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. 2010 May 1;20(9):2765-9.
doi: 10.1016/j.bmcl.2010.03.069. Epub 2010 Mar 21.

Synthesis and biological activity of 2H-quinolizin-2-one based p38alpha MAP kinase inhibitors

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Synthesis and biological activity of 2H-quinolizin-2-one based p38alpha MAP kinase inhibitors

Robert M Tynebor et al. Bioorg Med Chem Lett. .

Abstract

The development and synthesis of potent p38alpha MAP kinase inhibitors containing a 2H-quinolizin-2-one platform is described. Evolution of the 2H-quinolizin-2-one series from an early lead to solving off target activity and pharmacokinetic issues is also discussed.

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