Synthesis and biological evaluation of 2-(3-butynoicamidophenyl) benzothiazole derivatives as antitumor agents.
- Author:
Gui-Lin YIN
;
Yan LI
;
Ke TANG
;
Xiao-Feng JIN
;
Xiao-Guang CHEN
;
Li LI
;
Zhi-Qiang FENG
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
pharmacology;
Benzothiazoles;
chemical synthesis;
pharmacology;
Cell Line, Tumor;
Drug Screening Assays, Antitumor;
Humans;
Nitrobenzoates;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2014;49(6):888-895
- CountryChina
- Language:Chinese
-
Abstract:
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.
