Article ID Journal Published Year Pages File Type
1372487 Bioorganic & Medicinal Chemistry Letters 2010 4 Pages PDF
Abstract

We describe structure-based optimization of a series of novel 2,4-diaminopyrimidine MK2 inhibitors. Co-crystal structures (see accompanying Letter) demonstrated a unique inhibitor binding mode. Resulting inhibitors had IC50 values as low as 19 nM and moderate selectivity against a kinase panel. Compounds 15, 31a, and 31b inhibit TNFα production in peripheral human monocytes.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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