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- W3208341234 abstract "CDK8 and its paralog CDK19 are cyclin-dependent kinases that are core components of the so-called Mediator complex that has essential roles as a positive and negative regulator of gene expression. Several efforts to develop inhibitors have yielded natural and synthetic ATP-competitive compounds including cortistatin A, Sel120, BCD-115, CCT251921 (1), and MSC2530818 (2). Here, we used a hybridization approach starting from CCT251921 and MSC2530818 to derive new inhibitors with the aim of developing highly potent and selective inhibitors of CDK8/19. Initial compounds suffered from rapid aldehyde oxidase-mediated metabolism. This liability was overcome by utilizing a pyrazolopyridine hinge binder with a chlorine at the C-3 position. These efforts resulted in JH-XVI-178 (compound 15), a highly potent and selective inhibitor of CDK8/19 that displays low clearance and moderate oral pharmacokinetic properties." @default.
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- W3208341234 date "2021-10-22" @default.
- W3208341234 modified "2023-10-16" @default.
- W3208341234 title "Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19" @default.
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- W3208341234 doi "https://doi.org/10.1021/acsmedchemlett.1c00300" @default.
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