Synthesis and anticancer activity evaluation of some benzothiazole-piperazine derivatives

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Author
Gurdal, E.E.
Buclulgan, E.
Durmaz I.
Cetin-Atalay, R.
Yarim, M.
Date
2015
Source Title
Anti-Cancer Agents in Medicinal Chemistry
Print ISSN
18715206
Publisher
Bentham Science Publishers B.V.
Volume
15
Issue
3
Pages
382 - 389
Language
English
Type
Article
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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.
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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http://hdl.handle.net/11693/24159
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