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
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.
Keywords: Acetylcholinesterase, benzothiazole, cytotoxicity, docking, Ellman's method, piperazine, Sulforhodamine B.
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