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- W4309236475 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 (IC 50 range from = 0.071 - 0.303 μM, respectively). • Molecular docking and in silico ADME predictions were also performed. A novel series of benzophenone hydrazone derivatives were synthesized and evaluated for their antiproliferative activity. The thiosemicarbazone derivative 5c and guanylhydrazone derivatives 6d-f showed potent antiproliferative activities against A498 renal cancer cells with IC 50 = 14.5, 0.28, 0.30 and 0.3 μM, respectively. Compounds 5c, 6d, 6e and 6f showed inhibitory activities against cathepsin L and cathepsin B (IC 50 ranged from 0.071 to 0.303 μM. A mechanistic study revealed that compound 6e induced apoptosis on A498 cell line by 38.02% compared to 1.64% in control. This apoptotic effect was supported by an 8.58-fold increase in the level of caspase-3 compared to the control cells. Additionally, compound 6e inhibited A498 cell growth mostly at the S phase. Furthermore, molecular modeling studies showed that compound 6e possessed good fitting with cathepsin L and cathepsin B binding sites through their interaction with essential amino acids through hydrophobic H-bonding interactions. Therefore, compound 6e could be considered as a prospective anticancer lead compound and it worth further exploration/optimization as an antiproliferative agent via cathepsins inhibition." @default.
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- W4309236475 date "2023-02-01" @default.
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- W4309236475 title "Design, synthesis and mechanistic studies of benzophenones hydrazone derivatives as cathepsin inhibitors" @default.
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- W4309236475 doi "https://doi.org/10.1016/j.molstruc.2022.134583" @default.
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