Design, synthesis and mechanistic studies of benzophenones hydrazone derivatives as cathepsin inhibitors

Journal of Molecular Structure(2023)

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Abstract
•A series of benzophenone hydrazones have been designed and synthesized.•Compounds were evaluated for their in vitro antiproliferative activity against NCI 60 cancer cell line plate.•Compounds 5c, 6d, 6e, and 6f displayed the most promising NCI preliminary screening were selected for further assessment at five doses concentrations (0.01, 0.1, 1, 10, 100 µM).•Compounds 5c, 6d, 6e, and 6f were also evaluated for their cathepsin L and cathepsin B inhibitory activities in which they showed good activity against both enzymes (IC50 range from = 0.071 - 0.303 µM, respectively).•Molecular docking and in silico ADME predictions were also performed.
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Key words
Benzophenones,Hydrazones,Antiproliferative,Cathepsins,Cell cycle,Caspase -3
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