Synthesis of Novel Benzothiazole-Piperazine Derivatives and Their Biological Evaluation as Acetylcholinesterase Inhibitors and Cytotoxic Agents.

Autor:	Gurdal EE; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University, 34755, Kayisdagi, Istanbul. Turkey., Turgutalp B; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University, 34755, Kayisdagi, Istanbul. Turkey., Gulcan HO; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Eastern Mediterranean University, Famagusta. Cyprus., Ercetin T; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Eastern Mediterranean University, Famagusta. Cyprus., Sahin MF; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Eastern Mediterranean University, Famagusta. Cyprus., Durmaz I; Bioinformatics Department, Graduate School of Informatics, Middle East Technical University, Ankara. Turkey., Atalay RC; Bioinformatics Department, Graduate School of Informatics, Middle East Technical University, Ankara. Turkey., Nguyen QD; Martin-Luther- Universität Halle-Wittenberg, Institute of Pharmacy, Medicinal Chemistry Department, Halle (Saale). Germany., Sippl W; Martin-Luther- Universität Halle-Wittenberg, Institute of Pharmacy, Medicinal Chemistry Department, Halle (Saale). Germany., Yarim M; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Yeditepe University, 34755, Kayisdagi, Istanbul. Turkey.
Jazyk:	angličtina
Zdroj:	Anti-cancer agents in medicinal chemistry [Anticancer Agents Med Chem] 2017; Vol. 17 (13), pp. 1837-1845.
DOI:	10.2174/1871520617666170412153604
Abstrakt:	Objective and Method: A new series of benzothiazole-piperazine derivatives was synthesized and a complete chemical characterization of the novel compounds was provided. In vitro cytotoxic activities were screened against colorectal (HCT-116), breast (MCF-7) and hepatocellular (Huh7) cancer cell lines by Sulforhodamine B assay. Result and Discussion: All compounds showed cytotoxic activity against hepatocellular (Huh7) and breast (MCF-7) cancer cell lines. Dihalo substituted benzylpiperazine derivatives (2a, 2e) had the highest cytotoxic activities in all the tested cell lines. In addition, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of synthesized compounds were investigated by in vitro Ellman's method. Compound 2j led to moderate and selective inhibition against AChE. Docking study was utilized to understand the binding mode of compound 2j in comparision with donepezil on AChE. The other tested compounds showed weak or no inhibition against AChE as promising anticancer agents. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)
Databáze:	MEDLINE
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