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Bioorg Med Chem Lett. 2010 Jan 1;20(1):334-7. doi: 10.1016/j.bmcl.2009.10.103. Epub 2009 Oct 29.

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Author information

1
Abbott Laboratories, 100 Research Drive, Worcester, MA 01605-5314, USA.

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 IC(50) values as low as 19nM and moderate selectivity against a kinase panel. Compounds 15, 31a, and 31b inhibit TNFalpha production in peripheral human monocytes.

PMID:
19926477
DOI:
10.1016/j.bmcl.2009.10.103
[Indexed for MEDLINE]

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