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.