Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents

doi:10.1007/s40242-015-5034-1

Chemical Research in Chinese Universities ›› 2015, Vol. 31 ›› Issue (6): 958-963.doi: 10.1007/s40242-015-5034-1

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Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents

MA Junjie¹, HU Gang¹, XIE Lijun², CHEN Lei¹, XU Boxuan¹, GONG Ping¹

1. Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China;
2. Fujian Institute of Microbiology, Fuzhou 350007, P. R. China

Received:2015-01-26 Revised:2015-03-31 Online:2015-11-01 Published:2015-04-27
Contact: GONG Ping E-mail:gongpinggp@126.com
Supported by:
Supported by the Program for Liaoning Excellent Talents in University, China(No.LR2014030) and the National Natural Science Foundation of China(No.81102470).

Abstract

Abstract:

A series of novel benzothiazole derivatives bearing semicarbazone as a linker was designed and synthesized, and their in vitro antitumor activities were evaluated against four cancer cell lines(HT29, H460, A549 and MDA-MB-231). Most of them showed moderate to excellent activity against all the tested cell lines. Among them, compounds 12a―12i with fluoro-substituted benzyl-1H-indole moiety displayed more potent activity than those with phenyl moiety. The most promising compound 12d exhibited excellent antitumor activity with IC₅₀ values of 0.015, 0.28, 1.53 and 0.68 μmol/L against the four tested cell lines respectively.

Key words: Benzothiazole, Semicarbazone, Antitumor activity

MA Junjie, HU Gang, XIE Lijun, CHEN Lei, XU Boxuan, GONG Ping. Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents[J]. Chemical Research in Chinese Universities, 2015, 31(6): 958-963.

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Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents

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