Page last updated: 2024-08-07 16:54:14
Tubulin alpha-4A chain
A tubulin alpha-4A chain that is encoded in the genome of human. [PRO:DNx, UniProtKB:P68366]
Synonyms
Alpha-tubulin 1;
Testis-specific alpha-tubulin;
Tubulin H2-alpha;
Tubulin alpha-1 chain
Research
Bioassay Publications (117)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 7 (5.98) | 18.2507 |
| 2000's | 29 (24.79) | 29.6817 |
| 2010's | 55 (47.01) | 24.3611 |
| 2020's | 26 (22.22) | 2.80 |
Compounds (60)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nocodazole | Homo sapiens (human) | IC50 | 1.2975 | 4 | 4 |
| vincristine | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| colchicine | Homo sapiens (human) | IC50 | 22.8838 | 39 | 39 |
| colchicine | Homo sapiens (human) | Ki | 2.4000 | 1 | 1 |
| kokusaginine | Homo sapiens (human) | IC50 | 0.8200 | 1 | 1 |
| podophyllotoxin | Homo sapiens (human) | IC50 | 67.1914 | 7 | 7 |
| vinblastine | Homo sapiens (human) | IC50 | 0.8233 | 3 | 3 |
| desacetamidocolchicine | Homo sapiens (human) | IC50 | 2.6000 | 1 | 1 |
| thiocholchicine | Homo sapiens (human) | IC50 | 0.9400 | 5 | 5 |
| parbendazole | Homo sapiens (human) | IC50 | 9.5500 | 1 | 1 |
| paclitaxel | Homo sapiens (human) | GI50 | 0.0053 | 3 | 3 |
| 2-demethylthiocolchicine | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| 3-demethylthiocolchicine | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| quercetin 5,7,3',4'-tetramethyl ether | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| 5,4'-dihydroxy-3,6,7,8,3'-pentamethoxyflavone | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| 5-hydroxy-3,6,7,8,3',4'-hexamethoxyflavone | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| docetaxel | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| levofloxacin | Homo sapiens (human) | IC50 | 11.2700 | 1 | 1 |
| 3,3',4',5,6,7,8-heptamethoxyflavone | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| ustiloxin d | Homo sapiens (human) | IC50 | 1.5000 | 1 | 1 |
| 4'-demethyldesoxypodophyllotoxin | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| 2-phenyl-4-oxohydroquinoline | Homo sapiens (human) | IC50 | 7.3000 | 1 | 1 |
| ustiloxin a | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| vinblastine sulfate | Homo sapiens (human) | IC50 | 0.1500 | 1 | 1 |
| vincaleukoblastine | Homo sapiens (human) | IC50 | 0.7400 | 1 | 1 |
| gardenin a | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| 3',4',5'-trimethoxyflavone | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| anthricin | Homo sapiens (human) | IC50 | 2.4000 | 1 | 1 |
| 5-demethylnobiletin | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| 5,3'-dihydroxy-3,6,7,8,4'-pentamethoxyflavone | Homo sapiens (human) | IC50 | 0.8300 | 2 | 2 |
| epothilone b | Homo sapiens (human) | IC50 | 0.0035 | 1 | 1 |
| chalcone | Homo sapiens (human) | IC50 | 620.0000 | 1 | 1 |
| 2-amino-3-cyano-7-(dimethylamino)-4-(3-methoxy-4,5-methylenedioxyphenyl)-4h-chromene | Homo sapiens (human) | IC50 | 0.4000 | 1 | 1 |
| e 7010 | Homo sapiens (human) | IC50 | 2.6400 | 2 | 2 |
| e 7010 | Homo sapiens (human) | Ki | 1.5100 | 1 | 1 |
| eupatilin | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| ayanin | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| santin | Homo sapiens (human) | IC50 | 5.7000 | 1 | 1 |
| curacin a | Homo sapiens (human) | IC50 | 0.7200 | 1 | 1 |
| vinorelbine | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
| centaureidin | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| eupatin | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| 5,7-dihydroxy-4',6-dimethoxyflavone | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| fosbretabulin | Homo sapiens (human) | IC50 | 10.7722 | 58 | 58 |
| fosbretabulin | Homo sapiens (human) | Ki | 0.0615 | 2 | 2 |
| 5,7,3'-trihydroxy-3,4'-dimethoxyflavone | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| 1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene | Homo sapiens (human) | IC50 | 1.8500 | 2 | 2 |
| vinblastine sulfate | Homo sapiens (human) | IC50 | 0.1300 | 1 | 1 |
| ternatin (flavonoid) | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| cryptophycin 1 | Homo sapiens (human) | IC50 | 3.7000 | 1 | 1 |
| pironetin | Homo sapiens (human) | GI50 | 0.0222 | 2 | 2 |
| pironetin | Homo sapiens (human) | IC50 | 0.0260 | 1 | 1 |
| ave-8063 | Homo sapiens (human) | IC50 | 3.8500 | 2 | 2 |
| dolastatin 10 | Homo sapiens (human) | IC50 | 0.3012 | 4 | 4 |
| 3-hydroxy-4,3',4',5'-tetramethoxychalcone | Homo sapiens (human) | IC50 | 5.6833 | 3 | 3 |
| nsc 348103 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| dolastatin 15 | Homo sapiens (human) | IC50 | 23.0000 | 1 | 1 |
| arenastatin a | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| zampanolide | Homo sapiens (human) | GI50 | 0.0035 | 3 | 3 |
| isocombretastatin a-4 | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
| 2-styrylquinazolin-4(3h)-one | Homo sapiens (human) | IC50 | 11.0000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| colchicine | Homo sapiens (human) | Activity | 9.4733 | 9 | 9 |
| podophyllotoxin | Homo sapiens (human) | Activity | 23.5000 | 1 | 1 |
| paclitaxel | Homo sapiens (human) | ED50 | 0.5000 | 1 | 1 |
| docetaxel | Homo sapiens (human) | Activity | 0.9000 | 1 | 1 |
| pironetin | Homo sapiens (human) | Activity | 15.0000 | 1 | 1 |
Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Design, synthesis and biological evaluation of imidazopyridine-propenone conjugates as potent tubulin inhibitors.MedChemComm, , May-01, Volume: 8, Issue:5, 2017
Design, synthesis and biological evaluations of chirally pure 1,2,3,4-tertrahydroisoquinoline analogs as anti-cancer agents.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
Podoverine A--a novel microtubule destabilizing natural product from the Podophyllum species.Bioorganic & medicinal chemistry, , Sep-15, Volume: 22, Issue:18, 2014
Synthesis, antiproliferative activity and inhibition of tubulin polymerization by anthracenone-based oxime derivatives.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
Discovery of a Novel Stilbene Derivative as a Microtubule Targeting Agent Capable of Inducing Cell Ferroptosis.Journal of medicinal chemistry, , 03-24, Volume: 65, Issue:6, 2022
[no title available]RSC medicinal chemistry, , Aug-17, Volume: 13, Issue:8, 2022
Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Combretastatin A-4 sulfur-containing heterocyclic derivatives: Synthesis, antiproliferative activities and molecular docking studies.European journal of medicinal chemistry, , Apr-05, Volume: 215, 2021
Synthesis and structure-activity relationships of 5-phenyloxazole-2-carboxylic acid derivatives as novel inhibitors of tubulin polymerization.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Application of triazoles as bioisosteres and linkers in the development of microtubule targeting agents.RSC medicinal chemistry, , Mar-01, Volume: 11, Issue:3, 2020
New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation.Bioorganic & medicinal chemistry, , 11-01, Volume: 28, Issue:21, 2020
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.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
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.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors.European journal of medicinal chemistry, , May-25, Volume: 152, 2018
Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Antivascular and anti-parasite activities of natural and hemisynthetic flavonoids from New Caledonian Gardenia species (Rubiaceae).European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
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.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Concise syntheses of 7-anilino-indoline-N-benzenesulfonamides as antimitotic and vascular disrupting agents.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Discovery of potent cytotoxic ortho-aryl chalcones as new scaffold targeting tubulin and mitosis with affinity-based fluorescence.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin.Journal of medicinal chemistry, , Dec-26, Volume: 57, Issue:24, 2014
Furanylazaindoles: potent anticancer agents in vitro and in vivo.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.Journal of medicinal chemistry, , Jan-10, Volume: 56, Issue:1, 2013
Synthesis, antiproliferative activity and inhibition of tubulin polymerization by anthracenone-based oxime derivatives.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
4- and 5-aroylindoles as novel classes of potent antitubulin agents.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
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.Journal of medicinal chemistry, , Nov-29, Volume: 50, Issue:24, 2007
Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
9-Benzylidene-naphtho[2,3-b]thiophen-4-ones as novel antimicrotubule agents-synthesis, antiproliferative activity, and inhibition of tubulin polymerization.Journal of medicinal chemistry, , Dec-28, Volume: 49, Issue:26, 2006
Benzoylphenylurea sulfur analogues with potent antitumor activity.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.Journal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
[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.Journal of medicinal chemistry, , Sep-21, Volume: 49, Issue:19, 2006
7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents.Journal of medicinal chemistry, , Nov-16, Volume: 49, Issue:23, 2006
Synthesis and biological evaluation of B-ring modified colchicine and isocolchicine analogs.Bioorganic & medicinal chemistry letters, , May-15, Volume: 16, Issue:10, 2006
Arylthioindoles, potent inhibitors of tubulin polymerization.Journal of medicinal chemistry, , Dec-02, Volume: 47, Issue:25, 2004
Novel benzylidene-9(10H)-anthracenones as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization.Journal of medicinal chemistry, , Jul-17, Volume: 46, Issue:15, 2003
Antitumor agents. Part 204: synthesis and biological evaluation of substituted 2-aryl quinazolinones.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors.Journal of medicinal chemistry, , May-21, Volume: 41, Issue:11, 1998
Structure-activity requirements for flavone cytotoxicity and binding to tubulin.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Antitumor agents. 172. Synthesis and biological evaluation of novel deacetamidothiocolchicin-7-ols and ester analogs as antitubulin agents.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
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.Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
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.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
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.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
Effects on tubulin polymerization and down-regulation of c-Myc, hTERT and VEGF genes by colchicine haloacetyl and haloaroyl derivatives.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Synthesis of a terphenyl substituted 4-aza-2,3-didehydropodophyllotoxin analogues as inhibitors of tubulin polymerization and apoptosis inducers.Bioorganic & medicinal chemistry, , May-01, Volume: 22, Issue:9, 2014
Synthesis, antiproliferative activity and inhibition of tubulin polymerization by anthracenone-based oxime derivatives.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
Benzoylphenylurea sulfur analogues with potent antitumor activity.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
[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.Journal of medicinal chemistry, , Sep-21, Volume: 49, Issue:19, 2006
Antitumor agents. Part 204: synthesis and biological evaluation of substituted 2-aryl quinazolinones.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors.Journal of medicinal chemistry, , May-21, Volume: 41, Issue:11, 1998
Synthesis and biological evaluation of C-13' substituted 7'-homo-anhydrovinblastine derivatives.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 25, Issue:8, 2015
Identification of novel and improved antimitotic agents derived from noscapine.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
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.Journal of medicinal chemistry, , Dec-02, Volume: 47, Issue:25, 2004
New alpha-amino phosphonic acid derivatives of vinblastine: chemistry and antitumor activity.Journal of medicinal chemistry, , Volume: 34, Issue:7, 1991
Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors.Journal of medicinal chemistry, , May-21, Volume: 41, Issue:11, 1998
Antitumor agents. 172. Synthesis and biological evaluation of novel deacetamidothiocolchicin-7-ols and ester analogs as antitubulin agents.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
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.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Synthesis, conformational preferences, and biological activity of conformational analogues of the microtubule-stabilizing agents, (-)-zampanolide and (-)-dactylolide.MedChemComm, , May-01, Volume: 10, Issue:5, 2019
Design and synthesis of cyclopropylamide analogues of combretastatin-A4 as novel microtubule-stabilizing agents.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
Privileged structure-based quinazolinone natural product-templated libraries: identification of novel tubulin polymerization inhibitors.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin.Journal of medicinal chemistry, , Dec-26, Volume: 57, Issue:24, 2014
Novel C2-C3' N-peptide linked macrocyclic taxoids. Part 2: synthesis and biological activities of docetaxel analogues with a peptide side chain at C2 and their macrocyclic derivatives.Bioorganic & medicinal chemistry, , Jan-01, Volume: 15, Issue:1, 2007
Progress Toward the Development of Noscapine and Derivatives as Anticancer Agents.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
Identification of novel and improved antimitotic agents derived from noscapine.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
How to deal with low-resolution target structures: using SAR, ensemble docking, hydropathic analysis, and 3D-QSAR to definitively map the αβ-tubulin colchicine site.Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
Antitumor agents. Part 204: synthesis and biological evaluation of substituted 2-aryl quinazolinones.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Structure-activity requirements for flavone cytotoxicity and binding to tubulin.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Synthesis of 2-anilinopyridine dimers as microtubule targeting and apoptosis inducing agents.Bioorganic & medicinal chemistry, , Dec-15, Volume: 22, Issue:24, 2014
Synthesis and evaluation of N-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)nicotinamides as potential anticancer agents that inhibit tubulin polymerization.Bioorganic & medicinal chemistry, , Jul-01, Volume: 22, Issue:13, 2014
Furanylazaindoles: potent anticancer agents in vitro and in vivo.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Synthesis and biological evaluation of C-13' substituted 7'-homo-anhydrovinblastine derivatives.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 25, Issue:8, 2015
Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
[no title available]Bioorganic & medicinal chemistry letters, , 06-15, Volume: 66, 2022
Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Design, synthesis and biological evaluation of quinoline-2-carbonitrile-based hydroxamic acids as dual tubulin polymerization and histone deacetylases inhibitors.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Design, synthesis and biological evaluation of new parbendazole derivatives for the treatment of HNSCC.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.European journal of medicinal chemistry, , Nov-05, Volume: 223, 2021
Synthesis of the analogs of plocabulin and their preliminary structure-activity relationship study.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 51, 2021
Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia.European journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Novel pyrazolo[4,3-d]pyrimidine microtubule targeting agents (MTAs): Synthesis, structure-activity relationship, in vitro and in vivo evaluation as antitumor agents.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 41, 2021
Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
A facile synthesis of diaryl pyrroles led to the discovery of potent colchicine site antimitotic agents.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines.European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
Synthesis, biological evaluation, and structure-activity relationships of new tubulin polymerization inhibitors based on 5-amino-1,2,4-triazole scaffold.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 38, 2021
Ultrasound assisted synthesis of tetrazole based pyrazolines and isoxazolines as potent anticancer agents via inhibition of tubulin polymerization.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 30, Issue:22, 2020
Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.European journal of medicinal chemistry, , Jul-01, Volume: 173, 2019
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 29, Issue:18, 2019
[no title available]Bioorganic & medicinal chemistry letters, , 01-01, Volume: 29, Issue:1, 2019
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.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 28, Issue:14, 2018
New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors.European journal of medicinal chemistry, , May-25, Volume: 152, 2018
An overview of benzo[b]thiophene-based medicinal chemistry.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Design, Synthesis, and Preclinical Evaluation of 4-Substituted-5-methyl-furo[2,3-d]pyrimidines as Microtubule Targeting Agents That Are Effective against Multidrug Resistant Cancer Cells.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
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.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 26, Issue:1, 2016
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.Journal of medicinal chemistry, , Feb-12, Volume: 58, Issue:3, 2015
Novel hybrid nocodazole analogues as tubulin polymerization inhibitors and their antiproliferative activity.Bioorganic & medicinal chemistry letters, , May-01, Volume: 25, Issue:9, 2015
Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
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.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
Triazole linked mono carbonyl curcumin-isatin bifunctional hybrids as novel anti tubulin agents: Design, synthesis, biological evaluation and molecular modeling studies.Bioorganic & medicinal chemistry, , Nov-15, Volume: 23, Issue:22, 2015
Optimization of N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines as tubulin polymerization inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 23, Issue:17, 2015
Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers.Bioorganic & medicinal chemistry, , Oct-01, Volume: 22, Issue:19, 2014
Chalcone based azacarboline analogues as novel antitubulin agents: design, synthesis, biological evaluation and molecular modelling studies.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Concise syntheses of 7-anilino-indoline-N-benzenesulfonamides as antimitotic and vascular disrupting agents.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Optimization of 4-(N-cycloamino)phenylquinazolines as a novel class of tubulin-polymerization inhibitors targeting the colchicine site.Journal of medicinal chemistry, , Feb-27, Volume: 57, Issue:4, 2014
Synthesis and antiproliferative evaluation of novel benzoimidazole-contained oxazole-bridged analogs of combretastatin A-4.European journal of medicinal chemistry, , Volume: 68, 2013
N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines: a novel class of antitumor agents targeting the colchicine site on tubulin.European journal of medicinal chemistry, , Volume: 67, 2013
Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 23, Issue:16, 2013
Furanylazaindoles: potent anticancer agents in vitro and in vivo.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Synthesis and biological evaluation of enantiomerically pure cyclopropyl analogues of combretastatin A4.Bioorganic & medicinal chemistry, , Mar-01, Volume: 21, Issue:5, 2013
Synthesis and biological evaluation of N-alkyl-N-(4-methoxyphenyl)pyridin-2-amines as a new class of tubulin polymerization inhibitors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 21, Issue:3, 2013
Identification of diaryl 5-amino-1,2,4-oxadiazoles as tubulin inhibitors: the special case of 3-(2-fluorophenyl)-5-(4-methoxyphenyl)amino-1,2,4-oxadiazole.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.Journal of medicinal chemistry, , Jan-10, Volume: 56, Issue:1, 2013
Design, synthesis and anticancer properties of 5-arylbenzoxepins as conformationally restricted isocombretastatin A-4 analogs.European journal of medicinal chemistry, , Volume: 62, 2013
Design, synthesis, and biological evaluation of novel γ-carboline ketones as anticancer agents.European journal of medicinal chemistry, , Volume: 46, Issue:4, 2011
Highly potent triazole-based tubulin polymerization inhibitors.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
4- and 5-aroylindoles as novel classes of potent antitubulin agents.Journal of medicinal chemistry, , Sep-06, Volume: 50, Issue:18, 2007
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Conformationally restricted macrocyclic analogues of combretastatins.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.Journal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
Benzoylphenylurea sulfur analogues with potent antitumor activity.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.Journal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
Novel combretastatin analogues endowed with antitumor activity.Journal of medicinal chemistry, , Jun-01, Volume: 49, Issue:11, 2006
7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents.Journal of medicinal chemistry, , Nov-16, Volume: 49, Issue:23, 2006
Synthesis and structure-activity relationships of 1,2,4-triazoles as a novel class of potent tubulin polymerization inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Arylthioindoles, potent inhibitors of tubulin polymerization.Journal of medicinal chemistry, , Dec-02, Volume: 47, Issue:25, 2004
Antitumor agents. Part 204: synthesis and biological evaluation of substituted 2-aryl quinazolinones.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
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.Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Conformationally restricted macrocyclic analogues of combretastatins.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
2-amino and 2'-aminocombretastatin derivatives as potent antimitotic agents.Journal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
Identification of the Metabolic Profile of the α-Tubulin-Binding Natural Product (-)-Pironetin.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin.Journal of medicinal chemistry, , Dec-26, Volume: 57, Issue:24, 2014
Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 23, Issue:16, 2013
Identification of CKD-516: a potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Discovery and Development of Dolastatin 10-Derived Antibody Drug Conjugate Anticancer Drugs.Journal of natural products, , 03-25, Volume: 85, Issue:3, 2022
Marine Invertebrate Natural Products that Target Microtubules.Journal of natural products, , 03-23, Volume: 81, Issue:3, 2018
Total synthesis and biological evaluation of ustiloxin natural products and two analogs.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 16, Issue:18, 2006
Design, synthesis and biological evaluation of pyridine-chalcone derivatives as novel microtubule-destabilizing agents.European journal of medicinal chemistry, , Jul-01, Volume: 173, 2019
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.Bioorganic & medicinal chemistry letters, , 09-15, Volume: 29, Issue:18, 2019
Effects of alpha-substitutions on structure and biological activity of anticancer chalcones.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 16, Issue:22, 2006
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| hydrolase activity | molecular function | Catalysis of the hydrolysis of various bonds, e.g. C-O, C-N, C-C, phosphoric anhydride bonds, etc. [ISBN:0198506732] |
| protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| structural constituent of cytoskeleton | molecular function | The action of a molecule that contributes to the structural integrity of a cytoskeletal structure. [GOC:mah] |
| GTP binding | molecular function | Binding to GTP, guanosine triphosphate. [GOC:ai] |
Located In
This protein is located in 6 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| cytoskeleton | cellular component | A cellular structure that forms the internal framework of eukaryotic and prokaryotic cells. The cytoskeleton includes intermediate filaments, microfilaments, microtubules, the microtrabecular lattice, and other structures characterized by a polymeric filamentous nature and long-range order within the cell. The various elements of the cytoskeleton not only serve in the maintenance of cellular shape but also have roles in other cellular functions, including cellular movement, cell division, endocytosis, and movement of organelles. [GOC:mah, PMID:16959967, PMID:27419875] |
| microtubule | cellular component | Any of the long, generally straight, hollow tubes of internal diameter 12-15 nm and external diameter 24 nm found in a wide variety of eukaryotic cells; each consists (usually) of 13 protofilaments of polymeric tubulin, staggered in such a manner that the tubulin monomers are arranged in a helical pattern on the microtubular surface, and with the alpha/beta axes of the tubulin subunits parallel to the long axis of the tubule; exist in equilibrium with pool of tubulin monomers and can be rapidly assembled or disassembled in response to physiological stimuli; concerned with force generation, e.g. in the spindle. [ISBN:0879693568] |
| microtubule cytoskeleton | cellular component | The part of the cytoskeleton (the internal framework of a cell) composed of microtubules and associated proteins. [GOC:jl, ISBN:0395825172] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| microtubule | cellular component | Any of the long, generally straight, hollow tubes of internal diameter 12-15 nm and external diameter 24 nm found in a wide variety of eukaryotic cells; each consists (usually) of 13 protofilaments of polymeric tubulin, staggered in such a manner that the tubulin monomers are arranged in a helical pattern on the microtubular surface, and with the alpha/beta axes of the tubulin subunits parallel to the long axis of the tubule; exist in equilibrium with pool of tubulin monomers and can be rapidly assembled or disassembled in response to physiological stimuli; concerned with force generation, e.g. in the spindle. [ISBN:0879693568] |
Involved In
This protein is involved in 2 target(s):
| Target | Category | Definition |
|---|
| microtubule cytoskeleton organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of cytoskeletal structures comprising microtubules and their associated proteins. [GOC:mah] |
| mitotic cell cycle | biological process | Progression through the phases of the mitotic cell cycle, the most common eukaryotic cell cycle, which canonically comprises four successive phases called G1, S, G2, and M and includes replication of the genome and the subsequent segregation of chromosomes into daughter cells. In some variant cell cycles nuclear replication or nuclear division may not be followed by cell division, or G1 and G2 phases may be absent. [GOC:mah, ISBN:0815316194, Reactome:69278] |