期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 223, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113656
关键词
Cancer; Cytotoxicity; Indole; isoCA-4; Oxazinoindole; Pyridoindole; Quinazoline; Tubulin
资金
- CNRS
- University Paris-Saclay
- La Ligue contre le Cancer
- Spanish Ministry of Science, Innovation and Universities [RTI2018-099474-BI00]
- EU's European Regional Development Fund FEDER
- National Research Foundation (NRF) of Korea [019R1A2C1009231]
- Brain Korea (BK21) FOUR program
- Creative-Pioneering Researchers Program at Seoul National University [370C20160062]
In this study, various ligands related to Combretastatin A-4 and isoCombretastatin A-4 were designed, synthesized, and evaluated for their ability to inhibit tubulin polymerization. The lead compound 15d showed remarkable sub-nanomolar cytotoxicity against 9 human cancer cell lines, with an IC50 value below 1 nM.
In this study, a variety of original ligands related to Combretastatin A-4 and isoCombretastatin A-4, able to inhibit the tubulin polymerization into microtubules, was designed, synthesized, and evaluated. Our lead compound 15d having a quinazoline as A-ring and a 2-substituted indole as B-ring separated by a N-methyl linker displayed a remarkable sub-nanomolar level of cytotoxicity (IC50 < 1 nM) against 9 human cancer cell lines. (C) 2021 Elsevier Masson SAS. All rights reserved.
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
分享论文
