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Design, Synthesis and Antiproliferative Activity of Novel Benzothiazole Derivatives Conjugated with Semicarbazone Scaffold

[ Vol. 12 , Issue. 5 ]

Author(s):

Guanglong Bao, Baoquan Du, Yuxiu Ma, Meng Zhao, Ping Gong and Xin Zhai   Pages 489 - 498 ( 10 )

Abstract:


Two series of novel benzothiazole derivatives conjugated with semicarbazone scaffold were designed and synthesized through a structure-based molecular hybridization strategy. All the target compounds were evaluated for their cytotoxicity in vitro against three cancer cell lines (HT-29, MKN-45 and H460) by standard MTT assay. The pharmacological results indicated that seven compounds (17h-n) exhibited comparable or even better antiproliferative activity in comparison with reference drugs Sorafenib and PAC-1. Particularly, compound 17i displayed remarkable cytotoxicity against tested three cancer cell lines with IC50 values of 0.84, 0.06 and 0.52 µM, which were 4.3-, 36.6-, 4.2-folds more potent than Sorafenib and 1.2-, 13.7-, 6.9-times more active than PAC-1, respectively.

Keywords:

Benzothiazole, semicarbazone, synthesis, antiproliferative activity.

Affiliation:

School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.



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