phenylethylidene) moiety. |
| AID1500657 | Cell cycle arrest in human AGS cells assessed as accumulation at G2/M phase at 50 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 9.18%) | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of 9H-purins as potential tubulin polymerization inhibitors: Synthesis, biological evaluation and structure-activity relationships. |
| AID1189145 | Antiproliferative activity against human HepG2 cells after 48 hrs by SRB method | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID274814 | Cell cycle arrest in KB/HeLa cells by accumulation at S phase at 31.6 nM | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID303725 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G1 phase at 316 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1235365 | Displacement of 82.8 +/- 0.9 uM of [3H]colchicine from biotin-labeled tubulin (unknown origin) after 2 hrs by scintillation proximity assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes. |
| AID422579 | Displacement of [3H]colchicine from tubulin at 5 uM after 1 hr by scintillation counter | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Synthesis and evaluation of 3-aroylindoles as anticancer agents: metabolite approach. |
| AID1193499 | Thermodynamic equilibrium solubility, log S of the compound simulated intestinal fluid at pH 6.8 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
| AID1785487 | Induction of irreversible mitotic block in human A2780S cells at 100 uM incubated for 12 hrs followed by compound elution and measured after 10 hrs | |||
| AID1354606 | Inhibition of cell migration in human MDA-MB-231 cells at 5 uM incubated for 24 hrs by scratch wound healing assay relative to control | 2018 | Journal of natural products, 05-25, Volume: 81, Issue:5 | Inhibition of Breast Cancer Cell Migration by Cyclotides Isolated from Pombalia calceolaria. |
| AID744710 | Antimitotic activity in human HeLa cells assessed as cell density loss after 24 hrs by Hoechst 33342 staining | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID200637 | In vitro cytotoxicity against SNB-19 cell line. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Antitumor agents. 141. Synthesis and biological evaluation of novel thiocolchicine analogs: N-acyl-, N-aroyl-, and N-(substituted benzyl)deacetylthiocolchicines as potent cytotoxic and antimitotic compounds. |
| AID1877696 | Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 8 uM measured after 24 hrs by flow cytometry (Rvb = 15.37%) | 2022 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 57 | Shikonin N-benzyl matrinic acid ester derivatives as novel telomerase inhibitors with potent activity against lung cancer cell lines. |
| AID1740978 | Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Discovery of tertiary amide derivatives incorporating benzothiazole moiety as anti-gastric cancer agents in vitro via inhibiting tubulin polymerization and activating the Hippo signaling pathway. |
| AID479368 | Selectivity ratio of IC50 for vincristine-resistant human HL60 cells to IC50 for human HL60 cells | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Phenylcinnamides as novel antimitotic agents. |
| AID1503409 | Growth inhibition of human Colo-357 cells incubated for 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids. |
| AID1320440 | Disruption of interphase microtubule in HUVEC assessed as change in cell shape and morphology at 1 uM preincubated for 30 mins followed by compound washout measured after 120 mins by DAPI staining-based immunofluorescence assay | 2016 | Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20 | Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4. |
| AID494504 | Antiproliferative activity against human SKOV3 cells after 48 hrs by XTT assay | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis, antiproliferative activity and inhibition of tubulin polymerization by 1,5- and 1,8-disubstituted 10H-anthracen-9-ones bearing a 10-benzylidene or 10-(2-oxo-2-phenylethylidene) moiety. |
| AID1704315 | Inhibition of tubulin assembly in human COLO357 cells assessed as induction of chromosome disturbance at 5 nM incubated for 24 hrs by Hoechst 33342 staining based confocal microscopic analysis | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID733789 | Cytotoxicity against human MCF7 cells by MTT assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis and biological evaluation of novel pyranochalcone derivatives as a new class of microtubule stabilizing agents. |
| AID514411 | Cytotoxicity against human KB cells after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
| AID1163569 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Synthesis and biological evaluation of novel millepachine derivatives as a new class of tubulin polymerization inhibitors. |
| AID1500622 | Induction of alpha-tubulin depolymerization in human A2780S cells at 100 nM after 24 hrs by DAPI staining based immunofluorescence microscopic method | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Design, synthesis and biological evaluation of 4-anilinoquinoline derivatives as novel potent tubulin depolymerization agents. |
| AID551510 | Binding affinity to porcine tubulin after 1 hr by spectrofluorometric analysis | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Tubulin photoaffinity labeling study with a plinabulin chemical probe possessing a biotin tag at the oxazole. |
| AID1189151 | Antiproliferative activity against doxorubicin-resistant human MCF7 cells after 48 hrs by SRB method | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID336353 | Cytotoxicity against human SK-MEL-2 cells | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID404304 | Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2). |
| AID1731996 | Inhibition of pig brain tubulin polymerization by spectrophotometry | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Novel diaryl-2H-azirines: Antitumor hybrids for dual-targeting tubulin and DNA. |
| AID1850713 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2022 | RSC medicinal chemistry, May-25, Volume: 13, Issue:5 | Morpholine substituted quinazoline derivatives as anticancer agents against MCF-7, A549 and SHSY-5Y cancer cell lines and mechanistic studies. |
| AID1333475 | Effect on p27 mRNA expression in human MDA-MB-231 cells assessed as ratio of p27 to GAPDH expression level at 5 uM after 24 hrs by RT-PCR method (Rvb = 0.23 No_unit) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1897671 | Induction of microtubule disruption in human HCT-116 cells assessed as short microtubules at 20 nM incubated for 48 hrs by DAPI staining based confocal microscopic immunofluorescence analysis | 2022 | Bioorganic & medicinal chemistry, 12-15, Volume: 76 | Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities. |
| AID1125805 | Cytotoxicity against human HT-29 cells after 72 hrs by methylene blue assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Antimitotic and vascular disrupting agents: 2-hydroxy-3,4,5-trimethoxybenzophenones. |
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| AID1435782 | Cytotoxicity against 2D culture of human EAhy926 cells measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1226622 | Inhibition of acetylated tubulin accumulation in human HeLa cells at 30 to 100 nM after 6 hrs by Western blot analysis | 2015 | Journal of medicinal chemistry, May-28, Volume: 58, Issue:10 | Methyl 3-((6-methoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)amino)benzoate (GN39482) as a tubulin polymerization inhibitor identified by MorphoBase and ChemProteoBase profiling methods. |
| AID597797 | Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Imidazolone-amide bridges and their effects on tubulin polymerization in cis-locked vinylogous combretastatin-A4 analogues: synthesis and biological evaluation. |
| AID670878 | Inhibition of bovine brain microtubule polymerization by spectrophotometric analysis | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14 | Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents. |
| AID1807447 | Inhibition of microtubule (unknown origin) polymerization at 0.6 uM | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Design, structure-activity relationship study and biological evaluation of the thieno[3,2-c]isoquinoline scaffold as a potential anti-cancer agent. |
| AID1639379 | Inhibition of porcine brain tubulin alpha/beta polymerization at 10 uM measured every minute for 30 mins | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4 | Parvifoline Derivatives as Tubulin Polymerization Inhibitors. |
| AID611278 | Inhibition of pig brain tubulin polymerization after 30 mins by turbidimetry analysis | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Phenylimino-10H-anthracen-9-ones as novel antimicrotubule agents-synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID303684 | Antiproliferative activity against human K562 cells after 48 hrs | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID730203 | Selectivity ratio of IC50 for quesicent HUVECs to IC50 for activated HUVECs | 2013 | Journal 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. |
| AID611279 | Displacement of [3H]colchicine from biotinylated pig brain tubulin after 2 hrs by competitive scintillation proximity assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Phenylimino-10H-anthracen-9-ones as novel antimicrotubule agents-synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID351391 | Binding affinity to purine-binding protein in human red blood cells | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Novel carbazole and acyl-indole antimitotics. |
| AID758695 | Induction of apoptosis in human HepG2 cells assessed as apoptotic cells at 10 uM after 72 hrs by annexin V-FITC/PI staining-based FACS flow cytometric analysis (Rvb = 13.9 +/- 1.2%) | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID526951 | Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay | 2010 | Journal 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. |
| AID1296732 | Cytotoxicity against human A549 cells after 48 hrs by Celltiter-Glo luminescent cell viability assay | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology. |
| AID1435409 | Cytotoxicity against human Hs 371.T cells by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and cytotoxic activity of certain novel chalcone analogous compounds. |
| AID1785492 | Non-covalent binding affinity to tubulin (unknown origin) assessed as compound detected in tubulin fraction at 450 pmol incubated for 1 hr by UFLC-MS/MS analysis | |||
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| AID1888932 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Synthesis and biological evaluation of 3β-O-neoglycosides of caudatin and its analogues as potential anticancer agents. |
| AID1756949 | Resistance index, ratio of IC50 for antiproliferative activity against human Lovo/DX cells to IC50 for antiproliferative activity against human Lovo cells | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | An insight into the anticancer potential of carbamates and thiocarbamates of 10-demethoxy-10-methylaminocolchicine. |
| AID1492879 | Binding affinity to tubulin (unknown origin) by ITC method | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. |
| AID225315 | Percent inhibition of [3H]colchicine binding to tubulin with molar ratio of 1:10 (inhibitor: [3H]colchicine) | 1993 | Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6 | Synthesis and tubulin binding of novel C-10 analogues of colchicine. |
| AID404617 | Antiproliferative activity against human HT29 cells after 72 hrs | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | New C5-alkylated indolobenzazepinones acting as inhibitors of tubulin polymerization: cytotoxic and antitumor activities. |
| AID596143 | Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9 | Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors. |
| AID366382 | Induction of apoptosis in human T47D cells assessed as caspase 3 activation after 24 hrs | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a potent inducer of apoptosis with high in vivo activity. |
| AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID312973 | Induction of apoptosis in human SNU398 cells assessed as caspase activation after 24 hrs by HTS assay | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions. |
| AID603021 | Inhibition of purified bovine brain tubulin microtubule assembly at 2 uM | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis, antiproliferative activity, and mechanism of action of a series of 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides. |
| AID1628418 | Induction of apoptosis in human A549 cells assessed as induction of cytoplasmic membrane blebbing at 40 nM incubated for 24 hrs microscopy | 2016 | Journal 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. |
| AID602746 | Antiproliferative activity against human K562 cells at 10 uM after 48 hrs by trypan blue assay | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis, antiproliferative activity, and mechanism of action of a series of 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides. |
| AID670880 | Binding affinity to bovine brain tubulin by spectrophotometric analysis | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14 | Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents. |
| AID605775 | Resistant ratio of IC50 for multidrug-resistant human CEM-VLB cells to IC50 for human CEM cells | 2011 | Journal 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. |
| AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID637200 | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 5 ug/ml after 24 hrs by flow cytometric analysis (Rvb = 18%) | 2012 | Bioorganic & 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. |
| AID152355 | Cytotoxicity against murine P388 leukemia cell line | 1993 | Journal 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 |
| AID336348 | Antimitotic activity against rat ASK cells assessed as reversal of astrocyte morphology at 4 ug/ml | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID1296735 | Inhibition of microtubule network formation in human MDA-MB-231 cells at 100 nM after 24 hrs by DAPI staining based immunofluorescence microscopic analysis | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology. |
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| AID1582220 | Antiproliferative activity against human DU145-TxR cells measured after 72 hrs by MTS assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties. |
| AID1628432 | Induction of apoptosis in human A549 cells assessed as late apoptotic cells level at 40 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FACS flow cytometry (Rvb = 2.15%) | 2016 | Journal 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. |
| AID1785502 | Antiproliferative activity against human HT-29 cells incubated for 72 hrs by MTT assay | |||
| AID1628398 | Growth inhibition of human HepG2 cells incubated for 72 hrs by MTT assay | 2016 | Journal 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. |
| AID1807386 | Resistance index, ratio of IC50 for cytotoxicity against paclitaxel resistant human MDA-MB-231/TxR cells to IC50 cytotoxicity against human MDA-MB-231 cells | |||
| AID699540 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID1333485 | Inhibition of Akt in human MDA-MB-231 cells assessed as ratio of phosphorylated GSK-3beta to GAPDH expression level at 5 uM after 48 hrs by immunoblot analysis (Rvb = 0.14 to 1.50 No_unit) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID1673994 | Inhibition of tubulin polymerization (unknown origin) incubated for 20 mins | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1700959 | Induction of microtubule cytoskeleton disruption in human HepG2 cells assessed as microtubule shrinkage to the cell border at 10 nM measured after 24 hrs by Hoechst 33342 staining based immunofluorescence confocal microscopy analysis | |||
| AID270966 | Inhibition of [3H]colchicine binding to beta tubulin | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19 | [4-(imidazol-1-yl)thiazol-2-yl]phenylamines. A novel class of highly potent colchicine site binding tubulin inhibitors: synthesis and cytotoxic activity on selected human cancer cell lines. |
| AID719101 | Cytotoxicity against human HeLa cells harboring class 3 beta tubulin mutant assessed as growth inhibition | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24 | Synthesis and biological evaluation of colchicine C-ring analogues tethered with aliphatic linkers suitable for prodrug derivatisation. |
| AID1189150 | Antiproliferative activity against cis-platinum-resistant human A549 cells after 48 hrs by SRB method | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1756947 | Antiproliferative activity against human Lovo/DX cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | An insight into the anticancer potential of carbamates and thiocarbamates of 10-demethoxy-10-methylaminocolchicine. |
| AID90442 | Cytotoxic activity against human colon adenocarcinoma RKO cells without ectopic inducible expression of cyclin-dependent kinase inhibitor p27kip1 | 2003 | Journal 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. |
| AID1382774 | Antiproliferative activity against mouse L1210 cells after 96 hrs by coulter counting method | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity. |
| AID1586076 | Displacement of [3H]-colchicine from bovine brain tubulin at 5 uM by scintillation proximity assay relative to control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. |
| AID735023 | Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells in G2/M phase at 2uM concentration after 24 hrs by propidium iodide staining based cytofluorimetric analysis (Rvb = 12.95%) | 2013 | European 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. |
| AID716411 | Inhibition of sheep brain tubulin assembly compound incubated for 10 mins at 37 degC followed by 5 mins incubation at 0 degC by turbidimetry | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4. |
| AID721885 | Inhibition of tubulin (unknown origin) polymerization preincubated for 15 mins by spectrophotometry | 2013 | Journal 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. |
| AID1809655 | Antiproliferative activity against human Lovo/DX cells assessed as inhibition of cell proliferation incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Synthesis of thiocolchicine amine derivatives and evaluation of their antiproliferative activity. |
| AID1736443 | Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID665238 | Induction of mitotic arrest in human HeLa cells assessed as reduction in cell density by immunofluorescence staining | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | N⁴-Phenyl-substituted 2-acetylpyridine thiosemicarbazones: cytotoxicity against human tumor cells, structure-activity relationship studies and investigation on the mechanism of action. |
| AID384006 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation of 4N cells at 2 uM after 72 hrs by flow cytometry | 2008 | Journal 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. |
| AID624622 | Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID1185459 | Displacement of [3H]colchicine from long-chain biotin-labeled tubulin (unknown origin) at 5 uM after 2 hrs by competition-binding scintillation proximity assay | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Concise syntheses of 7-anilino-indoline-N-benzenesulfonamides as antimitotic and vascular disrupting agents. |
| AID1863114 | Induction of microtubule disruption in human MGC-803 cells at 25 nmol/L measured after 48 hrs by DAPI staining based immunofluorescence assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway. |
| AID662404 | Cytotoxicity against human HEP7402 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12 | Synthesis, characterization and in vitro anti-tumor activities of matrine derivatives. |
| AID1898097 | Antiproliferative activity against human NCI-H1437 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID1704323 | Acute toxicity in iv dosed CBA mouse assessed as mouse death at 5 mg/kg, iv measured after 16 hrs | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID626621 | Ratio of IC50 for colchicine and vinblastine-resistant CHO-VV 3-2 cells to IC50 for CHO cells | 2011 | European 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. |
| AID1189606 | Inhibition of purified tubulin (unknown origin) assessed as critical concentration of tubulin required to produce assembly at 10 uM after 30 mins by spectrophotometry (Rvb = 3.3 +/- 0.1 uM) | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID1163573 | Antiproliferative activity against human HCT116 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Synthesis and biological evaluation of novel millepachine derivatives as a new class of tubulin polymerization inhibitors. |
| AID1562394 | Inhibition of pig brain tubulin polymerization at 6 uM measured every 1 min for 25 mins by spectrophotometric method | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin. |
| AID514412 | Cytotoxicity against human KBVIN cells expressing p-glycoprotein after 2 days | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Antitumor agents 273. Design and synthesis of N-alkyl-thiocolchicinoids as potential antitumor agents. |
| AID657578 | Cell cycle arrest in human MCF7 cells assessed as accumulation in G0/G1 phase at 5 ug/ml after 24 hrs by flow cytometry (Rvb = 47.79%) | 2012 | Bioorganic & medicinal chemistry, May-15, Volume: 20, Issue:10 | Design, synthesis and biological evaluation of novel chalcone derivatives as antitubulin agents. |
| AID1435787 | Induction of apoptosis in 2D culture of human MIAPaCa2 cells assessed as accumulation at G2/M phase at 1 uM measured after 72 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Synthesis and cytostatic properties of polyfunctionalized furanoallocolchicinoids. |
| AID1863115 | Induction of microtubule disruption in human SGC-7901 cells at 25 nmol/L measured after 48 hrs by DAPI staining based immunofluorescence assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway. |
| AID336341 | Cytotoxicity against human BC1 cells | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID636070 | Cell cycle arrest in mouse B16F10 cells assessed as accumulation at Go/G1 phase at 1 ug/ml after 24 hrs by flow cytometry analysis (Rvb = 70.4 %) | 2012 | Bioorganic & 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. |
| AID137219 | In vivo antitumor activity was measured in mice (P388 leukemia) at dose 0.3 mg/kg after intraperitoneal administration | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Synthesis and antitumor activity of tropolone derivatives. |
| AID1694407 | Antiproliferative activity against human LoVo cells incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
| AID665241 | Induction of mitotic arrest in human HeLa cells assessed as mitotic index measuring phosphohistone H3-positive cells by Hoechst 33342 staining | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11 | N⁴-Phenyl-substituted 2-acetylpyridine thiosemicarbazones: cytotoxicity against human tumor cells, structure-activity relationship studies and investigation on the mechanism of action. |
| AID303722 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G1 phase at 10 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID95523 | Cytotoxicity against human solid tumor nasopharyngeal carcinoma KB cell line | 1993 | Journal 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 |
| AID1860216 | Apparent permeability of the compound from apical to basolateral side in human Caco-2 cells at pH 6.5 to 7.4 | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Design and synthesis of new quinoline derivatives as selective C-RAF kinase inhibitors with potent anticancer activity. |
| AID1189595 | Depolymerization of microtubule cytoskeleton in human A549 cells assessed as aberrant mitosis at 50 nM after 24 hrs by hoechst 33342-based fluorescence microscopy | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin. |
| AID780970 | Displacement of [3H]-colchicine from biotin-labeled tubulin (unknown origin) after 2 hrs by scintillation proximity assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20 | Furanylazaindoles: potent anticancer agents in vitro and in vivo. |
| AID312976 | Growth inhibition of human SNU398 cells after 48 hrs | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high throughput screening assay. 4. Structure-activity relationships of N-alkyl substituted pyrrole fused at the 7,8-positions. |
| AID553907 | Cell cycle arrest in human Jurkat cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. |
| AID1233599 | Induction of cell cycle arrest in human M21 cells assessed as cells accumulation at subG1 phase at 24 nM after 24 hrs by flow cytometry (Rvb = 1.2%) | 2015 | European journal of medicinal chemistry, Jul-15, Volume: 100 | Styryl-N-phenyl-N'-(2-chloroethyl)ureas and styrylphenylimidazolidin-2-ones as new potent microtubule-disrupting agents using combretastatin A-4 as model. |
| AID1863086 | Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway. |
| AID1756946 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | An insight into the anticancer potential of carbamates and thiocarbamates of 10-demethoxy-10-methylaminocolchicine. |
| AID1674005 | Cytotoxicity against human PC-3 cells incubated for 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID681121 | TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
| AID1306356 | Inhibition of tubulin polymerization in human MCF7 cells assessed as alteration of interphase microtubule network at 2 uM after 24 hrs by DAPI staining-based confocal microscopic analysis | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Design, synthesis and anti-cancer activity evaluation of podophyllotoxin-norcantharidin hybrid drugs. |
| AID291503 | Cell cycle arrest in HL60 cells assessed as accumulation in S phase at 600 nM | 2007 | Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14 | Discovery of novel antitumor antimitotic agents that also reverse tumor resistance. |
| AID1179655 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2014 | Bioorganic & 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. |
| AID386623 | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. |
| AID1163574 | Antiproliferative activity against human DLD1 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Synthesis and biological evaluation of novel millepachine derivatives as a new class of tubulin polymerization inhibitors. |
| AID297425 | Inhibition of tubulin polymerization in presence of microtubule associated proteins after 30 mins | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | 4- and 5-aroylindoles as novel classes of potent antitubulin agents. |
| AID1736486 | Cell cycle arrest in human HT29 cells assessed as cell accumulation at S phase at 1 uM incubated for 24 hrs by propidium iodide staining based flow cytometry (Rvb = 20.44 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID605717 | Antiproliferative activity against mouse L1210 cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID678720 | Metabolic stability in human liver microsomes assessed as low signal/noise ratio (S/N of 1 to 10) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1435405 | Antiproliferative activity against human HepG2 cells after 48 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and cytotoxic activity of certain novel chalcone analogous compounds. |
| AID383961 | Cytotoxicity against human SNB75 cells | 2008 | Journal 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. |
| AID1384307 | Downregulation of c-Myc gene expression in human HT-29 cells assessed as c-Myc mRNA level at 10 nM after 48 hrs by RT-PCR method (Rvb = 100%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID1856345 | Inhibition of porcine Tubulin polymerization assessed as decrease in AUC fold change at 3 uM incubated for 1 hr by fluorescence microscopy | |||
| AID347991 | Cell cycle arrest in human KB/HeLa cells assessed as G2/M phase accumulation at 1 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID711167 | Cytotoxicity against human HeLa cells after 96 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24 | Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. |
| AID521220 | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 2007 | Nature chemical biology, May, Volume: 3, Issue:5 | Chemical genetics reveals a complex functional ground state of neural stem cells. |
| AID1903072 | Selectivity ratio of IC50 for human Hep3B cells to IC50 for human MCF7 cells | 2022 | Bioorganic & medicinal chemistry, 03-15, Volume: 58 | Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors. |
| AID288670 | Displacement of MTC from tubulin | 2007 | Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12 | Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies. |
| AID494506 | Antiproliferative activity against human NCI-H460 cells after 48 hrs by XTT assay | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Synthesis, antiproliferative activity and inhibition of tubulin polymerization by 1,5- and 1,8-disubstituted 10H-anthracen-9-ones bearing a 10-benzylidene or 10-(2-oxo-2-phenylethylidene) moiety. |
| AID611834 | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors. |
| AID214375 | Inhibition of [3H]colchicine binding to microtubule protein tubulin | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Biological effects of modified colchicines. Improved preparation of 2-demethylcolchicine, 3-demethylcolchicine, and (+)-colchicine and reassignment of the position of the double bond in dehydro-7-deacetamidocolchicines. |
| AID1736452 | Selectivity index, ratio of IC50 for drug resistant human MCF7 cells to IC50 for human MCF7 cells | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1420828 | Inhibition of tubulin polymerization in porcine brain assessed as disruption of tubulin assembly by spectrophotometric analysis | |||
| AID1883510 | Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID613261 | Antiproliferative activity against human KB-VIN10 cells over-expressing P-gp 170/MDR1 after 72 hrs by methylene blue assay | 2011 | European 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. |
| AID1883533 | Inhibition of porcine brain tubulin polymerization by fluorescence based assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities. |
| AID1435410 | Inhibition of tubulin beta polymerization in human HepG2 cells after 18 to 24 hrs by spectrophotometric method relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and cytotoxic activity of certain novel chalcone analogous compounds. |
| AID96173 | Inhibition of K562 cell proliferation | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24 | Novel antiproliferative agents derived from lavendustin A. |
| AID1628430 | Induction of apoptosis in human A549 cells assessed as live cells level at 40 nM incubated for 24 hrs by Annexin V-FITC/PI staining based FACS flow cytometry (Rvb = 96.83%) | 2016 | Journal 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. |
| AID132741 | Percent increase in life-span against in vivo P388 murine leukemia at a dose 0.06 mg/kg in trail 1 | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID280072 | Antiproliferative activity against drug sensitive Messa cell line by Alamar Blue assay | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5 | Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles. |
| AID100329 | In vivo antitumor activity against L1210 intraperitoneally implanted L1210 leukemia cells | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
| AID214548 | In vitro inhibition of mammalian tubulin polymerization by 50% | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors. |
| AID303715 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G2M phase at 100 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID342492 | Growth inhibition of human HT29 cells after 48 hrs by sulforhodamine B assay | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Aromatic 2-chloroethyl urea derivatives and bioisosteres. Part 2: Cytocidal activity and effects on the nuclear translocation of thioredoxin-1, and the cell cycle progression. |
| AID1382493 | Efflux ratio of apparent permeability in human Caco2 cells at 10 uM after 60 mins by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA). |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID1500634 | Antiproliferative activity against human SH-SY5Y cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of 9H-purins as potential tubulin polymerization inhibitors: Synthesis, biological evaluation and structure-activity relationships. |
| AID605770 | Antiproliferative activity against paclitaxel-resistant CHO-TAX 5-6 cells after 48 hrs by sulforhodamine B assay | 2011 | Journal 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. |
| AID1320441 | Disruption of interphase microtubule in HUVEC assessed as formation of actin stress fiber at 1 uM preincubated for 30 mins followed by compound washout measured after 120 mins by DAPI staining-based immunofluorescence assay | 2016 | Journal of medicinal chemistry, Oct-27, Volume: 59, Issue:20 | Sydnone Cycloaddition Route to Pyrazole-Based Analogs of Combretastatin A4. |
| AID1421771 | Antiproliferative activity against human HT1080 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Conformation impacts on the bioactivities of SMART analogues. |
| AID1163578 | Antiproliferative activity against human ES2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Synthesis and biological evaluation of novel millepachine derivatives as a new class of tubulin polymerization inhibitors. |
| AID744705 | Cell cycle arrest in human HeLa cells assessed as disorganized microtubules at 62 nM after 24 hrs by Hoechst 33342 staining | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Cytotoxic 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors. |
| AID1673998 | Inhibition of porcine tubulin polymerization by UV/visible spectrophotometry | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID274785 | Inhibition of tubulin polymerization in porcine brain | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | 9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID696749 | Toxicity against brine shrimp | 2012 | Journal of natural products, Nov-26, Volume: 75, Issue:11 | Meroterpenoid and diphenyl ether derivatives from Penicillium sp. MA-37, a fungus isolated from marine mangrove rhizospheric soil. |
| AID1500633 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of 9H-purins as potential tubulin polymerization inhibitors: Synthesis, biological evaluation and structure-activity relationships. |
| AID1566303 | Selectivity index, ratio of IC50 of mouse BALB/3T3 cells to IC50 of human LoVo/DX cells | |||
| AID404812 | Inhibition of tubulin polymerization at 5 uM by microplate assay | 2008 | Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12 | Aroyl hydrazones of 2-phenylindole-3-carbaldehydes as novel antimitotic agents. |
| AID1201723 | Inhibition of tubulin (unknown origin) polymerization at 10 uM | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID1507109 | Inhibition of porcine brain tubulin polymerization at 0.3 uM incubated for 5 mins by fluorimetry | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | |
| AID1677817 | Inhibition of tubulin polymerization (unknown origin) at 10 uM relative to control | 2020 | Bioorganic & medicinal chemistry, 11-01, Volume: 28, Issue:21 | New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation. |
| AID479366 | Cytotoxicity against human HL60 cells after 72 hrs MTS assay | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Phenylcinnamides as novel antimitotic agents. |
| AID1245425 | Selectivity index, ratio of IC50 for human HuDe cells to IC50 human K562 cells | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality. |
| AID680305 | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.5 uM, Colchicine: 100 uM) in MDR1-expressing NIH-3T3 cells | 2004 | Biochemical and biophysical research communications, Mar-19, Volume: 315, Issue:4 | Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. |
| AID736173 | Antiproliferative activity against human HeLa cells assessed as median dose after 24 hrs | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6 | A synthetic dolastatin 10 analogue suppresses microtubule dynamics, inhibits cell proliferation, and induces apoptotic cell death. |
| AID1527072 | Antiproliferative activity against human DLD1 cells assessed as reduction in cell viability | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
| AID1695284 | Induction of mitotic arrest in human COLO357 cells assessed as disruption of mitotic spindle arrangement at 5 uM incubated for 72 hrs by immunofluorescence based confocal microscopic analysis | 2020 | RSC medicinal chemistry, Jun-01, Volume: 11, Issue:6 | Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin. |
| AID1221978 | Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1863109 | Inhibition of porcine brain microtubule polymerization measured after 1 hrs by fluorescence based assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway. |
| AID397420 | Cytotoxicity against CHO cells assessed as chromatin condensation after 48 hrs by fluorescence microscopy | 2009 | Bioorganic & medicinal chemistry, Jun-15, Volume: 17, Issue:12 | Insecticidal heterolignans--tubuline polymerization inhibitors with activity against chewing pests. |
| AID1395589 | Effect on VEGFR2 protein expression in human HT-29 cells assessed as VEGFR2 level at 25 nM after 48 hrs by ELISA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID1674003 | Cytotoxicity against human BxPC-3 cells incubated for 48 hrs by MTT assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives. |
| AID1628412 | Inhibition of alpha tubulin polymerization in human A549 cells assessed as induction of microtubule network dis-organization at 40 nM by Immunofluorescent staining based fluorescence microscopy | 2016 | Journal 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. |
| AID333743 | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay | 2004 | Journal of natural products, Dec, Volume: 67, Issue:12 | Isomalabaricane-type compounds from the marine sponge Rhabdastrella aff. distincta. |
| AID1414060 | Fungicidal activity against Penicillium funiculosum BAM22 ATCC 11797 after 7 days by microtiter method | 2018 | MedChemComm, Oct-01, Volume: 9, Issue:10 | 7-Deacetyl-10-alkylthiocolchicine derivatives - new compounds with potent anticancer and fungicidal activity. |
| AID716402 | Induction of morphological changes in human HaCaT cells assessed as cell detachment at 10 '-6 M by confocal microscopy | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4. |
| AID1758697 | Inhibition of tubulin polymerization (unknown origin) measured every 30 secs for 90 mins | 2021 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 40 | Synthesis and structure-activity relationships of 5-phenyloxazole-2-carboxylic acid derivatives as novel inhibitors of tubulin polymerization. |
| AID404870 | Antiproliferative activity against human MCF7 cells after 72 hrs | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | New C5-alkylated indolobenzazepinones acting as inhibitors of tubulin polymerization: cytotoxic and antitumor activities. |
| AID261687 | Antiproliferative activity against NCI60 cell line | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6 | Assessment of in vitro and in vivo activities in the National Cancer Institute's anticancer screen with respect to chemical structure, target specificity, and mechanism of action. |
| AID1191359 | Inhibition of bovine brain tubulin polymerization at 10 uM measured for 1 hr by fluorescence assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and structure-activity relationships of pyridinyl-1H-1,2,3-triazolyldihydroisoxazoles as potent inhibitors of tubulin polymerization. |
| AID1203385 | Antiproliferative activity in sea urchin embryo assessed as destabilization of microtubule by measuring embryo spinning after 15 mins to 20 hrs | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | A facile synthesis and microtubule-destabilizing properties of 4-(1H-benzo[d]imidazol-2-yl)-furazan-3-amines. |
| AID1651309 | Antiarthritic activity against MSU-induced acute gout arthritis rat model assessed as degree of ankle joint swelling after 24 hrs (Rvb = 5.6 +/- 1.8 No_unit) | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Development of novel NLRP3-XOD dual inhibitors for the treatment of gout. |
| AID479354 | Cell cycle arrest in human HeLa cells by accumulation of cells at G2 phase at 100 nM after 9 hrs by propidium iodide staining based flow cytometry | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10 | Phenylcinnamides as novel antimitotic agents. |
| AID1651313 | Antiarthritic activity in rat at model of acute gout arthritis assessed as effect on MSU-induced ankle joint swelling after 24 hrs (Rvb = 5.6 +/- 1.8 No_unit) | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Development of novel NLRP3-XOD dual inhibitors for the treatment of gout. |
| AID1183705 | Inhibition of tubulin (unknown origin) polymerization incubated 15 mins prior to GTP addition by spectrophotometry | 2014 | Journal 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. |
| AID1822506 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Structure-Based Design and Synthesis of N-Substituted 3-Amino-β-Carboline Derivatives as Potent αβ-Tubulin Degradation Agents. |
| AID1875316 | Cytotoxicity in human HCT-116 cells assessed as growth inhibition level after 48 hrs by SRB assay | 2022 | Journal of natural products, 10-28, Volume: 85, Issue:10 | Resin Glycosides from |
| AID1125803 | Cytotoxicity against human KB cells after 72 hrs by methylene blue assay | 2014 | European journal of medicinal chemistry, Apr-22, Volume: 77 | Antimitotic and vascular disrupting agents: 2-hydroxy-3,4,5-trimethoxybenzophenones. |
| AID1407732 | Induction of apoptosis in human A375 cells assessed as necrotic cells at 1000 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.13%) | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1142149 | Antimigratory activity against human MDA-MB-231 cells at 0.08 uM after 17 hrs by Transwell assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach. |
| AID1201722 | Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 10 to 20 nM after 24 hrs by flow cytometric analysis | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. |
| AID612424 | Cell cycle arrest in mouse B16F10 cells assessed as accumulation at S phase at 1 ug/ml after 24 hrs by flow cytometry analysis (Rvb = 9.40%) | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16 | Synthesis, biological evaluation, and molecular modeling of cinnamic acyl sulfonamide derivatives as novel antitubulin agents. |
| AID1527075 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Recent developments on (-)-colchicine derivatives: Synthesis and structure-activity relationship. |
| AID695930 | Cytotoxicity against human HeLa cells after 48 hrs | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis and biological evaluation of a series of podophyllotoxins derivatives as a class of potent antitubulin agents. |
| AID45400 | Effect on cross resistance of CHO cells resistant to colchicine (CHRC5) | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Structure-activity relationships of antineoplastic agents in multidrug resistance. |
| AID326376 | Inhibition of tubulin polymerization in rat A10 cells after 18 hrs by indirect immunofluorescence technique | 2008 | Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5 | Docking and hydropathic scoring of polysubstituted pyrrole compounds with antitubulin activity. |
| AID1333463 | Effect on Bid gene expression in human MDA-MB-231 cells assessed as ratio of Bid to beta-actin expression level at 5 uM after 24 hrs by RT-PCR method (Rvb = 0.17 No_unit) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | 2-Azetidinones: Synthesis and biological evaluation as potential anti-breast cancer agents. |
| AID758705 | Growth inhibition of human HuDe cells after 72 hrs by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | 2-cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action. |
| AID1566315 | Cell cycle arrest in human MCF7 cells assessed as accumulation in G2 phase at 5 times of antiproliferative IC50 incubated for 48 hrs by propidium iodide based flow cytometry (Rvb = 16 %) | |||
| AID1736527 | Induction of apoptosis in human HT-29 cells assessed as early apoptotic cells at 0.25 uM measured after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.6 %) | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID617075 | Binding affinity to bovine tubulin assessed as half life of compound-tubulin complex | 2011 | Journal 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. |
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| AID287691 | Cytotoxicity against human PC3 cells after 3 days by MTT assay | 2007 | Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6 | Synthesis and biological activity of 2,5-diaryl-3-methylpyrimido[4,5-c]quinolin-1(2H)-one derivatives. |
| AID103729 | Cytotoxicity against human breast cancer cells (MCF-7) using SRB assay. | 1998 | Journal 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. |
| AID277283 | Inhibition of tubulin polymerization | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | Highly potent triazole-based tubulin polymerization inhibitors. |
| AID336352 | Antimitotic activity against rat ASK cells assessed as reversal of astrocyte morphology at 0.0064 ug/ml | 1993 | Journal of natural products, Dec, Volume: 56, Issue:12 | Novel antimitotic dibenzocyclo-octadiene lignan constituents of the stem bark of Steganotaenia araliacea. |
| AID103435 | In vivo growth inhibitory activity against human neoplastic MCF-7 cell line | 1999 | Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3 | The synthesis and evaluation of temperature sensitive tubulin toxins. |
| AID1338404 | Cell cycle arrest in human 786-0 cells assessed as accumulation at S phase at 1.25 uM after 24 hrs by propidium iodide staining-based flow cytometry (Rvb=12.6+/-0.7%) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and evaluation of novel hybrids β-carboline-4-thiazolidinones as potential antitumor and antiviral agents. |
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| AID1692984 | Inhibition of porcine brain tubulin polymerization assessed as reduction in tubulin assembly at 37 degreeC measured after 40 mins in presence of GTP by turbidimetric analysis | 2021 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 32 | 10-(4-Phenylpiperazine-1-carbonyl)acridin-9(10H)-ones and related compounds: Synthesis, antiproliferative activity and inhibition of tubulin polymerization. |
| AID310118 | Cytotoxicity against human A2780/ADR cells after 72 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23 | New functional assay of P-glycoprotein activity using Hoechst 33342. |
| AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID1906175 | Antiproliferation activity against human SiHa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay | |||
| AID1550786 | Antiproliferative activity against mouse L1210 cells measured after 96 hrs by Coulter counter method | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop. |
| AID596138 | Antiproliferative activity against human Bel7402 cells after 72 hrs by sulforhodamine B assay | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9 | Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors. |
| AID1359654 | Antiproliferative activity against human A549/TR cells after 48 to 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Discovery of novel β-carboline/acylhydrazone hybrids as potent antitumor agents and overcome drug resistance. |
| AID1238299 | Inhibition of VEGF production in human HT-29 cells assessed as VEGF level at 5 ug/ml incubated for 72 hrs by ELISA method relative to control | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Inhibitory effect of pironetin analogue/colchicine hybrids on the expression of the VEGF, hTERT and c-Myc genes. |
| AID1407714 | Antiproliferative activity against human SW480 cells after 72 hrs by MTS assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1189168 | Inhibition of tubulin polymerization (unknown origin) by DAPI staining-based fluorescence microscopy | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1771026 | Antiproliferative activity against human M14 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
| AID347996 | Cell cycle arrest in human KB/HeLa cells assessed as S phase accumulation at 10 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1535575 | Inhibition of bovine brain tubulin polymerization preincubated for 15 mins followed by GTP addition measured after 20 mins by turbidimetric method | 2019 | Bioorganic & 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. |
| AID1785091 | Cytotoxicity against human HEK293T cells expressing ABCB1 (unknown origin) measured after 72 hrs by MTT assay | |||
| AID391282 | Displacement of [3H]colchicine from tubulin by scintillation proximity assay | 2008 | Journal 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. |
| AID1384324 | Downregulation of VEGF gene expression in human HT-29 cells assessed as VEGF mRNA level at 40 nM after 48 hrs by RT-PCR method (Rvb = 100%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID1272836 | Inhibition of sheep brain tubulin polymerization by UV spectrophotometric analysis | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | New MKLP-2 inhibitors in the paprotrain series: Design, synthesis and biological evaluations. |
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| AID1569089 | Antiproliferative activity against human DU145-TxR cells | |||
| AID1639380 | Inhibition of porcine brain tubulin alpha/beta polymerization at 5 uM measured every minute for 30 mins | 2019 | Journal of natural products, 04-26, Volume: 82, Issue:4 | Parvifoline Derivatives as Tubulin Polymerization Inhibitors. |
| AID335771 | Antimitotic activity in rat ASK cells assessed as reversal of astrocyte formation at 100 ug/mL | 1993 | Journal of natural products, Oct, Volume: 56, Issue:10 | Cytotoxic constituents from Hyptis verticillata. |
| AID388962 | Toxicity in C57BL/J6 mouse assessed as liver lactate dehydrogenase level | 2008 | Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21 | Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis. |
| AID716406 | Induction of morphological changes in human SKv-a cells assessed as cell rounding at 10 '-6 M by confocal microscopy | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4. |
| AID1897646 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 12-15, Volume: 76 | Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities. |
| AID1898107 | Anti-angiogenesis activity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID132746 | Percent increase in life-span against in vivo P388 murine leukemia at a dose 0.25 mg/kg in trail 2 | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Toxicity quantitative structure--activity relationships of colchicines. |
| AID1189966 | Reduction in blood-brain barrier permeability in C57BL/6 mouse endothelial cells | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Synthesis and biological evaluation of furanoallocolchicinoids. |
| AID303720 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at G1 phase at 1 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1569052 | Inhibition of anchorage-dependent colony formation in human A375 cells assessed as decrease in colony number at 5 nM after 12 days by crystal violet-staining based assay relative to control | |||
| AID271652 | Cytotoxicity against human MKN45 cell line by methylene blue dye assay | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23 | 7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents. |
| AID296576 | Effect on thrombin-induced human platelet aggregation assessed as lag time at 0.1 uM | 2007 | Journal of medicinal chemistry, Aug-09, Volume: 50, Issue:16 | Characterization of the intracellular mechanisms involved in the antiaggregant properties of cinnamtannin B-1 from bay wood in human platelets. |
| AID595051 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2011 | Bioorganic & 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. |
| AID553913 | Cell cycle arrest in human PC3 cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis | 2011 | Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1 | Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent. |
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| AID1899070 | Resistant index, ratio IC50 for KB/VCR cells over IC50 for KB cells | |||
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| AID397290 | Cytotoxicity against human K562 cells after 72 hrs | 2009 | Journal 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. |
| AID732807 | Cytotoxicity against human BT-483 cells assessed as growth inhibition | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Design, synthesis, biological evaluation and molecular modeling studies of 1-aryl-6-(3,4,5-trimethoxyphenyl)-3(Z)-hexen-1,5-diynes as a new class of potent antitumor agents. |
| AID1821972 | Induction of cell cycle arrest in mouse B16-F10 cells assessed as accumulation of cells at G2/M phase incubated for 48 hrs by RNase/PI staining based flow cytometry analysis | |||
| AID303705 | Cell cycle arrest in KB/HeLa cells assessed as accumulation at S phase at 31.6 nM after 24 hrs by flow cytometric analysis | 2007 | Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24 | Sulfonate derivatives of naphtho[2,3-b]thiophen-4(9H)-one and 9(10H)-anthracenone as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1882710 | Anticancer activity against human HepG2 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Recent advances of antitumor shikonin/alkannin derivatives: A comprehensive overview focusing on structural classification, synthetic approaches, and mechanisms of action. |
| AID3330 | In vivo antitumor activity against 3M531 is the sarcoma M5076; reproducible minimal activity | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
| AID288694 | Growth inhibition of human HT29 cells after 48 hrs | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13 | Alkylation potency and protein specificity of aromatic urea derivatives and bioisosteres as potential irreversible antagonists of the colchicine-binding site. |
| AID1402705 | Antiproliferative activity against human MDA231 cells after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Design and characterization of α-lipoic acyl shikonin ester twin drugs as tubulin and PDK1 dual inhibitors. |
| AID1384315 | Downregulation of hTERT gene expression in human HT-29 cells assessed as hTERT mRNA level at 40 nM after 48 hrs by RT-PCR method (Rvb = 100%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID1704317 | Inhibition of tubulin assembly in human SW-620 cells assessed as induction of tubulin dissipation at 5 nM incubated for 24 hrs by Hoechst 33342 staining based confocal microscopic analysis | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Discovery of dihydrofuranoallocolchicinoids - Highly potent antimitotic agents with low acute toxicity. |
| AID1407709 | Antiproliferative activity against mouse B16F10 cells after 72 hrs by MTS assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis and characterization of potent microtubule inhibitors with dual anti-proliferative and anti-angiogenic activities. |
| AID1872844 | Cytotoxicity against human HeLa cells treated for 72 hrs by MTT assay | 2022 | European journal of medicinal chemistry, May-05, Volume: 235 | Tandem construction of biological relevant aliphatic 5-membered N-heterocycles. |
| AID1384276 | Antiproliferative activity against human A549 cells after 2 days by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives. |
| AID1435408 | Cytotoxicity against mouse AML-12 cells by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Design, synthesis and cytotoxic activity of certain novel chalcone analogous compounds. |
| AID1566310 | Cell cycle arrest in human ALL5 cells assessed as accumulation in G1 phase at 5 times of antiproliferative IC50 incubated for 72 hrs by propidium iodide based flow cytometry (Rvb = 59.7 %) | |||
| AID412961 | Growth inhibition of human Pgp170 overexpressing multidrug resistant-KB-VIN10 cells after 72 hrs by methylene blue dye assay | 2008 | Journal 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. |
| AID1898100 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 12-22, Volume: 65, Issue:24 | Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. |
| AID1736444 | Antiproliferative activity against human HT29 cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID1431295 | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID735028 | Induction of cell cycle arrest in human K562 cells assessed as accumulation of cells in S phase at 4 uM concentration after 24 hrs by propidium iodide staining based cytofluorimetric analysis (Rvb = 26.17%) | 2013 | European 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. |
| AID1063554 | Displacement of [3H]-colchicine from tubulin (unknown origin) at 20 uM preincubated for 1 hr followed by radioligand addition measured after 30 mins by competitive binding assay | 2014 | Bioorganic & medicinal chemistry, Jan-15, Volume: 22, Issue:2 | Synthesis and biological evaluation of 6H-pyrido[2',1':2,3]imidazo[4,5-c]isoquinolin-5(6H)-ones as antimitotic agents and inhibitors of tubulin polymerization. |
| AID398312 | Inhibition of tubulin polymerization | 1995 | Journal of natural products, Apr, Volume: 58, Issue:4 | Antitumor agents, 154. Cytotoxic and antimitotic flavonols from Polanisia dodecandra. |
| AID721879 | Cytotoxicity against human HCT15 cells assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay | 2013 | Journal 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. |
| AID409954 | Inhibition of mouse brain MAOA | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
| AID1389609 | Inhibition of MSU-induced MyD88 protein level in synovial homogenate of acute gouty arthritis Sprague-Dawley rat model at 10 mg/kg, po qd pretreated via gavage for 5 days followed by MSU treatment at 1 hr post last dose measured up to 24 hrs by Western bl | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. |
| AID1473726 | Cytotoxicity against human DU145-TxR cells after 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy. |
| AID404612 | Antiproliferative activity against human MDA-MB-435 cells after 72 hrs | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | New C5-alkylated indolobenzazepinones acting as inhibitors of tubulin polymerization: cytotoxic and antitumor activities. |
| AID1750229 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay | |||
| AID730204 | Antiangiogenic activity in activated HUVECs assessed as inhibition of capillary tube formation at 0.1 uM after 22 hrs by light microscopic analysis | 2013 | Journal 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. |
| AID1193492 | Thermodynamic equilibrium solubility, log S of the compound in water at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
| AID1465168 | Antiproliferative activity against human MDA-MB-468 cells by SRB assay | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | Design, synthesis and biological evaluation of 2-phenylquinoline-4-carboxamide derivatives as a new class of tubulin polymerization inhibitors. |
| AID214892 | Binding affinity towards tubulin protein measured by their ability to displace [3H]colchicine from rat brain at the dose 2.5 M | 1985 | Journal of medicinal chemistry, Sep, Volume: 28, Issue:9 | Synthesis and biological effects of novel thiocolchicines. 3. Evaluation of N-acyldeacetylthiocolchicines, N-(alkoxycarbonyl) deacetylthiocolchicines, and O-ethyldemethylthiocolchicines. New synthesis of thiodemecolcine and antileukemic effects of 2-demet |
| AID1736450 | Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-15, Volume: 190 | Synthesis and biological evaluation of novel shikonin-benzo[b]furan derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. |
| AID347995 | Cell cycle arrest in human KB/HeLa cells assessed as G1 phase accumulation at 3.16 nM after 24 hrs by FACS analysis | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | 10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization. |
| AID1202430 | Inhibition of tubulin (unknown origin) at 10 uM measured for 20 mins by turbidity method | 2015 | European journal of medicinal chemistry, , Volume: 96 | Design, synthesis, biological evaluation and preliminary mechanism study of novel benzothiazole derivatives bearing indole-based moiety as potent antitumor agents. |
| AID150755 | Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. |
| AID409675 | Cytotoxicity against african green monkey Vero cells after 48 hrs by luminescence cell viability assay | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 | Synthesis and characterization of BODIPY-labeled colchicine. |
| AID1694405 | Antiproliferative activity against human A549 cells incubated for 72 hrs by SRB assay | 2021 | Bioorganic & medicinal chemistry, 02-15, Volume: 32 | Synthesis, anticancer activity and molecular docking studies of N-deacetylthiocolchicine and 4-iodo-N-deacetylthiocolchicine derivatives. |
| AID1628409 | Inhibition of porcine brain tubulin polymerization incubated for 60 mins by fluorescence-based assay | 2016 | Journal 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. |
| AID721875 | Cytotoxicity against human MESSA cells assessed as growth inhibition after 72 hrs by Celltiter-Glo luminescent assay | 2013 | Journal 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. |
| AID1431311 | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at IC50 after 24 hrs by propidium iodide staining-based flow cytometric method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Interactions of long-chain homologues of colchicine with tubulin. |
| AID1501686 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel chemotypes targeting tubulin at the colchicine binding site and unbiasing P-glycoprotein. |
| AID1903070 | Antiproliferative activity against human HT-29 cells over expressing GLUT1 measured after 72 hrs by MTT assay | 2022 | Bioorganic & medicinal chemistry, 03-15, Volume: 58 | Design, synthesis and biological evaluation of colchicine glycoconjugates as tubulin polymerization inhibitors. |
| AID1183718 | Cytotoxicity against human MESSA/DX5 cells assessed as growth inhibition after 72 hrs by CellTitre-Glo assay | 2014 | Journal 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. |
| AID331398 | Antiproliferative activity against human MCF7 cells | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Cycloalkyl-substituted aryl chloroethylureas inhibiting cell cycle progression in G0/G1 phase and thioredoxin-1 nuclear translocation. |
| AID264021 | Inhibition of microtubule polymerization | 2006 | Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10 | Synthesis and biological evaluation of B-ring modified colchicine and isocolchicine analogs. |
| AID1732755 | Antiproliferative activity against human MIA PaCa-2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies. |
| AID1189146 | Antiproliferative activity against human A2780 cells after 48 hrs by SRB method | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15 | Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS 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. |
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS 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. |
| AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346118 | Human tubulin beta class I (Tubulins) | 2006 | Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10 | Synthesis and biological evaluation of B-ring modified colchicine and isocolchicine analogs. |
| AID1508591 | NCATS Rat Liver Microsome Stability Profiling | 2020 | Scientific reports, 11-26, Volume: 10, Issue:1 | Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models. |
| AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3 | Highly predictive and interpretable models for PAMPA permeability. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2014 | Journal of molecular biology, Apr-17, Volume: 426, Issue:8 | The novel microtubule-destabilizing drug BAL27862 binds to the colchicine site of tubulin with distinct effects on microtubule organization. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS 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. |
| AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
| AID1347411 | qHTS 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) Libary | 2020 | ACS 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. |
| AID1645871 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling in pH 5 buffer | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Using in vitro ADME data for lead compound selection: An emphasis on PAMPA pH 5 permeability and oral bioavailability. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2013 | Angewandte Chemie (International ed. in English), Dec-23, Volume: 52, Issue:52 | 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 7146 (48.84) | 18.7374 |
| 1990's | 2336 (15.97) | 18.2507 |
| 2000's | 1928 (13.18) | 29.6817 |
| 2010's | 2058 (14.07) | 24.3611 |
| 2020's | 1162 (7.94) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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 very strong demand-to-supply ratio for research on this compound.
| This Compound (109.26) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 404 (2.61%) | 5.53% |
| Reviews | 1,231 (7.96%) | 6.00% |
| Case Studies | 1,459 (9.43%) | 4.05% |
| Observational | 27 (0.17%) | 0.25% |
| Other | 12,351 (79.83%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Multicenter, Randomized, Double Blind, Placebo Controlled, Parallel Group, 1 Week, Dose Comparison Study to Evaluate the Efficacy, Safety, and Tolerability of MPC-004 in Patients With an Acute Gout Flare [NCT00506883] | Phase 3 | 185 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
| Post-Ablation Pericarditis Reduction Study [NCT04906720] | Phase 2 | 248 participants (Actual) | Interventional | 2021-05-20 | Completed | ||
| Colchicine in Patients With Heart Failure and Preserved Left Ventricular Ejection Fraction [NCT05637398] | Phase 1/Phase 2 | 40 participants (Anticipated) | Interventional | 2022-12-15 | Recruiting | ||
| An Open Non Randomized Comparative Study Exploring Drug Interaction Between Colchicine and Calcineurin Inhibitors in 2 Groups (Ciclosporin Group and Tacrolimus Group) of Renal Graft Recipients [NCT01160276] | Phase 1 | 17 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| Single-blinded Randomized Investigator-initiated Controlled Trial to Assess the Efficacy of Colchicine to Treat Patients With Cardiomyopathy With Myocarditis (Chronic Inflammatory Cardiomyopathy) [NCT06158698] | Phase 3 | 80 participants (Anticipated) | Interventional | 2023-11-14 | Recruiting | ||
| Colchicine in Postoperative Fontan Patients (CPFP) [NCT03575572] | Phase 2/Phase 3 | 11 participants (Actual) | Interventional | 2018-08-29 | Terminated(stopped due to Staffing changes impacted by COVID-19 pandemic resulting in inadequate personnel to facilitate study.) | ||
| Colchicine For The Prevention Of Perioperative Atrial Fibrillation In Patients Undergoing Thoracic Surgery (COP-AF) [NCT03310125] | Phase 3 | 3,209 participants (Actual) | Interventional | 2018-02-14 | Completed | ||
| Clinical Protocol for Administration of Topical Pentoxifylline Gel on Behcet's Disease Oral Ulcers [NCT03888846] | Phase 2 | 41 participants (Actual) | Interventional | 2019-03-25 | Completed | ||
| PET Imaging of Inflammation and Lipid Lowering Study [NCT04073797] | 63 participants (Anticipated) | Interventional | 2023-03-20 | Recruiting | |||
| Colchicine Coronavirus SARS-CoV2 Trial (COLCORONA) [NCT04322682] | Phase 3 | 4,506 participants (Actual) | Interventional | 2020-03-23 | Terminated(stopped due to Due to several considerations (logistical, human and budgetary), the study was stopped early.) | ||
| Colchicine in Periprocedural Myocardial Infarction: the Role of Alpha Defensin [NCT03735134] | 180 participants (Anticipated) | Interventional | 2018-11-30 | Not yet recruiting | |||
| Impact of Colchicine on Peri-Operative Major Adverse Cardiovascular Events in Patients With Prior Coronary Revascularization [NCT05618353] | Phase 4 | 700 participants (Anticipated) | Interventional | 2023-08-01 | Recruiting | ||
| Randomised Evaluation of COVID-19 Therapy [NCT04381936] | Phase 2/Phase 3 | 50,000 participants (Anticipated) | Interventional | 2020-03-19 | Recruiting | ||
| Effects of Standard Protocol Therapy With or Without Colchicine in Covid-19 Infection: A Randomized Double Blind Clinical Trial [NCT04360980] | Phase 2 | 80 participants (Actual) | Interventional | 2020-03-20 | Completed | ||
| The Effect of Colchicine on Inflammation in Acute Coronary Syndrome Patients [NCT06054100] | Phase 3 | 88 participants (Actual) | Interventional | 2020-02-01 | Completed | ||
| Colchicine Compared With Placebo to Reduce Hs-CRP in Patients With Acute Coronary Syndromes- Targeting Inflammation in Atherosclerosis Trial [NCT00754819] | Phase 2/Phase 3 | 80 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| Impact of Ursodeoxycholic Acid, Silymarin, Antioxidants and Colchicine on Fibrosis Regression in HCV After Achieving Sustained Virological Response [NCT03659058] | 400 participants (Actual) | Interventional | 2016-03-02 | Completed | |||
| A Translational Study to Understand the Mechanism of Apolipoprotein CIII Reduction Via Colchicine [NCT02083510] | Early Phase 1 | 5 participants (Actual) | Interventional | 2014-02-28 | Completed | ||
| Does COlchicine Improve EnDothElial Function in Non ST Elevation Myocardial Infarction Patients?: A Prospective Randomized, Double-blind Placebo Controlled Study [NCT02095522] | 0 participants (Actual) | Interventional | 2014-03-31 | Withdrawn(stopped due to The investigators did not find suiable patients) | |||
| Anti-Coronavirus Therapies to Prevent Progression of COVID-19, a Randomized Trial [NCT04324463] | Phase 3 | 6,667 participants (Actual) | Interventional | 2020-04-21 | Active, not recruiting | ||
| Diacerein Combined With Febuxostat Relieves Symptoms of Gout by Suppressing IL-1βinflammation [NCT02060552] | Phase 4 | 96 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| Revisiting the Mechanism of the Anti-inflammatory Effect of Colchicine [NCT04355585] | Phase 1 | 18 participants (Anticipated) | Interventional | 2020-05-06 | Recruiting | ||
| Study of Anti-inflammatory Treatment With Colchicine in Patients Undergoing Elective Coronary Artery Bypass Graft Surgery to Reduce Reperfusion Damage [NCT02122484] | Phase 4 | 60 participants (Actual) | Interventional | 2013-11-30 | Completed | ||
| A Single-center, Open-access Study to Evaluate Drug Interactions Between XNW3009, Febuxostat, and Colchicine in Patients With Gout [NCT05324423] | Phase 1 | 20 participants (Anticipated) | Interventional | 2021-10-18 | Recruiting | ||
| Effect of Colchicine on Inflammation and Myocardial Fibrosis Assessed by Magnetic Resonance Imaging in Patients With Chagas' Heart Disease [NCT03704181] | Phase 2 | 60 participants (Anticipated) | Interventional | 2018-10-01 | Recruiting | ||
| A One-Directional, Open-Label Drug Interaction Study to Investigate the Effects of Multiple-Dose Atorvastatin on the Single-Dose Pharmacokinetics of Colchicine in Healthy Volunteers [NCT00960323] | Phase 1 | 24 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| A Randomized Controlled Trial of Colchicine for Symptom and Inflammation Modification in Knee Osteoarthritis [NCT02176460] | Phase 2/Phase 3 | 109 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
| Cochicine Treatment for Post- Operative Pericardial Effusion: The POPE 2 Study A Multicenter, Double-blind, Randomized Trial [NCT01266694] | Phase 4 | 199 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
| Use of Colchicine to Decrease Atrial Fibrillation Recurrence After Ablation: Randomized Placebo Controlled Trial (Colchicine AF Trial) [NCT05459974] | Phase 3 | 224 participants (Anticipated) | Interventional | 2022-06-20 | Recruiting | ||
| Role of Ivermectin and Colchicine in Treatment of COVID-19: Randomized Controlled Clinical Trial [NCT05930002] | 120 participants (Actual) | Interventional | 2021-07-21 | Completed | |||
| Imaging of Inflammation in the Postischemic Myocardium: Effect of Anti-inflammatory Treatment With Colchicine [NCT02281305] | Phase 4 | 20 participants (Anticipated) | Interventional | 2014-10-31 | Recruiting | ||
| Colchicine in Patients Undergoing Coronary Artery Bypass Grafting After Acute Coronary Syndrome: an Open-label Randomized Trial [NCT05726019] | Phase 2 | 100 participants (Anticipated) | Interventional | 2022-02-05 | Recruiting | ||
| Colchicine for Reduction of Periprocedural Myocardial Injury in Percutaneous Coronary Intervention [NCT05745818] | 300 participants (Anticipated) | Observational | 2023-03-01 | Not yet recruiting | |||
| A Phase I, Single-Center, Open-Label, Single-Group Study to Evaluate Potential Pharmacodynamics of Drug-Drug Interaction Between SHR4640 and Febuxostat and Between SHR4640 and Colchicine in Patients With Gout [NCT03131583] | Phase 1 | 15 participants (Actual) | Interventional | 2017-02-17 | Completed | ||
| COLchicine and Non-enteric Coated Aspirin in the Cardiovascular Outcomes Trial of Patients With Type 2 Diabetes (COLCOT-T2D) [NCT05633810] | Phase 3 | 10,000 participants (Anticipated) | Interventional | 2022-12-21 | Recruiting | ||
| Evaluation of Efficacy of Colchicine to Prevent Skin Relapses in Adult's IgA Vasculitis [NCT04008316] | Phase 3 | 264 participants (Anticipated) | Interventional | 2019-11-12 | Recruiting | ||
| Impact of Colchicine Therapy on Arrhythmia Recurrence After Acute Pericardial Effusion Following Catheter Ablation of Atrial Fibrillation [NCT02260206] | Phase 4 | 170 participants (Anticipated) | Interventional | 2014-07-31 | Recruiting | ||
| Safety and Efficacy of Low Dose Colchicine or Prednisone Combining With Standard Drug in Patients With Recurrent In-stent Restenosis: a Prospective, Randomized, Open-label Trial [NCT06090890] | Phase 4 | 252 participants (Anticipated) | Interventional | 2023-10-30 | Not yet recruiting | ||
| Treat-to-Target Serum Urate Versus Treat-to-Avoid Symptoms in Gout: A Randomized Controlled Trial [NCT04875702] | 650 participants (Anticipated) | Interventional | 2023-11-15 | Not yet recruiting | |||
| Colchicine After Electrocardioversion for Atrial Fibrillation - The COLECTRO-AF Trial [NCT05890664] | Phase 3 | 416 participants (Anticipated) | Interventional | 2023-10-31 | Not yet recruiting | ||
| Effect of Low Dose of Colchicine on Platelet Reactivty in Patients With Chronic Coronary Disease [NCT05956145] | Phase 3 | 80 participants (Anticipated) | Interventional | 2021-06-17 | Recruiting | ||
| COLSIO Trial: Phase II Randomized, Controlled Trial of Colchicine to Suppress Inflammation and Improve Insulin Resistance in Adults and Adolescents With Obesity [NCT05017571] | Phase 2 | 500 participants (Anticipated) | Interventional | 2021-11-08 | Recruiting | ||
| Adjuvant Use Of Colchicine With The Standard Therapy In Moderate And Severe Corona Virus Disease-19 Infection: Randomized Controlled Clinical Trial [NCT05151614] | Phase 1 | 160 participants (Actual) | Interventional | 2021-04-01 | Completed | ||
| A Phase 2B Study to Evaluate the Efficacy and Safety in Combination With Standard of Care in Adult Subjects With Gout, and Hyperuricemia Refractory to Conventional XOI Therapy [NCT05690204] | Phase 2 | 80 participants (Anticipated) | Interventional | 2022-12-12 | Recruiting | ||
| A Phase IV, Randomized, Double-Blind, Placebo-Controlled, Single-Center Study of the Effects of Colchicine on Pain and Inflammation in Subjects With Knee Osteoarthritis [NCT03913442] | Phase 4 | 120 participants (Anticipated) | Interventional | 2019-05-15 | Recruiting | ||
| A Phase 2, Open-label Study to Evaluate the Safety and Efficacy of Arhalofenate (MBX-102) in Combination With Febuxostat for the Treatment of Hyperuricemia in Patients With Gout [NCT01416402] | Phase 2 | 27 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
| A Phase 2 Randomized Double-Blind Placebo-Controlled Study to Evaluate the Safety and Efficacy of MBX-102 in the Treatment of Hyperuricemia in Patients With Gout [NCT01336686] | Phase 2 | 67 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
| Targeting Inflammation in Atrial Fibrillation to Prevent Ischemic Stroke: A Feasibility Study Evaluating the Effect of Colchicine on D-dimer and Hs-CRP in Anticoagulated Patients With Atrial Fibrillation [NCT02282098] | Phase 3 | 80 participants (Actual) | Interventional | 2014-11-30 | Completed | ||
| Pilot Study to Evaluate the Efficacy of Low Dose Colchicine (LoDoCo ®) to Improve Exercise Capacity Among Patients With Chronic Stable HFpEF and Systemic Inflammation [NCT06130059] | Phase 2 | 60 participants (Anticipated) | Interventional | 2024-03-15 | Not yet recruiting | ||
| Polygenic Risk-based Detection of Subclinical Coronary Atherosclerosis and Intervention With Statin and Colchicine [NCT05850091] | Phase 4 | 200 participants (Anticipated) | Interventional | 2023-11-30 | Recruiting | ||
| Colchicine Effect on Perivascular Inflammation Index on Coronary CTA(COPIX Trial) [NCT05347316] | Phase 1 | 40 participants (Anticipated) | Interventional | 2022-03-07 | Recruiting | ||
| On-admission Low-dose Colchicine in Addition to Atorvastatin to Reduce Inflammation in Acute Coronary Syndrome [NCT05250596] | Phase 2 | 175 participants (Anticipated) | Interventional | 2022-02-24 | Recruiting | ||
| Study Of Colchicine Resistance In Familial Mediterranean Fever [NCT05418686] | 30 participants (Anticipated) | Interventional | 2022-07-31 | Not yet recruiting | |||
| Impact of Colchicine and Low-dose Naltrexone on COVID-19 Disease Progression and Clinical Course in Hospitalized Patients [NCT04756128] | Phase 2 | 142 participants (Actual) | Interventional | 2021-01-25 | Completed | ||
| Preoperative Colchicine, Dronedarone Or Amiodarone for Prophylaxis Against Postoperative Atrial Fibrillation in Patients Undergoing On-pump CABG; A Comparative Study [NCT03905759] | Phase 2/Phase 3 | 48 participants (Anticipated) | Interventional | 2019-04-03 | Recruiting | ||
| [NCT01173107] | Phase 4 | 80 participants (Anticipated) | Interventional | 2010-12-31 | Completed | ||
| COLchicine and Thiamine in Heart Failure Due to Ischemic Heart Disease [NCT05873881] | Phase 3 | 2,500 participants (Anticipated) | Interventional | 2023-11-30 | Not yet recruiting | ||
| Atrial Fibrillation Recurrence Following Cardioversion: the Role of Clinical Factors and Alpha Defensin Levels [NCT04155879] | 300 participants (Anticipated) | Interventional | 2019-11-30 | Not yet recruiting | |||
| Colchicine/Statins for the Prevention of COVID-19 Complications (COLSTAT) Trial [NCT04472611] | Phase 3 | 250 participants (Actual) | Interventional | 2020-10-30 | Completed | ||
| Colchicine for Acute Coronary Syndromes. A Multicenter Double Blind Randomized Trial. [NCT01906749] | Phase 4 | 500 participants (Anticipated) | Interventional | 2013-06-30 | Recruiting | ||
| A Randomized, Double-blind, Placebo-controlled Study to Evaluate the Effects of Colchicine on Vascular Inflammation as Assessed With Position Emission Tomography (PET) Imaging in Patients With Atherosclerotic Vascular Disease (COLPET) [NCT02162303] | Phase 2 | 106 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| Colchicine to Suppress Pro-tumorigenic Inflammation in Patients With Urothelial Cancer and Other Solid Tumors [NCT05279690] | Phase 1 | 45 participants (Anticipated) | Interventional | 2022-02-14 | Recruiting | ||
| Low-dose Colchicine With or Without Stepwise Dose Titration of Febuxostat for Flare Prophylaxis in Patients With Gout and Hyperuricemia During the Initial Phase of Urate-lowering Therapy: an Open-label Randomized Controlled Trial [NCT04697602] | 21 participants (Actual) | Interventional | 2021-01-20 | Terminated(stopped due to Slow recruitment) | |||
| COHERENT - The COlchicine HypERtENsion Trial [NCT04916522] | Phase 2 | 150 participants (Anticipated) | Interventional | 2021-08-10 | Recruiting | ||
| The Effect of Colchicine Treatment on the Progression of Proteinuria in Patients With Diabetic Nephropathy. [NCT02442921] | Phase 1/Phase 2 | 40 participants (Anticipated) | Interventional | 2016-02-22 | Recruiting | ||
| Effectiveness of Colchicine Among Patients With COVID-19 Infection [NCT04867226] | Phase 2 | 100 participants (Actual) | Interventional | 2021-05-08 | Completed | ||
| Double-blind, Placebo-controlled Clinical Trial of the Use of Colchicine for the Management of Patients With Mild and Severe SARS-Cov2 Infection [NCT04367168] | Phase 2 | 116 participants (Actual) | Interventional | 2020-05-27 | Terminated(stopped due to The intervention was not effective for the outcomes) | ||
| Controlled Ceasing of Colchicine Therapy in Familial Mediterranean Fever (FMF) Patients With Single MEFV (Mediterranean Fever) Gene Mutation [NCT02175589] | Phase 2 | 80 participants (Anticipated) | Interventional | 2014-06-30 | Enrolling by invitation | ||
| Colchicine for Patients With Aortic Stenosis Undergoing Transcatheter Aortic Valve Replacement (Co-STAR): a Randomized-controlled Trial [NCT04870424] | Phase 3 | 200 participants (Anticipated) | Interventional | 2021-09-21 | Recruiting | ||
| Repurposing Colchicine for Reduction of Residual Inflammatory Risk in Type 1 Diabetes: A Randomized, Double-blind, Placebo-controlled, Investigator-initiated Trial [NCT05949281] | Phase 2 | 100 participants (Anticipated) | Interventional | 2023-08-29 | Recruiting | ||
| Effect of Colchicine on Coronary Reperfusion in Patients With Acute Coronary Syndrome [NCT05472337] | Phase 2 | 50 participants (Anticipated) | Interventional | 2022-08-01 | Recruiting | ||
| A 2x2 Factorial Randomized Controlled Trial of Colchicine and Spironolactone in Patients With Myocardial Infarction / SYNERGY Stent Registry - Organization to Assess Strategies for Ischemic Syndromes 9 [NCT03048825] | Phase 3 | 7,063 participants (Actual) | Interventional | 2018-02-01 | Active, not recruiting | ||
| Colchicine Use in Intracranial Atherosclerotic Disease - a Pilot Open-labelled Randomized Trial [NCT05503225] | Phase 2 | 72 participants (Anticipated) | Interventional | 2022-11-28 | Recruiting | ||
| Low-dose Colchicine Intervention in Patients With Type 2 Diabetes Mellitus and Microalbuminuria: Chongqing Study [NCT02035891] | 160 participants (Actual) | Interventional | 2013-12-31 | Active, not recruiting | |||
| Colchicine in Belgium in Patients With Coronary Artery Disease [NCT06095765] | Phase 3 | 2,770 participants (Anticipated) | Interventional | 2024-02-01 | Not yet recruiting | ||
| Efficacy and Safety of a Fixed Combination (Thiocolchicoside 8 mg + Ketoprofen 100 mg ) Compared to Thiocolchicoside 8 mg Administered Twice a Day for 7 Days in Patients Suffering From Acute Non Specific Low Back Pain [NCT00679146] | Phase 3 | 334 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| Pharmacokinetics, Pharmacodynamics, and Safety Profile of Understudied Drugs [NCT04278404] | 5,000 participants (Anticipated) | Observational | 2020-03-05 | Recruiting | |||
| Colchicine Treatment for Chronic Shoulder Pain Related to Calcific Tendonitis: Double Blind Placebo-controlled Study [NCT00983177] | 80 participants (Anticipated) | Interventional | 2010-03-31 | Recruiting | |||
| Aspirin-free Therapy After Successful Percutaneous Coronary Intervention for Acute Coronary Syndrome: the MACT (Mono Antiplatelet and Colchicine Therapy) Pilot Study [NCT04949516] | Phase 4 | 200 participants (Actual) | Interventional | 2021-06-15 | Completed | ||
| A 24-week, Dose-ranging, Multicenter, Double-blind, Double-dummy, Active-controlled Core Study to Evaluate Canakinumab for Prophylaxis of Signs and Symptoms of Acute Flares in Chronic Gout Patients Initiating Allopurinol Therapy and a 24-week Open-label, [NCT00819585] | Phase 2 | 432 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| The Comparison of the Efficacy of Once and Twice Daily Colchicine Dosage in Pediatric Patients With Familial Mediterranean Fever: A Randomized Trial [NCT02602028] | Phase 4 | 79 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
| Colchicine for the Prevention of Atrial Fibrillation Recurrence After Electrical Cardioversion of Persistent Atrial Fibrillation. [NCT02582190] | Phase 3 | 0 participants (Actual) | Interventional | 2017-12-02 | Withdrawn(stopped due to Investigational Medicinal Product Supplies) | ||
| A Randomized Multicenter Study for Isolated Skin Vasculitis [NCT02939573] | Phase 2 | 90 participants (Anticipated) | Interventional | 2017-01-01 | Recruiting | ||
| Efficacy of Atorvastatin vs Colchicine in Decrease of Troponin I of High Sensitivity as a Biomarker of Myocardial Damage in Patients With Rheumatoid Arthritis With Severe Activity. [NCT04056039] | Phase 2 | 60 participants (Actual) | Interventional | 2018-08-14 | Completed | ||
| Colchicine or Prednisone for the Treatment of Acute Calcium Pyrophosphate Deposition (CPPD) Arthritis: Open-label, Randomized, Multicenter, Equivalence Trial of Efficacy and Safety [NCT03128905] | Phase 3 | 111 participants (Actual) | Interventional | 2018-02-05 | Completed | ||
| Outcomes of Low-dose Colchicine in Patients With Myocardial Infarction: A Randomized Controlled Trial [NCT04218786] | Phase 2 | 0 participants (Actual) | Interventional | 2025-12-31 | Withdrawn(stopped due to Due to the pandemic, there were logistical issues in continuing the study.) | ||
| Colchicine in Circulating Inflammatory Markers After Stroke [NCT06062277] | Phase 2 | 91 participants (Anticipated) | Interventional | 2023-10-31 | Not yet recruiting | ||
| Withdrawal of Colchicine in Behçet Syndrome Patients With Skin and Mucosa Involvement [NCT06146192] | 130 participants (Anticipated) | Observational | 2023-11-20 | Not yet recruiting | |||
| Colchicine Versus Placebo in Acute Myocarditis Patients to Reduce Late Gadolinium Enhancement Mass on Cardiac Magnetic Resonance and the Risk of Clinical Outcomes: The ARGO Trial [NCT05855746] | Phase 3 | 300 participants (Anticipated) | Interventional | 2024-01-22 | Not yet recruiting | ||
| Shifting the Paradigm of Gout: An Assessment of Chronic Synovial-Based Inflammation and Its Role With Serum Urate Levels. [NCT01112982] | Phase 4 | 74 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| A Pilot Bioavailability Study of Colcrys® Tablet 0.6 mg Versus Colcrys® Tablets 0.6 mg Crushed and Sprinkled on Applesauce Under Fasting Conditions [NCT01130051] | Phase 1 | 16 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| Phase II Trial of Long-term Monotherapy With Ribavirin Against Colchicine on Progression of Chronic Hepatitis C With Advanced Fibrosis in Patients With Non-response to Standard Antiviral Therapy [NCT00840489] | Phase 2 | 50 participants (Actual) | Interventional | 2009-01-31 | Terminated(stopped due to Preliminary analysis) | ||
| Randomized, 3-Way Crossover Bioequivalence Study of Single Dose Colchicine Tablets and Effect of Food [NCT01021020] | Phase 1 | 28 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
| Clinical Outcome of Patients With COVID-19 Pneumonia Treated With Corticosteroids and Colchicine in Colombia [NCT04654416] | 301 participants (Actual) | Observational | 2020-03-20 | Completed | |||
| Efficacy and Safety of Residual Inflammatory Risk-Guided Low-dose Colchicine Therapy in Elderly Patients With Multivessel Coronary Artery Disease: A Multicenter Randomized Controlled Trial [NCT06025071] | Phase 4 | 800 participants (Anticipated) | Interventional | 2023-09-30 | Not yet recruiting | ||
| A Single-center Clinical Trial to Evaluate the Efficacy and Safety of Colchicine Combined With Conventional Therapy in Multiple Myeloma Patients [NCT05802992] | Phase 3 | 30 participants (Anticipated) | Interventional | 2022-03-30 | Recruiting | ||
| The Effect of Colchicine on Food-related Effort-based Decision Making in Brain and Behaviour in Overweight and Obesity: the FLAIR-i Study [NCT05785429] | 60 participants (Anticipated) | Interventional | 2022-08-02 | Recruiting | |||
| An Open-label, Parallel-group, Multiple-Dose, Pharmacokinetic and Safety Study of Colchicine Pediatric Formulation in Pediatric and Adult Patients With FMF [NCT01075906] | Phase 1 | 75 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
| Study of Anti-inflammatory Treatment With Colchicine in the Acute Phase of ST-elevation Myocardial Infarction to Reduce Infarct Size [NCT01936285] | Phase 4 | 150 participants (Anticipated) | Interventional | 2013-07-31 | Recruiting | ||
| Evaluation the Palliative Effects of Colchicine on Primary Hepatic Malignant Tumors Unable to Receive Curative Treatment [NCT04264260] | Phase 2 | 80 participants (Anticipated) | Interventional | 2019-12-24 | Recruiting | ||
| A One-Directional, Open-Label Drug-Food Interaction Study to Investigate the Effects of Multiple-Daily Consumptions of Seville Orange Juice on the Single-Dose Pharmacokinetics of Colchicine in Healthy Volunteers [NCT00960193] | Phase 1 | 24 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| The ECLA PHRI COLCOVID Trial [NCT04328480] | Phase 3 | 1,279 participants (Actual) | Interventional | 2020-04-17 | Completed | ||
| Low Dose ColchicinE in pAtients With Peripheral Artery DiseasE to Address Residual Vascular Risk: A Randomized Trial (Vanguard Phase) [NCT04774159] | Phase 3 | 150 participants (Anticipated) | Interventional | 2021-05-06 | Recruiting | ||
| Randomized, Double-blinded, Placebo-controlled Study of the Efficacy and Safety of DYV700 for Reducing Pain Associated With an Acute Gout Flare [NCT04130204] | Phase 2 | 284 participants (Actual) | Interventional | 2020-02-12 | Completed | ||
| Evaluation of Therapeutic Effect of 0.5 mg Colchicine and 5 mg Prednisolone on Oral Aphthae [NCT00723268] | Phase 2 | 30 participants (Anticipated) | Interventional | 2007-05-31 | Active, not recruiting | ||
| Colchicine for Diabetic Nephropathy [NCT01005121] | Phase 2 | 12 participants (Anticipated) | Interventional | 2009-12-31 | Recruiting | ||
| A Double Blind Cross Over Clinical Trial to Determine Colchicine Efficacy in Behcet's Disease [NCT00700297] | Phase 2 | 169 participants (Actual) | Interventional | 2002-08-31 | Completed | ||
| Colchicine Protective Effect in Patients Undergoing Elective Percutaneous Coronary Intervention (COLCHICINE-PROTECT) A Randomized, Placebo-controlled, Double-blind Clinical Trial [NCT05739929] | Phase 3 | 400 participants (Anticipated) | Interventional | 2023-03-01 | Recruiting | ||
| Impact of Colchicine in Hospitalized Colombian Patients With COVID-19 [NCT04539873] | Phase 3 | 128 participants (Actual) | Interventional | 2021-04-30 | Terminated(stopped due to non-inclusion of patients in the study effectively) | ||
| Evaluate the Safety of Colchicine for Treatment and Prevention of Radiation-Induced Dermatitis [NCT05335148] | Phase 1 | 30 participants (Anticipated) | Interventional | 2022-05-10 | Recruiting | ||
| A Phase 2, Open-label, Drug-Drug Interaction Study to Evaluate the Pharmacodynamics, Pharmacokinetics, and Safety of Arhalofenate in Combination With Febuxostat for the Treatment of Hyperuricemia in Patients With Gout [NCT02252835] | Phase 2 | 32 participants (Actual) | Interventional | 2014-08-31 | Completed | ||
| Randomized, Open-Label, Controlled Trial of Colchicine to Reduce Cardiac Injury in Hospitalized COVID-19 (Coronavirus Disease 2019) Patients (COLHEART-19) [NCT04355143] | Phase 2 | 93 participants (Actual) | Interventional | 2020-05-01 | Completed | ||
| Effect of Colchicine in Regulating MMP-9, NOX-2, and TGF- β1 After Myocardial Infraction in Stable Patients [NCT05709509] | Phase 4 | 148 participants (Anticipated) | Interventional | 2022-06-01 | Recruiting | ||
| Treatment With COLchicine of Patients Affected by COVID-19: a Pilot Study [NCT04375202] | Phase 2 | 227 participants (Actual) | Interventional | 2020-04-18 | Terminated(stopped due to Insufficient rate of patient accrual and newly available scientific evidence) | ||
| Impact of Colchicine on the Clinical Outcome of COVID-19 and the Development of Post-COVID-19 Pulmonary Fibrosis: Randomized Controlled Clinical Trial [NCT04818489] | Phase 4 | 260 participants (Actual) | Interventional | 2021-03-25 | Active, not recruiting | ||
| Colchicine to Counteract Inflammatory Response in COVID-19 Pneumonia [NCT04322565] | Phase 2 | 193 participants (Actual) | Interventional | 2020-04-20 | Completed | ||
| The Efficacy and Safety of Colchicine in Improving the Stability of Coronary Plaque in Patients With Acute Coronary Syndrome [NCT04848857] | Phase 4 | 128 participants (Actual) | Interventional | 2021-05-03 | Completed | ||
| Treatment and Prevention of Pericarditis With Colchicine. A Multicenter Double Blind Randomized Trial. The COPPS Trial: COlchicine for the Prevention of Postpericardiotomy Syndrome [NCT00128427] | Phase 3 | 360 participants (Anticipated) | Interventional | 2005-06-30 | Completed | ||
| Treatment and Prevention of Pericarditis With Colchicine. A Multicenter Double Blind Randomized Trial. The ICAP Trial: Investigation on Colchicine for Acute Pericarditis [NCT00128453] | Phase 3 | 240 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
| A One-Directional, Open-Label Drug Interaction Study to Investigate the Effects of Multiple-Dose Diltiazem ER on Single-Dose Pharmacokinetics of Colchicine in Healthy Volunteers [NCT00983372] | Phase 1 | 24 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
| Effect of Colchicine on Range of Motion After Manipulation Under Anesthesia for the Stiff Total Knee Replacement: A Prospective Randomized Controlled Trial [NCT02926248] | Phase 4 | 112 participants (Anticipated) | Interventional | 2016-05-31 | Suspended(stopped due to Continuing IRB review was not submitted. Study was inactivated with the institutional IRB.) | ||
| The GReek Study in the Effects of Colchicine in Covid-19 cOmplications Prevention [NCT04326790] | Phase 2 | 105 participants (Actual) | Interventional | 2020-04-03 | Terminated(stopped due to Slow enrollment as a result of the rapid flattening of the curve of COVID-19 cases in Greece) | ||
| A Randomized, Double-Blind, Active and Placebo-Controlled Study to Evaluate the Efficacy and Safety of Arhalofenate for Preventing Flares and Reducing Serum Uric Acid in Gout Patients [NCT02063997] | Phase 2 | 248 participants (Actual) | Interventional | 2014-03-31 | Completed | ||
| A Pharmacokinetic Study to Evaluate the Effect of Clarithromycin on the Pharmacokinetic Profile of Colchicine in Healthy Adults [NCT00984061] | Phase 1 | 24 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| A One-Directional, Open-Label, Drug Interaction Study to Investigate the Effects of Multiple-Dose Colchicine on Single-Dose Pharmacokinetics of Theophylline in Healthy Volunteers [NCT00983905] | Phase 1 | 30 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
| A One-Directional, Open-label Drug Interaction Study to Investigate the Effects of Multiple-Dose Ritonavir on Single-Dose Pharmacokinetics of Colchicine in Healthy Volunteers [NCT00983515] | Phase 1 | 24 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| Colchicine Has Anti-diabetic Effect and May be an Option for Type 2 Diabetes Management [NCT04377321] | 150 participants (Actual) | Observational [Patient Registry] | 2019-10-10 | Completed | |||
| An Open Label, Two Period, Sequential, Single Dose and Multiple Dose Pharmacokinetic Study With 0.6mg Colchicine Tablets in Healthy Volunteers [NCT01017003] | Phase 1 | 14 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
| Studies on the Effects of Colchicine on Neutrophil Biology in Acute Myocardial Infarction: A Substudy of the CLEAR SYNERGY (OASIS 9) Trial [NCT03874338] | 670 participants (Anticipated) | Observational | 2019-03-04 | Recruiting | |||
| [NCT00004368] | Phase 1 | 15 participants | Interventional | 1990-05-31 | Active, not recruiting | ||
| Mechanistic Effects of Colchicine in Patients With Myocardial Infarction A Single Center Phase 4 Single Arm Open-label Study Evaluating the FDA-approved Drug, Colchicine, at the FDA-approved Gout Dose in Patients With Myocardial Infarction [NCT02995512] | Phase 4 | 0 participants (Actual) | Interventional | 2017-05-01 | Withdrawn(stopped due to feasibility) | ||
| Phase II Trial of Oral Colchicine in Men With Castrate-Resistant Prostate Cancer Who Have Failed Taxotere-Based Chemotherapy [NCT01481233] | Phase 2 | 0 participants (Actual) | Interventional | 2013-05-31 | Withdrawn(stopped due to Due to funding) | ||
| Colchicine Use for Primary Prevention in People at High Risk of Coronary Artery Disease [NCT05175274] | Phase 3 | 6,792 participants (Anticipated) | Interventional | 2022-12-06 | Not yet recruiting | ||
| Administration of Colchicine Plus Standard Treatment vs. Standard Therapy, in Hospitalized Patients With COVID-19, Within the First 48 Hours, and no Severity Criteria. [NCT04350320] | Phase 3 | 102 participants (Actual) | Interventional | 2020-04-30 | Completed | ||
| A Biomarker Study Assessing the Effects of Colchicine on Inflammation and Extra-Cellular Matrix Turnover in Patients With Heart Failure and Preserved Ejection Fraction. [NCT04857931] | Phase 2 | 14 participants (Actual) | Interventional | 2022-06-17 | Terminated(stopped due to Lack of funds to support opening of new sites to help patient recruitment, which was found to be more challenging than initially expected.) | ||
| The Effects of Different Doses of Colchicine on High-sensitivity C-reactive Protein in Patients After Percutaneous Coronary Intervention [NCT06078904] | Phase 4 | 200 participants (Anticipated) | Interventional | 2023-10-10 | Recruiting | ||
| Relative Bioavailability of Colcrys™ (Colchicine, USP) 0.6 mg Tablets in Healthy Young and Elderly Volunteers Under Fasted Conditions [NCT01001052] | Phase 1 | 38 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
| Open-Label Pharmacokinetic Study of a Low-Dose Acute Gout Regimen [NCT01017042] | Phase 1 | 13 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
| Single-Dose, Open-Label Study of the Pharmacokinetics, Safety, and Tolerability of Colcrys (Colchicine, USP) Tablets 0.6 mg Administered to Healthy Subjects and Subjects With Mild, Moderate, Severe Renal Impairment, and End-Stage Renal Disease [NCT01084278] | Phase 4 | 40 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| A Phase 2 Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Safety and Efficacy of MBX-102 in Combination With Allopurinol in Gout Patients With an Inadequate Hypouricemic Response to Allopurinol Alone [NCT01399008] | Phase 2 | 100 participants (Actual) | Interventional | 2011-06-30 | Completed | ||
| A Randomized, Open Lable, Multi-center, Active Competitor Phase 2 Study for Evaluating Efficacy and Safety of Genakumab for Injection as First Line Therapy in Patients With Gout Flare [NCT05936268] | Phase 2 | 106 participants (Anticipated) | Interventional | 2023-06-30 | Recruiting | ||
| A Pilot Bioavailability Study of Colcrys® Tablet 0.6 mg Versus Colcrys® Tablet 0.6 mg Crushed and Dissolved in Apple Juice Under Fasting Conditions [NCT01123395] | Phase 1 | 16 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| A Pharmacokinetic Study to Evaluate the Effect of Colchicine on the Pharmacokinetic Profile of an Oral Contraceptive Containing Ethinyl Estradiol and Norethindrone in Healthy Women [NCT01040845] | Phase 1 | 30 participants (Actual) | Interventional | 2007-08-31 | Completed | ||
| COlchicine for Prevention of the Post-pericardiotomy Syndrome and Post-operative Atrial Fibrillation (COPPS-2 Trial). [NCT01552187] | Phase 3 | 360 participants (Anticipated) | Interventional | 2012-03-31 | Active, not recruiting | ||
| Colchicine for Amyotrophic Lateral Sclerosis: a Phase II, Randomized, Double Blind, Placebo Controlled, Multicenter Clinical Trial [NCT03693781] | Phase 2 | 54 participants (Actual) | Interventional | 2019-04-10 | Completed | ||
| Treatment and Prevention of Pericarditis With Colchicine. A Multicenter Double Blind Randomized Trial. The CORP Trial: COlchicine for Recurrent Pericarditis [NCT00128414] | Phase 3 | 120 participants (Anticipated) | Interventional | 2005-08-31 | Completed | ||
| An IIT, Randomized, Single-Center, Open-Lable, Standard Therapy Controlled Study to Evaluate the Efficacy and Safety of Colchicine Tablets in Patients With COVID-19 [NCT05038449] | 60 participants (Anticipated) | Interventional | 2021-09-06 | Not yet recruiting | |||
| Randomized Double-blind Trial to Study the Benefit of Colchicine in Patients With Acutely Decompensated Heart Failure [NCT04705987] | Phase 3 | 278 participants (Anticipated) | Interventional | 2021-02-08 | Recruiting | ||
| Pragmatic, Randomized, Multicenter, Double-blind, Controlled, Clinical Trial of Prednisolone Versus Colchicine for Acute Gout in Primary Care [NCT05698680] | Phase 4 | 314 participants (Anticipated) | Interventional | 2023-01-18 | Recruiting | ||
| Anti-Inflammatory Treatment of Uremic Cardiomyopathy With Colchicine [NCT04500665] | Phase 2 | 20 participants (Anticipated) | Interventional | 2021-11-01 | Recruiting | ||
| Pilot Study of the Effects of Colchicine in Non-Diabetic Adults With Metabolic Syndrome [NCT02153983] | Phase 1/Phase 2 | 77 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| Short Course Low Dose Oral Colchicine After ST Elevation Myocardial Infarction(STEMI) [NCT06020300] | Phase 4 | 64 participants (Anticipated) | Interventional | 2023-07-28 | Recruiting | ||
| Efficacy and Safety of Hydroxychloroquine in Colchicine-RESistant Glucocorticoid-DependenT IdiOpathic REcurrent Pericarditis: A Randomized Clinical Trial (The RESTORE Randomized Clinical Trial) [NCT05737680] | Phase 3 | 30 participants (Anticipated) | Interventional | 2023-02-28 | Not yet recruiting | ||
| The Colchicine and Atrial Fibrillation Trial [NCT05928728] | Phase 3 | 500 participants (Anticipated) | Interventional | 2023-07-01 | Not yet recruiting | ||
| A Randomized, Double-blind, Placebo-controlled Phase II Trial to Evaluate the Dose-dependent Effect of Colchicine on Inflammatory Response and Endothelial Function in Type 2 Diabetic Patients With Coronary Artery Disease and Leukocyte Activation [NCT03376698] | Phase 2 | 54 participants (Actual) | Interventional | 2017-06-15 | Completed | ||
| Phase IV Study of Long Term Peg-Intron for Patients Who Have Failed to Respond to Rebetron/Interferon With Advanced Fibrosis and Cirrhosis Secondary to Hepatitis C- The Copilot Trial [NCT00179413] | Phase 4 | 549 participants (Actual) | Interventional | 2000-01-15 | Completed | ||
| Treatment and Prevention of Pericarditis With Colchicine. A Multicenter Double Blind Randomized Trial. The CORP 2 Trial: COlchicine for Recurrent Pericarditis. [NCT00235079] | Phase 4 | 240 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
| Colchicine in Moderate Symptomatic COVID-19 Patients: Double Blind, Randomized, Placebo Controlled Trial to Observe the Efficacy [NCT04527562] | 299 participants (Actual) | Interventional | 2020-07-14 | Completed | |||
| Oral Colchicine in Argentina (ORCA Trial) for the Prevention of Adverse Events After Percutaneous Coronary Interventions [NCT04382443] | Phase 4 | 450 participants (Anticipated) | Interventional | 2020-03-12 | Recruiting | ||
| A RANDOMIZED, MULTICENTRE PHASE IIa OPEN-LABEL, ACTIVE-COMPARATOR TRIAL TO ASSESS THE EFFICACY AND SAFETY OF TWO REGIMENS OF BUCILLAMINE 100 MG TABLETS AS COMPARED TO COLCHICINE 0.6 MG TABLETS FOR THE TREATMENT OF AN ACUTE GOUT FLARE IN SUBJECTS WITH MODE [NCT02330796] | Phase 2 | 66 participants (Actual) | Interventional | 2015-04-30 | Completed | ||
| COLchicine to Prevent Sympathetic Denervation After an Acute Myocardial Infarction [NCT04420624] | Phase 2/Phase 3 | 54 participants (Actual) | Interventional | 2020-12-04 | Terminated(stopped due to Inclusion period completed) | ||
| Study to Investigate the Treatment Effect of Colchicine in Patients With COVID-19 [NCT04667780] | Phase 3 | 102 participants (Actual) | Interventional | 2020-12-01 | Completed | ||
| Anti-inflammatory Therapy During Percutaneous Coronary Intervention [NCT02594111] | Phase 4 | 714 participants (Actual) | Interventional | 2013-05-30 | Completed | ||
| A Phase 4, Study to Evaluate the Safety and Efficacy of Lesinurad 200 mg in Combination With a Xanthine Oxidase Inhibitor (XOI), Compared With an XOI Alone, in Subjects With Gout and Estimated Creatinine Clearance (eCrCl) 30 to <60 mL/Min Who Have Not Ach [NCT03226899] | Phase 4 | 242 participants (Actual) | Interventional | 2017-07-19 | Terminated(stopped due to This action was a business decision & not related to any efficacy, safety or clinical concerns with lesinurad.) | ||
| Application of Colchicine Plus Herbal Phenolic Monoterpene Fractions to Treat COVID-19 [NCT04392141] | Phase 1/Phase 2 | 120 participants (Actual) | Interventional | 2020-04-01 | Completed | ||
| Prospective-randomized Adaptive Study, With Active Control to Evaluate the Efficacy and Safety of Interleukin (IL)-17 Inhibitor Treatment Versus Low Doses of IL-2 Versus Indirect IL-6 Inhibitor in Hospitalized Patients With Severe Forms of COVID-19 [NCT04724629] | Phase 3 | 60 participants (Actual) | Interventional | 2021-01-05 | Completed | ||
| A Randomized, Double-Blind, Double-Dummy Pharmacokinetic and Exploratory Electrocardiogram (ECG) Safety Study of a Standard Acute Gout Regimen [NCT01018420] | Phase 1 | 18 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| COlchicine for Left VEntricular Remodeling Treatment in Acute Myocardial Infarction, a Phase II, Multicenter, Randomized, Double Blinded, Placebo Controlled Clinical Trial [NCT03156816] | Phase 2 | 194 participants (Actual) | Interventional | 2018-07-23 | Completed | ||
| Effectiveness and Safety of Medical Treatment for SARS-CoV-2 (COVID-19) in Colombia: A Pragmatic Randomized Controlled Trial [NCT04359095] | Phase 2/Phase 3 | 650 participants (Actual) | Interventional | 2020-08-18 | Completed | ||
| A One-Directional, Open-Label Drug Interaction Study to Investigate the Effects of Multiple-Dose Azithromycin on Single-Dose Pharmacokinetics of Colchicine in Healthy Volunteers [NCT00983294] | Phase 1 | 24 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| Effect of Colchicine on the Progression of Aortic Valve Stenosis - A Pilot Study [NCT05253794] | Phase 2/Phase 3 | 24 participants (Anticipated) | Interventional | 2022-07-01 | Recruiting | ||
| Efficacy and Safety of Edoxaban and or Colchicine for Patients With SARS-CoV-2 Infection Managed in the Out of Hospital Setting [NCT04516941] | Phase 3 | 60 participants (Actual) | Interventional | 2021-01-21 | Terminated(stopped due to Insufficient rate of patient accrual and newly available scientific evidence) | ||
| CONVINCE - (COlchicine for preventioN of Vascular Inflammation in Non- CardioEmbolic Stroke) - a Randomised Clinical Trial of Low-dose Colchicine for Secondary Prevention After Stroke [NCT02898610] | Phase 3 | 3,154 participants (Actual) | Interventional | 2016-12-12 | Active, not recruiting | ||
| Repurposing Colchicine to Improve Vascular Function in Hypertension [NCT04303689] | 31 participants (Actual) | Interventional | 2020-08-01 | Completed | |||
| Effect of Low Dose ColchiciNe on the InciDence of Atrial Fibrillation in Open Heart Surgery Patients [NCT03015831] | Phase 3 | 254 participants (Actual) | Interventional | 2017-10-02 | Terminated(stopped due to Statistical analysis of interim data showed no advantage of colchicine) | ||
| A Phase 2, Randomized, Double Blind, Multicenter, Placebo Controlled Study to Evaluate the Efficacy and Safety of Febuxostat 40 mg XR, 80 mg XR, 40 mg IR and 80 mg IR in Subjects With Gout and Moderate Renal Impairment [NCT02128490] | Phase 2 | 189 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| Does Colchicine Reduce Progression of Aortic Valve Stenosis? [NCT05162742] | Phase 3 | 150 participants (Anticipated) | Interventional | 2022-12-22 | Recruiting | ||
| The Effect of Intensive Urate Lowering Therapy (ULT) With Febuxostat in Comparison With Allopurinol on Cardiovascular Risk in Patients With Gout Using Surrogate Markers: a Randomized, Controlled Trial [NCT02500641] | Phase 4 | 196 participants (Actual) | Interventional | 2015-08-17 | Completed | ||
| Inflammation and Coronary Endothelial Function in Patients With Coronary Artery Disease [NCT02366091] | Phase 2 | 111 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
| Reducing Inflammation in Ischemic Stroke With Colchicine, and Ticagrelor in High-risk Patients-extended Treatment in Ischemic Stroke [NCT05476991] | Phase 3 | 2,800 participants (Anticipated) | Interventional | 2023-05-17 | Recruiting | ||
| Colchicine in High-risk Patients With Acute Minor-to-moderate Ischemic Stroke or Transient Ischemic Attack (CHANCE-3) [NCT05439356] | Phase 3 | 8,238 participants (Anticipated) | Interventional | 2022-08-11 | Recruiting | ||
| Colchicine Cardiovascular Outcomes Trial (COLCOT) [NCT02551094] | Phase 3 | 4,745 participants (Actual) | Interventional | 2015-12-04 | Completed | ||
| [NCT00370201] | Phase 3 | 0 participants | Interventional | 2004-03-31 | Active, not recruiting | ||
| A One-Directional, Open-Label Drug-Food Interaction Study to Investigate the Effects of Multiple-Daily Consumptions of Grapefruit Juice on the Single-Dose Pharmacokinetics of Colchicine in Healthy Volunteers [NCT00984009] | Phase 1 | 24 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
| A One-Directional, Open-label Drug Interaction Study to Investigate the Effects of Single-Dose Cyclosporine on Single-Dose Pharmacokinetics of Colchicine in Healthy Volunteers [NCT00983931] | Phase 1 | 24 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
| Asthma Clinical Research Network (ACRN) [NCT00000577] | Phase 3 | 0 participants (Actual) | Interventional | 1993-09-30 | Withdrawn(stopped due to Record is an ACRN grant summary & not reflective of an individual trial. All ACTs conducted by ACRN were individually registered on the PRS.) | ||
| Phase III Randomized, Double-Blind, Placebo-Controlled Study of Low-Dose Oral Methotrexate Versus Colchicine for Primary Biliary Cirrhosis [NCT00004748] | Phase 3 | 90 participants | Interventional | 1989-11-30 | Completed | ||
| Evaluation the Potential of Colchicine for the Palliative Management of Hepatocellular Carcinoma Patients With Distant Metastasis or Large Vessel Invasion [NCT01935700] | Phase 2 | 15 participants (Actual) | Interventional | 2013-06-06 | Completed | ||
| Multi-centre, Open-label, Active-comparator, Pragmatic Clinical Trial of Low-dose Colchicine Versus Naproxen in Patients With Acute Gout. [NCT01994226] | Phase 4 | 399 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
| Impact and Time Course of Colchicine Therapy on C-reactive Protein Elevation in Chronic Atrial Fibrillation (AF) and Post AF Ablation [NCT01755949] | Phase 2 | 26 participants (Actual) | Interventional | 2013-03-31 | Completed | ||
| An Open-Label, One Sequence, Pharmacokinetic Drug Interaction Study of Colchicine and Theophylline in Healthy Subjects [NCT01601132] | Phase 4 | 30 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
| Phase 2/3, Randomized, Open Study to Compare the Efficacy and Safety of Colchicine and Glucocorticoids Compared With the Standard of Treatment for Moderate/Severe COVID-19 in a Fragile and Vulnerable Population, Admitted to a Geriatric Hospital Unit or in [NCT04492358] | Phase 2/Phase 3 | 54 participants (Actual) | Interventional | 2020-10-22 | Terminated(stopped due to No candidates for the recruitment) | ||
| Colchicine For Prevention of Perioperative Atrial Fibrillation in Patients Undergoing Thoracic Surgery Pilot Study. [NCT01985425] | Phase 3 | 100 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
| The Canadian Study of Arterial Inflammation in Patients With Diabetes and Recent Vascular Events: EvaluatioN of Colchicine Effectiveness (CADENCE) [NCT04181996] | Phase 3 | 115 participants (Anticipated) | Interventional | 2020-08-01 | Recruiting | ||
| Inflammatory Pathogenesis of Coronary Atherosclerosis in HIV [NCT02624180] | Phase 2 | 81 participants (Actual) | Interventional | 2015-11-30 | Completed | ||
| [NCT00370760] | Phase 3 | 0 participants | Interventional | 2006-09-30 | Recruiting | ||
| Effect of ColchiciNe on the InciDence of Atrial Fibrillation in Open Heart Surgery Patients: END-AF Trial [NCT03021343] | Phase 3 | 360 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| Colchicine Influence on Chronic Inflammation in Hemodialysis Patients [NCT05677555] | Phase 2 | 50 participants (Anticipated) | Interventional | 2022-11-01 | Recruiting | ||
| [NCT01451645] | Phase 4 | 82 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
| Evaluation of Colchicine and Nonsteroidal Anti-inflammatory Drug Combination Therapy and Renal Function in Gout Patients [NCT05006001] | 2,000 participants (Anticipated) | Observational | 2012-01-01 | Active, not recruiting | |||
| Colchicine Treatment for Patients With Hand Osteoarthritis: A Randomised, Placebo-controlled Trial. [NCT04601883] | Phase 4 | 100 participants (Actual) | Interventional | 2021-01-15 | Completed | ||
| Colchicine Versus Placebo in Post-Cardiac Surgery Patients to Prevent Post-Pericardiotomy Syndrome and Atrial Fibrillation [NCT02177266] | Phase 3 | 2 participants (Actual) | Interventional | 2015-05-31 | Terminated(stopped due to Difficulty in recruiting patients) | ||
| A Phase 3, Randomized, Double Blind, Multicenter, Placebo Controlled Study to Evaluate the Efficacy and Safety of Febuxostat 40 mg XR, 80 mg XR, 40 mg IR and 80 mg IR in Subjects With Gout [NCT02139046] | Phase 3 | 1,790 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
| Impact of Short-course Colchicine Versus Placebo After Pulmonary Vein Isolation (IMPROVE-PVI): A Pilot Study [NCT04160117] | Phase 3 | 200 participants (Anticipated) | Interventional | 2020-01-14 | Recruiting | ||
| Colchicine for Prevention Atrial Fibrillation After Cardiac Surgery in the Early Postoperative Period [NCT04224545] | Phase 4 | 267 participants (Actual) | Interventional | 2019-12-23 | Completed | ||
| The Effects of Probiotic Lactobacillus Acidophilus and Colchicine on the Control of Symptoms, Duration, and Disease Progression of Mild and Moderate Cases of COVID-19: A Randomized Controlled Clinical Trial. [NCT05911022] | 150 participants (Actual) | Interventional | 2021-07-01 | Completed | |||
| COlchicine in Moderate-severe Hospitalized Patients Before ARDS to Treat COVID-19 (the COMBAT-COVID-19 Pilot Study) [NCT04363437] | Phase 2 | 21 participants (Actual) | Interventional | 2020-04-26 | Terminated(stopped due to Stopped due to widespread corticosteroid use in 2020 for COVID infection, which confounds and likely supercedes the effect of colchicine.) | ||
| A One-Directional, Open-Label Drug Interaction Study to Investigate the Effects of Multiple-Dose Ketoconazole on Single-Dose Pharmacokinetics of Colchicine in Healthy Volunteers [NCT00983216] | Phase 1 | 24 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| The COLchicine HEART Failure PRESERVED Trial (COLHEART-PRESERVED) [NCT06081049] | Phase 2 | 152 participants (Anticipated) | Interventional | 2024-01-31 | Not yet recruiting | ||
| Low-dose Colchicine Inhibit Abdominal Aortic Aneurysm Growth Trial [NCT05361772] | 230 participants (Anticipated) | Interventional | 2022-06-01 | Not yet recruiting | |||
| Anti-platelet Effects of Colchicine in Healthy Volunteers [NCT02140372] | Phase 4 | 10 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| Measurement of Colchicine Levels in the Serum of FMF Patients [NCT03210610] | 80 participants (Anticipated) | Observational | 2017-10-19 | Recruiting | |||
| A One-Directional, Open Label Drug Interaction Study to Investigate the Effects of Multiple Dose Verapamil HCl ER on Single Dose Pharmacokinetics of Colchicine in Healthy Volunteers [NCT00983242] | Phase 1 | 24 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
| The Role of Colchicine in Reducing The Rate of Myocardial Reperfusion Injury in Patients With ST-Elevation Myocardial Infarction After Primary Percutaneous Coronary Intervention: Study on NLRP3, ASC, Caspase, and Troponin [NCT05734612] | Phase 3 | 80 participants (Anticipated) | Interventional | 2022-12-04 | Enrolling by invitation | ||
| Comparison of Maximum Blood Concentrations of Colchicine Between Responders and Non-responders to Colchicine Treatment During Gout Flare [NCT03933007] | Phase 4 | 88 participants (Anticipated) | Interventional | 2019-09-10 | Recruiting | ||
| Effect of Combined Use of Ivermectin and Colchicine in COVID-19 Patients [NCT05246072] | Phase 4 | 135 participants (Actual) | Interventional | 2021-11-01 | Completed | ||
| Open-label (Unblinded) Randomization to Treatment of Colchicine Plus Current Care Per Institution Treating Physicians vs. Current Care Per Institution Treating Physicians (Control Arm) [NCT04762771] | Phase 1/Phase 2 | 2 participants (Actual) | Interventional | 2020-12-23 | Terminated(stopped due to Recovery Trial showed no convincing evidence that further recruitment would provide conclusive proof of worthwhile benefit for the evaluation of Colchicine in patients with Covid-19.) | ||
| Two-center, Prospective, Randomized, Open-label, Controlled Clinical Trial With Endpoint Evaluation [NCT06102720] | Phase 4 | 200 participants (Anticipated) | Interventional | 2023-01-12 | Recruiting | ||
| Effect of Colchicine Use On Left Ventricle Systolic Function Using Speckle Tracking Echocardiography in Patients With Anterior S-T Segment Elevation Myocardial Infarction [NCT05200052] | Phase 4 | 100 participants (Actual) | Interventional | 2022-02-01 | Completed | ||
| Impact of Anti-Inflammatory and Anti-Fibrotic Drugs on Post-acute COVID-19 Pulmonary Fibrosis [NCT05648734] | 200 participants (Actual) | Observational | 2022-03-10 | Completed | |||
| COLchicine Versus Ruxolitinib and Secukinumab in Open-label Prospective Randomized Trial in Patients With COVID-19 [NCT04403243] | Phase 2 | 70 participants (Actual) | Interventional | 2020-05-08 | Completed | ||
| Adding Colchicine to Tocilizumab in Hospitalized Patients With Severe COVID-19 Pneumonia: An Open-Label Randomized Controlled Trial [NCT05118737] | Early Phase 1 | 230 participants (Anticipated) | Interventional | 2021-10-01 | Recruiting | ||
| A Vanguard, Double-blind, Randomized, Placebo-controlled, Phase 2 Pilot Study to Investigate Prevention of Cardiovascular Events With Oral Colchicine 0.5mg Once Daily Compared With Placebo in Participants With Spontaneous ICH and Established, or Risk Fact [NCT05159219] | Phase 2 | 100 participants (Anticipated) | Interventional | 2022-08-04 | Recruiting | ||
| Anti-inflammatory Effects of Colchicine in Patients Undergoing Percutaneous Coronary Intervention: Inflammatory Marker Substudy of the Colchicine-PCI Trial [NCT01709981] | Phase 4 | 280 participants (Actual) | Interventional | 2013-05-30 | Completed | ||
| Efficacy and Safety of Low-Dose Colchicine on Surrogate Markers of Cardiovascular Events in People Living With HIV Receiving Antiretroviral Therapy [NCT05168137] | Phase 4 | 84 participants (Anticipated) | Interventional | 2020-02-01 | Recruiting | ||
| Colchicine Prevents Myocardial Injury After Non-Cardiac Surgery Pilot Study (COPMAN) [NCT04139655] | 0 participants (Actual) | Interventional | 2020-09-01 | Withdrawn(stopped due to Feasibility) | |||
| Effect of Colchicine on Perioperative Anti-inflammatory Organ Injury in Cardiac Surgery : a Multi-center, Randomized, Controlled, Double-blind Clinical Trial [NCT06118034] | Phase 3 | 768 participants (Anticipated) | Interventional | 2024-01-01 | Not yet recruiting | ||
| PREEMPTIVE THERAPY WITH COLCHICINE IN PATIENTS OLDER THAN 60 YEARS WITH HIGH RISK OF SEVERE PNEUMONIAE DUE TO CORONAVIRUS SARS-CoV2 (COVID-19) [NCT04416334] | Phase 3 | 70 participants (Actual) | Interventional | 2020-08-19 | Completed | ||
| Effect of Inflammasome Inhibitor on High-sensitivity C-reactive Protein in Patients After Percutaneous Coronary Intervention [NCT05130892] | Phase 4 | 132 participants (Actual) | Interventional | 2021-11-15 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||