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

Autor: Gui-Lin, Yin, Yan, Li, Ke, Tang, Xiao-Feng, Jin, Xiao-Guang, Chen, Li, Li, Zhi-Qiang, Feng
Rok vydání: 2014
Předmět:
Zdroj: Yao xue xue bao = Acta pharmaceutica Sinica. 49(6)
ISSN: 0513-4870
Popis: 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 x 10(-8) mol x L(-1) against U87-MG and HCT116 respectively. The structure-activity relationship of compounds was also discussed preliminarily.
Databáze: OpenAIRE