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

doi:10.1007/s40242-015-5034-1

高等学校化学研究 ›› 2015, Vol. 31 ›› Issue (6): 958-963.doi: 10.1007/s40242-015-5034-1

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

收稿日期:2015-01-26 修回日期:2015-03-31 出版日期:2015-11-01 发布日期:2015-04-27
通讯作者: GONG Ping E-mail:gongpinggp@126.com
基金资助:
Supported by the Program for Liaoning Excellent Talents in University, China(No.LR2014030) and the National Natural Science Foundation of China(No.81102470).

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).

摘要/Abstract

摘要：

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.

关键词: Benzothiazole, Semicarbazone, Antitumor activity

Abstract:

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]. 高等学校化学研究, 2015, 31(6): 958-963.

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

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

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