Title:Synthesis and Anticancer Activity Evaluation of Some Benzothiazole-Piperazine Derivatives
VOLUME: 15 ISSUE: 3
Author(s):Enise Ece Gurdal, Ebru Buclulgan, Irem Durmaz, Rengul Cetin-Atalay and Mine Yarim
Affiliation:Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University, 34755, Kayisdagi, Istanbul, Turkey.
Keywords:Anticancer, apoptosis, benzothiazole, cytotoxicity, piperazine, sulphorhodamine B.
Abstract:Synthesis, characterization and cytotoxic activities of ten benzothiazole-piperazine derivatives were
reported. In vitro cytotoxic activities of compounds were screened against hepatocellular (HUH-7), breast (MCF-7)
and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. Based on the GI50 values of the compounds,
most of the benzothiazole-piperazine derivatives are active against HUH-7, MCF-7 and HCT-116 cancer cell lines.
Aroyl substituted compounds 1h and 1j were found to be the most active derivatives. In addition, further investigation
of compounds 1h and 1j by Hoechst staining and FACS revealed that these compounds cause apoptosis by cell cycle
arrest at subG1 phase.
