Guanglong Bao, Baoquan Du, Yuxiu Ma, Meng Zhao, Ping Gong and Xin Zhai Pages 489 - 498 ( 10 )
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.
Benzothiazole, semicarbazone, synthesis, antiproliferative activity.
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.