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- W3198060595 abstract "The antiapoptotic protein B-cell lymphoma 2 (Bcl-2), overexpressed in many tumor cells, is an attractive target for potential small molecule anticancer drug discovery. Herein, a series of novel derivatives with acyl sulfonamide skeleton was designed, synthesized, and evaluated as Bcl-2 inhibitors by means of bioisosteric replacement. Among them, compound 24g demonstrated equal efficient inhibition activity against RS4;11 cell line compared to positive control ABT-199. Moreover, it showed improved selectivity for Bcl-2/Bcl-xL inhibitory effects, the result of which was consistent with platelet toxicity studies. In vitro and in vivo pharmacokinetic properties of compound 24g had a significantly improved profiles. Taken together, those results suggested it as a promising candidate for development of novel therapeutics targeting Bcl-2 in cancer." @default.
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- W3198060595 date "2021-10-01" @default.
- W3198060595 modified "2023-09-26" @default.
- W3198060595 title "Discovery of potent and selective Bcl-2 inhibitors with acyl sulfonamide skeleton" @default.
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- W3198060595 doi "https://doi.org/10.1016/j.bmc.2021.116350" @default.
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