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Bioorg Med Chem Lett. 2010 Aug 15;20(16):4885-91. doi: 10.1016/j.bmcl.2010.06.073. Epub 2010 Jun 17.

Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors.

Author information

1
Department of Chemistry, Cambridge South Laboratories, Pfizer Inc., 620 Memorial Drive, Cambridge, MA 02139, USA. hu.liu@pfizer.com

Abstract

By targeting an extended region of the conventional 'DFG-out' pocket of p38alpha, while minimizing interactions with the specificity pocket and eliminating interactions with the adenine binding site, we are able to design and synthesize a number of pyrazole-urea based DFG-out p38alpha inhibitors with good potencies, and excellent selectivity.

PMID:
20620059
DOI:
10.1016/j.bmcl.2010.06.073
[Indexed for MEDLINE]

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