Synthesis and antitumor activity of 5-substituted-2-(pyridyl)benzothiazole compounds.
- Author:
Wen-Hu LIU
1
;
Jin-Xia CHANG
;
Yi LIU
Author Information
1. Department of Pharmacology, North Sichuan Medical College, Nanchong 637007, China. lwh790214@163.com
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Benzothiazoles;
chemical synthesis;
chemistry;
pharmacology;
Cell Line, Tumor;
Cell Proliferation;
drug effects;
Drug Screening Assays, Antitumor;
Humans;
Molecular Structure;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2013;48(1):83-88
- CountryChina
- Language:Chinese
-
Abstract:
Fifteen novel 5-substituted-2-(pyridyl)benzothiazole compounds were designed and synthesized by simple hydrolization and condensation reaction of the 2-amino-5-substituent benzothiazole. Activities of these synthesized compounds were evaluated on Bcap-37, HCT-15 and HepG2 tumor cells in vitro by standard MTT assay. 5-Fluorouracil (5-FU) was used as the positive control. The results revealed that most of the new compounds had potent effects on Bcap-37, HCT-15 and HepG2 tumor cells, and had no or less effect on 293T and L02 normal cells. Particularly, compounds 1c and 2e exhibited better activities on HCT-15 and HepG2 cells with IC50 values of 41.59 and 38.65 micromol x L(-1), and 1i showed excellent activities on Bcap-37 and HepG2 cells with IC50 values of 46.63 and 23.51 micromol x L(-1), respectively. The structure-activity relationship of 5-substituted-2-(pyridyl)benzothiazole compounds were also discussed preliminarily.
