Synthesis and Anticancer Activity Evaluation of Some Benzothiazole-Piperazine Derivatives

Author(s):

Enise Ece Gurdal, Ebru Buclulgan, Irem Durmaz, Rengul Cetin-Atalay and Mine Yarim   Pages 382 - 389 ( 8 )

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.

Keywords:

Anticancer, apoptosis, benzothiazole, cytotoxicity, piperazine, sulphorhodamine B.

Affiliation:

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University, 34755, Kayisdagi, Istanbul, Turkey.

Graphical Abstract:

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