Synthesis and biological evaluation of 2-(3-butynoicamidophenyl) benzothiazole derivatives as antitumor agents

A series of 2-(3-butynoicamidophenyl)benzothiazole derivatives were synthesized starting from 4-fluoro-3-nitrobenzoic acid.Structures of all the synthesized compounds were confirmed by ¹H NMR and HR-MS.Their antitumor activities against human tumor cells lines (HCT116, Mia-PaCa2, U87-MG, A549, NCI-H1975) were evaluated by MTT assay.The results revealed that most of the synthesized compounds showed potent activities against HCT116, Mia-PaCa2, U87-MG tumor cells lines.Particularly, compounds 14c and 14h exhibited better activity with IC₅₀ values of 1×10^-8 mol·L^-1 against U87-MG and HCT116 respectively.The structure-activity relationship of compounds was also discussed preliminarily.