Design, synthesis and activities of novel benzothiazole derivatives containing arylpiperazine.
- Author:
Wen-Hu LIU
1
;
Jin-Xia CHANG
;
Yi LIU
;
Jie-Wei LUO
;
Jian-Wu ZHANG
Author Information
1. Department of Pharmacology, North Sichuan Medical College, Nanchong 637007, China.
- 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;
Inhibitory Concentration 50;
Molecular Structure;
Piperazines;
chemistry;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2013;48(8):1259-1265
- CountryChina
- Language:Chinese
-
Abstract:
Twenty-four novel benzothiazole derivatives containing arylpiperazine were designed and synthesized by bioisosterism principle. Anti-proliferative effect of these synthesized compounds against four cancer cell and two normal cell lines were evaluated in vitro by the standard MTT assay. Pharmacological test showed that most of the compounds exhibited potent antitumor activity. Some of the compounds (II2, II3, II6, II7) showed strong anti-proliferation activities against HepG2 and HeLa229 cell lines with the IC 50 values of 1.6-4.5 micromol x L(-1) and 2.5-5.3 micromol x L(-1), respectively, and compounds having cyan in p-substituted benzene ring (I4, I8, I12, II4, II8 and II12) were found to have better antitumor activities against AsPC-1 cell lines with the IC50 values of 5.2-11.3 micromol x L(-1). The structure-activity relationship of benzothiazole derivatives containing arylpiperazine was also discussed preliminarily.
