4.4 Article

Synthesis and Anticancer Activity Evaluation of Some Benzothiazole-Piperazine Derivatives

Journal

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
Volume 15, Issue 3, Pages 382-389

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1871520615666141216151101

Keywords

Anticancer; apoptosis; benzothiazole; cytotoxicity; piperazine; sulphorhodamine B

Funding

  1. Scientific & Technological Research Council of Turkey (TUBITAK) [114S115]

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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. HN

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