Synthesis and anticancer activity evaluation of some benzothiazole-piperazine derivatives
Date
2015
Authors
Gurdal, E.E.
Buclulgan, E.
Durmaz I.
Cetin-Atalay, R.
Yarim, M.
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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. © 2015 Bentham Science Publishers.
Source Title
Anti-Cancer Agents in Medicinal Chemistry
Publisher
Bentham Science Publishers B.V.
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Keywords
Anticancer, Apoptosis, Benzothiazole, Cytotoxicity, Piperazine, Sulphorhodamine B, benzothiazole derivative, flurouracil, n (4 methyl 1,3 benzothiazol 2 yl) 2 (4 acetylpiperazin 1 yl)acetamide, n (4 methyl 1,3 benzothiazol 2 yl) 2 (4 benzoylpiperazin 1 yl)acetamide, n (4 methyl 1,3 benzothiazol 2 yl) 2 [4 (2 furoyl)piperazin 1 yl]acetamide, n (4 methylbenzothiazol 2 yl) 2 (4 chlorobenzylpiperazin 1 yl)acetamide, n (4 methylbenzothiazol 2 yl) 2 (4 methylpiperazin 1 yl)acetamide, n (4 methylbenzothiazol 2 yl) 2 [1 (4 methylphenyl)piperazine 1 yl)acetamide, n (4 methylbenzothiazol 2 yl) 2 [4 (2 hydroxyphenyl)piperazin 1 yl)]acetamide, n (4 methylbenzothiazol 2 yl) 2 [4 (3,4 dichlorophenyl)piperazin 1 yl]acetamide, n (4 methylbenzothiazol 2 yl) 2 [4 (4 fluorophenyl)piperazin 1 yl]acetamide, n (4 methylbenzothiazol 2 yl) 2 [4 (4 nitrophenyl)piperazin 1 yl]acetamide, piperazine derivative, unclassified drug, antineoplastic agent, benzothiazole, benzothiazole derivative, piperazine, piperazine derivative, antineoplastic activity, apoptosis, Article, bioassay, carbon nuclear magnetic resonance, cell cycle arrest, controlled study, cytotoxicity, drug structure, drug synthesis, fluorescence activated cell sorting, Hoechst staining, human, human cell, infrared spectroscopy, proton nuclear magnetic resonance, sulphorhodamine B assay, cell cycle, cell death, cell proliferation, chemical structure, chemistry, dose response, drug effects, drug screening, HCT116 cell line, MCF 7 cell line, structure activity relation, synthesis, tumor cell culture, Antineoplastic Agents, Benzothiazoles, Cell Cycle, Cell Death, Cell Proliferation, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, HCT116 Cells, Humans, MCF-7 Cells, Molecular Structure, Piperazines, Structure-Activity Relationship, Tumor Cells, Cultured
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Language
English