期刊
FUTURE MEDICINAL CHEMISTRY
卷 10, 期 24, 页码 2791-2814出版社
FUTURE SCI LTD
DOI: 10.4155/fmc-2018-0226
关键词
anticancer activity; apoptosis; -carboline; cell cycle arrest; docking; KSP; multitarget agents; National Cancer Institute; topoisomerase-I; triazoles
Aim: Some anticancer -carbolines exhibited dual inhibition of topo-I and KSP. Methodology/Results: Novel -carbolines were synthesized and screened for their anticancer activity according to the NCI protocol. Five dose assays results indicated that compounds 9, 10, 12, 17 and 20 were potent and non selective anticancer agents; the sulfanyltriazole 12 was the most potent. Compounds 10, 12 and 20 showed dual topo-I and KSP inhibition with compound 12 being the most potent. Active compounds elicited Pre-G1 apoptosis and cell cycle arrest at G2/M phase of melanoma MDA-MB-435 cells. Docking results, in silico physicochemical and absorption, distribution, metabolism, excretion (ADME) properties were appropriate. Conclusion: Compounds 10, 12 and 20 are potent apoptosis-inducing multitarget anticancer agents that act via dual inhibition of topo-I and KSP-ATPase.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据