Query String: Colchicine
- Andres, C; Bernardo, J; Yan, Q; Hastie, S; Macdonald, T Combretatroponeshybrids of combretastatin and colchicine. Synthesis and biochemical evaluation Bioorg Med Chem Lett 3: 565-570 (1993)
- Nakagawa-Goto, K; Chen, CX; Hamel, E; Wu, CC; Bastow, KF; Brossi, A; Lee, KH Antitumor agents. Part 236: Synthesis of water-soluble colchicine derivatives. Bioorg Med Chem Lett 15: 235-8 (2004)
- Dual-target inhibitors of colchicine binding site for cancer treatment.
- Thomopoulou, P; Sachs, J; Teusch, N; Mariappan, A; Gopalakrishnan, J; Schmalz, HG New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology. ACS Med Chem Lett 7: 188-91 (2016)
- Jiang, J; Zhang, H; Wang, C; Zhang, Q; Fang, S; Zhou, R; Hu, J; Zhu, J; Zhou, Y; Luo, C; Zheng, C 1-Phenyl-dihydrobenzoindazoles as novel colchicine site inhibitors: Structural basis and antitumor efficacy. Eur J Med Chem 177: 448-456 (2019)
- Lucena-Agell, D; Guillén, MJ; Matesanz, R; Álvarez-Bernad, B; Hortigüela, R; Avilés, P; Martínez-Díez, M; Santamaría-Núñez, G; Contreras, J; Plaza-Menacho, I; Giménez-Abián, JF; Oliva, MA; Cuevas, C; Díaz, JF PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin. J Med Chem 67: 2619-2630 (2024)
- Choudhary, S; Kaku, K; Robles, AJ; Hamel, E; Mooberry, SL; Gangjee, A Simple monocyclic pyrimidine analogs as microtubule targeting agents binding to the colchicine site. Bioorg Med Chem 82: (2023)
- Zhang, X; Zhang, J; Tong, L; Luo, Y; Su, M; Zang, Y; Li, J; Lu, W; Chen, Y The discovery of colchicine-SAHA hybrids as a new class of antitumor agents. Bioorg Med Chem 21: 3240-4 (2013)
- Li, X; Wu, H; Feng, KW; Xu, J; Wu, S; Zhou, ZZ; Li, XF Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors. Bioorg Med Chem 73: (2022)
- Cosentino, L; Redondo-Horcajo, M; Zhao, Y; Santos, AR; Chowdury, KF; Vinader, V; Abdallah, QM; Abdel-Rahman, H; Fournier-Dit-Chabert, J; Shnyder, SD; Loadman, PM; Fang, WS; Díaz, JF; Barasoain, I; Burns, PA; Pors, K Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties. J Med Chem 55: 11062-6 (2012)
- Brossi, A Alfred Burger award address. Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine. J Med Chem 33: 2311-9 (1990)
- Zhang, X; Kong, Y; Zhang, J; Su, M; Zhou, Y; Zang, Y; Li, J; Chen, Y; Fang, Y; Zhang, X; Lu, W Design, synthesis and biological evaluation of colchicine derivatives as novel tubulin and histone deacetylase dual inhibitors. Eur J Med Chem 95: 127-35 (2015)
- Lin, S; Du, T; Zhang, J; Wu, D; Tian, H; Zhang, K; Jiang, L; Lu, D; Sheng, L; Li, Y; Ji, M; Chen, X; Xu, H Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. J Med Chem 65: 16372-16391 (2022)
- Hahn, KM; Humphreys, W; Helms, AM; Hastie, SB; Macdonald, TL Structural requirements for the binding of colchicine analogs to tubulin: the role of the C-10 substituent Bioorg Med Chem Lett 1: 471-476 (1991)
- Li, W; Shuai, W; Sun, H; Xu, F; Bi, Y; Xu, J; Ma, C; Yao, H; Zhu, Z; Xu, S Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site. Eur J Med Chem 163: 428-442 (2019)
- Banerjee, M; Poddar, A; Mitra, G; Surolia, A; Owa, T; Bhattacharyya, B Sulfonamide drugs binding to the colchicine site of tubulin: thermodynamic analysis of the drug-tubulin interactions by isothermal titration calorimetry. J Med Chem 48: 547-55 (2005)
- Zhang, SX; Feng, J; Kuo, SC; Brossi, A; Hamel, E; Tropsha, A; Lee, KH Antitumor agents. 199. Three-dimensional quantitative structure-activity relationship study of the colchicine binding site ligands using comparative molecular field analysis. J Med Chem 43: 167-76 (2000)
- Jiang, J; Zhang, Q; Guo, J; Fang, S; Zhou, R; Zhu, J; Chen, X; Zhou, Y; Zheng, C Synthesis and biological evaluation of 7-methoxy-1-(3,4,5-trimethoxyphenyl)-4,5-dihydro-2H-benzo[e]indazoles as new colchicine site inhibitors. Bioorg Med Chem Lett 29: 2632-2634 (2019)
- Romagnoli, R; Baraldi, PG; Salvador, MK; Prencipe, F; Lopez-Cara, C; Schiaffino Ortega, S; Brancale, A; Hamel, E; Castagliuolo, I; Mitola, S; Ronca, R; Bortolozzi, R; Porcù, E; Basso, G; Viola, G Design, synthesis, in vitro, and in vivo anticancer and antiangiogenic activity of novel 3-arylaminobenzofuran derivatives targeting the colchicine site on tubulin. J Med Chem 58: 3209-22 (2015)
- Liu, YN; Wang, JJ; Ji, YT; Zhao, GD; Tang, LQ; Zhang, CM; Guo, XL; Liu, ZP 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. J Med Chem 59: 5341-55 (2016)
- Ren, Y; Wang, Y; Liu, J; Liu, T; Yuan, L; Wu, C; Yang, Z; Chen, J X-ray Crystal Structure-Guided Discovery of Novel Indole Analogues as Colchicine-Binding Site Tubulin Inhibitors with Immune-Potentiating and Antitumor Effects against Melanoma. J Med Chem 66: 6697-6714 (2023)
- Cushman, M; He, HM; Katzenellenbogen, JA; Lin, CM; Hamel, E Synthesis, antitubulin and antimitotic activity, and cytotoxicity of analogs of 2-methoxyestradiol, an endogenous mammalian metabolite of estradiol that inhibits tubulin polymerization by binding to the colchicine binding site. J Med Chem 38: 2041-9 (1995)
- Mahboobi, S; Sellmer, A; Höcher, H; Eichhorn, E; Bär, T; Schmidt, M; Maier, T; Stadlwieser, JF; Beckers, TL [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. J Med Chem 49: 5769-76 (2006)
- ChEMBL_211871 (CHEMBL819253) Inhibition of colchicine binding(ICB). [3H]colchicine concentration was 5 uM
- ChEMBL_212012 (CHEMBL816886) Percent inhibition of colchicine binding(ICB) at 5 uM [3H]colchicine concentration
- ChEMBL_212055 (CHEMBL815360) Compound was tested for competitive inhibition with radioligand [3H]colchicine at colchicine site of mammalian tubulin
- ChEMBL_967216 (CHEMBL2400153) Competitive binding affinity to pig brain tubulin colchicine binding site after 1 hr by mass spectrophotometric analysis in presence of colchicine
- ChEBML_211170 Activity towards binding at colchicine site of bovine brain tubulin
- ChEMBL_211665 (CHEMBL821417) Binding affinity against tubulin using [3H]colchicine as radioligand
- ChEMBL_211669 (CHEMBL821421) Binding affinity against tubulin usingf [3H]-colchicine as radioligand
- ChEMBL_211170 (CHEMBL817535) Activity towards binding at colchicine site of bovine brain tubulin
- ChEMBL_211870 (CHEMBL819252) Inhibition of colchicine binding(ICB). Tubulin concentration was 1 uM
- ChEMBL_212205 (CHEMBL817768) Inhibition of tubulin polymerization interacting at the colchicine binding site
- ChEMBL_212206 (CHEMBL817769) Inhibition of tubulin polymerization interacting at the colchicine binding site.
- ChEMBL_302732 (CHEMBL838680) Binding affinity against tubulin from goat brain relative to colchicine
- ChEMBL_311916 (CHEMBL834683) Inhibition of tubulin polymerization interacting at the colchicine binding site.
- ChEMBL_211685 (CHEMBL819856) Ability to inhibit the binding of [3H]colchicine to porcine tubulin
- ChEMBL_496040 (CHEMBL998470) Displacement of [3H]Colchicine from pig biotinylated tubulin after 2 hrs by SPA
- ChEMBL_1625349 (CHEMBL3867818) Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 50 nM after 72 hrs by MTT assay (Rvb = 487.57 +/- 30.54 nM)
- ChEMBL_1625350 (CHEMBL3867819) Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 100 nM after 72 hrs by MTT assay (Rvb = 487.57 +/- 30.54 nM)
- ChEMBL_1625351 (CHEMBL3867820) Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 200 nM after 72 hrs by MTT assay (Rvb = 487.57 +/- 30.54 nM)
- ChEMBL_1625352 (CHEMBL3867821) Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 500 nM after 72 hrs by MTT assay (Rvb = 487.57 +/- 30.54 nM)
- ChEMBL_1625353 (CHEMBL3867822) Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 487.57 +/- 30.54 nM)
- ChEMBL_1625397 (CHEMBL3867866) Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 50 nM after 72 hrs by MTT assay (Rvb = 1607.50 +/- 497.42 nM)
- ChEMBL_1625398 (CHEMBL3867867) Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 100 nM after 72 hrs by MTT assay (Rvb = 1607.50 +/- 497.42 nM)
- ChEMBL_1625399 (CHEMBL3867868) Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 200 nM after 72 hrs by MTT assay (Rvb = 1607.50 +/- 497.42 nM)
- ChEMBL_1625400 (CHEMBL3867869) Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 500 nM after 72 hrs by MTT assay (Rvb = 1607.50 +/- 497.42 nM)
- ChEMBL_1625401 (CHEMBL3867870) Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of colchicine-induced cytotoxicity by measuring colchicine IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 1607.50 +/- 497.42 nM)
- ChEMBL_2135231 (CHEMBL4844841) Inhibition of ABCB1 (unknown origin) expressed in HEK293T cells assessed as reduction in colchicine IC50 at 0.5 uM pre-incubated for 4 hrs followed by colchicine addition and measured after 72 hrs by MTT assay
- ChEMBL_2135232 (CHEMBL4844842) Inhibition of ABCB1 (unknown origin) expressed in HEK293T cells assessed as reduction in colchicine IC50 at 1 uM pre-incubated for 4 hrs followed by colchicine addition and measured after 72 hrs by MTT assay
- ChEMBL_2135233 (CHEMBL4844843) Inhibition of ABCB1 (unknown origin) expressed in HEK293T cells assessed as reduction in colchicine IC50 at 2 uM pre-incubated for 4 hrs followed by colchicine addition and measured after 72 hrs by MTT assay
- ChEMBL_1546323 (CHEMBL3748554) Displacement of [3H]-colchicine from biotinylated porcine tubulin after 2 hrs by competitive binding assay
- ChEMBL_211691 (CHEMBL820473) In vitro inhibitory concentration required to displace [3H]colchicine from its binding site on Tubulin
- ChEMBL_211692 (CHEMBL820474) In vitro inhibitory concentration required to displace [3H]colchicine from its binding site on tubulin
- ChEMBL_211688 (CHEMBL819859) Concentration required to cause 50% decrease in the binding of [3H]colchicine from purified porcine tubulin.
- ChEMBL_1814005 (CHEMBL4313579) Inhibition of [3H] colchicine binding to bovine brain tubulin incubated for 30 mins by scintillation proximity assay
- ChEMBL_761290 (CHEMBL1816744) Displacement of [3H]colchicine from biotinylated pig brain tubulin after 2 hrs by competitive scintillation proximity assay
- ChEBML_212054 Compound was evaluated for its ability to inhibit the binding of [3H]-colchicine to tubulin in competitive binding assay
- ChEMBL_1454886 (CHEMBL3364189) Displacement of [3H]colchicine from bovine brain tubulin assessed as rate of assembly after 10 mins by liquid scintillation counting
- ChEMBL_1995641 (CHEMBL4629536) Reversal of human ABCB1-mediated multidrug resistance in HEK293/MDR19 cells assessed as effect on colchicine-induced cytotoxicity at 3 uM by measuring colchine IC50 after 72 hrs by CCK8 assay (Rvb = 97.58 +/- 17.62 uM)
- ChEMBL_1995642 (CHEMBL4629537) Reversal of human ABCB1-mediated multidrug resistance in HEK293/MDR19 cells assessed as effect on colchicine-induced cytotoxicity at 2 uM by measuring colchine IC50 after 72 hrs by CCK8 assay (Rvb = 97.58 +/- 17.62 uM)
- ChEMBL_1995643 (CHEMBL4629538) Reversal of human ABCB1-mediated multidrug resistance in HEK293/MDR19 cells assessed as effect on colchicine-induced cytotoxicity at 1 uM by measuring colchine IC50 after 72 hrs by CCK8 assay (Rvb = 97.58 +/- 17.62 uM)
- ChEMBL_1995644 (CHEMBL4629539) Reversal of human ABCB1-mediated multidrug resistance in HEK293/MDR19 cells assessed as effect on colchicine-induced cytotoxicity at 0.5 uM by measuring colchine IC50 after 72 hrs by CCK8 assay (Rvb = 97.58 +/- 17.62 uM)
- ChEMBL_2377198 Displacement of fluorescent probe (R)-(+)-ethyl 5-amino2-methyl-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-ylcarbamate from calf brain tubulin colchicine binding site assessed as dissociation constant at 0.05 to 70 uM incubated for 30 mins by fluorescence based assay
