Design,Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents |
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Authors: | MA Junjie HU Gang XIE Lijun CHEN Lei XU Boxuan GONG Ping |
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Institution: | 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 |
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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. |
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Keywords: | Benzothiazole Semicarbazone Antitumor activity |
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