Synthesis, anti-cancer evaluation of benzenesulfonamide derivatives as potent tubulin-targeting agents

被引：28
|
作者：
Yang, Jun [1 ]
Yang, Simin [1 ]
Zhou, Shanshan [1 ]
Lu, Dongbo [1 ]
Ji, Liyan [1 ]
Li, Zhongjun [1 ]
Yu, Siwang [1 ]
Meng, Xiangbao [1 ]
机构：
[1] Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 122卷
基金：
中国国家自然科学基金;
关键词：
Tubulin-targeting agents; Sulfonamides; Benzoxazepine; Benzodiazepine; Benzothiazepine; CANCER-CELL; DISCOVERY; POLYMERIZATION; MICROTUBULES; INHIBITORS; INSIGHT; GROWTH;
D O I：
10.1016/j.ejmech.2016.07.002
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of benzenesulfonamide derivatives were synthesized and evaluated for their anti-proliferative activity and interaction with tubulin. These new derivatives showed significant activities against cellular proliferative and tubulin polymerization. Compound BA-3b proved to be the most potent compound with IC50 value ranging from 0.007 to 0.036 mu M against seven cancer cell lines, and three drug-resistant cancer cell lines, which indicated a promising anti-cancer agent. The target tubulin was also verified by dynamic tubulin polymerization assay and tubulin intensity assay. (C) 2016 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：488 / 496
页数：9
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