期刊
BIOORGANIC CHEMISTRY
卷 97, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.103695
关键词
Tubulin polymerization inhibitors; Colchicine binding site; Anti-proliferative; Colorectal carcinoma
资金
- National SAMP
- T Major Special Project on Major New Drug Innovations of China [2018ZX09201018]
- Sichuan Provincial Science and Technology Program for Key Research and Development, China [2018SZ0007]
- Fundamental Research Funds for the Central Universities, China [2017SCU12046]
- (Postdoctoral Foundation of Sichuan University)
A series of 3-(((9H-purin-6-yl) amino) methyl) pyridin-2(1H)-one derivatives were designed, synthesized and confirmed as tubulin polymerization inhibitors. All compounds were evaluated for their anti-proliferative activities on three colorectal carcinoma (CRC) cell lines. Among these compounds, SKLB0565 displayed noteworthy potency against eight CRC cell lines with IC50 values ranging from 0.012 mu M and 0.081 mu M. Besides, SKLB0565 inhibited tubulin polymerization, caused G2/M phase cell cycle arrest, depolarized mitochondria and induced cell apoptosis in CRC cells. Furthermore, SKLB0565 suppressed cell migration and disrupted the capillary tube formation of human umbilical vein endothelial cells (HUVECs). Our data clarified that SKLB0565 is a promising anti-tubulin agent for CRC therapy which is worthy of further evaluation.
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