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SIS3 is a specific inhibitor of Smad3 that inhibits the TGFβ1-induced phosphorylation of Smad3. In this article, a variety of SIS3 derivatives were designed and synthesized to discover potential inhibitors… Click to show full abstract
SIS3 is a specific inhibitor of Smad3 that inhibits the TGFβ1-induced phosphorylation of Smad3. In this article, a variety of SIS3 derivatives were designed and synthesized to discover potential inhibitors against P-glycoprotein-mediated multidrug resistance to cancer cells aided by late-stage functionalization of 2-(4-(pyridin-2-yl)phenoxy)pyridine analogue. A novel class of potent P-gp reversal agents were investigated and a lead compound 37 was identified as a potent P-gp reversal agent with strong bioactivity and outstanding affinity for ABCB1.
Journal Title: Journal of medicinal chemistry
Year Published: 2020
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