Synthesis of Novel Benzothiazole-Piperazine Derivatives and Their Biological Evaluation as Acetylcholinesterase Inhibitors and Cytotoxic Agents
| Autor: | Tugba Ercetin, Rengul Cetin Atalay, Wolfgang Sippl, Bengisu Turgutalp, Mustafa Fethi Sahin, Hayrettin Ozan Gulcan, Mine Yarim, Irem Durmaz, Quoc Dat Nguyen, Enise Ece Gurdal |
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| Rok vydání: | 2018 |
| Předmět: |
Cancer Research
Sulforhodamine B Pharmacology 01 natural sciences Structure-Activity Relationship chemistry.chemical_compound Cell Line Tumor Humans Donepezil Benzothiazoles Cytotoxicity Piperazine Butyrylcholinesterase Spectrum Analysis Acetylcholinesterase digestive system diseases In vitro 0104 chemical sciences Molecular Docking Simulation 010404 medicinal & biomolecular chemistry chemistry Benzothiazole Docking (molecular) Molecular Medicine Cholinesterase Inhibitors Drug Screening Assays Antitumor |
| Zdroj: | Anti-Cancer Agents in Medicinal Chemistry. 17 |
| ISSN: | 1871-5206 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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