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Rationale Design, Synthesis, Cytotoxicity Evaluation and Molecular Docking Studies of 3-Chloro-4-aryl-1-(phenazin-7-yl) Azetidin-2-ones Analogues

INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY(2022)

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摘要
2-phenazinamines (3-chloro-4-aryl-1-(phenazin-7-yl) azetidin-2-ones) possess a broad spectrum of biological activities. They were reported as antineoplastic agents. Hence it is of great interest to design newer 2- phenazinamine derivatives (3-chloro-4-aryl-1-(phenazin-7-yl) azetidin-2-ones) by molecular docking studies to evaluate their anticancer potential. The 2-phenazinamine derivatives (4a-e) were prepared with the reduction of 2, 4-dinitrodiphenylamine by adding tin chloride and catalytic agents (nitrobenzene and magnesium sulfate) fallowed by cyclization process, The in-vitro cytotoxic activity of all compounds (4a-e) carried on K562 human chronic myelogenous leukemia cell line by employing 3-(4,5-dimethylthiazol-2-4yl)-2,5-diphenyl tetrazolium bromide assay method. Molecular docking studies were done by using docking study for the assessment of their anticancer potential. All five compounds (4a-e) showed the best and lowest the binding energy scores among all of the ligands. Compound 4c showed binding energy of -7.99. Amongst the two series of 2- phenazinamines.
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关键词
Anticancer,Drug design,K562,Phenazinamines
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