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

Eur J Med Chem. 2016 Oct 21:122:488-496. doi: 10.1016/j.ejmech.2016.07.002.

Jun Yang ¹, Simin Yang ¹, Shanshan Zhou ¹, Dongbo Lu ¹, Liyan Ji ¹, Zhongjun Li ¹, Siwang Yu ², Xiangbao Meng ³

Affiliations

1 The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
2 The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: swang_yu@bjmu.edu.cn.
3 The State Key Laboratory of Natural and Biomimetic Drugs, Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. Electronic address: xbmeng@bjmu.edu.cn.

PMID: 27423028 DOI: 10.1016/j.ejmech.2016.07.002

Abstract

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 μM 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.

Keywords

Benzodiazepine; Benzothiazepine; Benzoxazepine; Sulfonamides; Tubulin-targeting agents.

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