Synthesis of Novel Benzothiazole-Piperazine Derivatives and Their Biological Evaluation as Acetylcholinesterase Inhibitors and Cytotoxic Agents
2018
A new series of benzothiazole-piperazine derivatives were
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. 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 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.
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