- 英文名称
- thiocolchicine
- 分子式
- C22H25NO5S
- 分子量
- 415.5
- 中文别名
- 硫秋水仙碱; 硫秋水仙素EP杂质B; 硫秋水仙苷杂质B; (S)-N-(1,2,3-三甲氧基-10-(甲硫基)-9-氧代-5,6,7,9-四氢苯并[a]庚搭烯-7-基)乙酰胺; thiocholchicine; (S)-7-Acetylamino-6,7-dihydro-10-methylthio-1,2,3-trimethoxybenzo[a]heptalen-9(5H)-one; (S)-7α-Acetylamino-6,7-dihydro-10-(methylthio)-1,2,3-trimethoxybenzo[a]heptalene-9(5H)-one; 10-Demethoxy-10-methylthiocolchicine; N-[(S)-5,6,7,9-Tetrahydro-1,2,3-trimethoxy-10-methylthio-9-oxobenzo[a]heptalen-7-yl]acetamide; N-[(7S)-5,6,7,9-Tetrahydro-1,2,3-triMethoxy-10-(Methylthio)-9-oxobenzo[a]heptalen-7-yl]acetaMide; thiocolhicine; N-[(7S)-1,2,3-trimethoxy-10-methylsulfanyl-9-oxo-6,7-dihydro-5H-benzo[a]heptalen-7-yl]acetamide; N-[(7S)-1,2,3-trimethoxy-10-methylsulfanyl-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide; N-((S)-1,2,3-trimethoxy-10-methylsulfanyl-9-oxo-5,6,7,9-tetrahydro-benzo[a]heptalen-7-yl)-acetamide; Colchicine,10-thio; N-((S)-1,2,3-Trimethoxy-10-methylmercapto-9-oxo-5,6,7,9-tetrahydro-benzo[a]heptalen-7-yl)-acetamid; Colchicine,10-demethoxy-10-(methylthio)
- 用途
- - 生物活性
Thiocolchicine 是秋水仙碱 (HY-16569) 的衍生物，是一种有效的微管蛋白聚合 (tubulin polymerization) 抑制剂 (IC50=2.5 µM)，竞争性结合微管蛋白 (Ki=0.7 µM)。Thiocolchicine 可以作为 ADC 的毒素分子。
- 体外研究
Thiocolchicine is against MCF-7, LoVo, LoVo/DX, A-549 and BALB/3T3 cells with IC
50
values of 0.01 μM, 0.021 μM, 0.398 μM, 0.011 μM and 0.114 μM, respectively.Thiocolchicine (1 nM-100 μM; 24-72 hours) shows a relationship between cell cycle blocking activity and growth inhibition in breast cancer cells. It inhibits cell proliferation of MDA-MB-231 and multidrug resistant (MDR) MCF-7 ADRr breast cancer cells with IC
50
s of 0.6 nM and 400 nM, respectively, as well as MDR CEM-VBL leukemia cells (IC
50
=50 nM).
