Design and optimization of piperlongumine analogs as potent senolytics
Bioorganic & medicinal chemistry letters(2024)
Abstract
Selective removal of senescent cells (SnCs) offers a promising therapeutic strategy to treat chronic and age -related diseases. Our prior investigations led to the discovery of piperlongumine (PL) and its derivatives as senolytic agents. In this study, our medicinal chemistry campaign on both the alpha,ll-unsaturated 8-valerolactam ring and the phenyl ring of PL culminated in the identification of compound 24, which exhibited an impressive 50-fold enhancement in senolytic activity against senescent WI-38 fibroblasts compared to PL.
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Key words
Piperlongumine,Cellular senescence,Senescent cells,Senolytics,Structure activity relationship
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