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Design, synthesis and biological evaluation of novel benzothiazole derivatives bearing semicarbazone moiety as antitumor agents

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Design, synthesis and biological evaluation of novel benzothiazole derivatives bearing semicarbazone moiety as antitumor agents

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产品描述
作者
Junjie Ma;Gang Hu;Lijun Xie;Lei Chen;Boxuan Xu;Ping Gong*
刊物名称
Chemical Research in Chinese Universities
2015
31
6
958-963

{Author}: Junjie Ma;Gang Hu;Lijun Xie;Lei Chen;Boxuan Xu;Ping Gong*

{Journal}: Chemical Research in Chinese Universities

{Year}: 2015

{Volume}: 31

{Issue}: 6

{Pages}:958-963

{Keywords}: Benzothiazole;Semicarbazone;Antitumor activity

{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 12 a― 12 i with fluoro-substituted benzyl-1 H -indole moiety displayed more potent activity than those with phenyl moiety. The most promising compound 12 d exhibited excellent antitumor activity with IC<sub>50</sub> values of 0.015, 0.28, 1.53 and 0.68 μmol/L against the four tested cell lines respectively.

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