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.
Anti-Cancer Agents in Medicinal Chemistry
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:
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.
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Gurdal Ece Enise, Buclulgan Ebru, Durmaz Irem, Cetin-Atalay Rengul and Yarim Mine, Synthesis and Anticancer Activity Evaluation of Some Benzothiazole-Piperazine Derivatives, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (3) . https://dx.doi.org/10.2174/1871520615666141216151101
DOI https://dx.doi.org/10.2174/1871520615666141216151101 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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