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Bioorg Med Chem Lett. 2010 Mar 1;20(5):1604-9. doi: 10.1016/j.bmcl.2010.01.060. Epub 2010 Jan 25.

Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template.

Author information

1
Pfizer Inc. St. Louis Laboratory, PGRD Research, 700 Chesterfield PKWY W, Chesterfield, MO 63017, USA. jl47wang@yahoo.com

Abstract

Here we describe the SAR of a series of potent and selective mPGES-1 inhibitors based on an oxicam template. Compound 13j demonstrated low nanomolar mPGES-1 inhibition in an enzyme assay. In addition, it displayed PGE(2) inhibition in a cell-based assay (0.42microM) and had over 238-fold selectivity for mPGES-1 over COX-2 and over 200-fold selectivity for mPGES-1 over 6-keto PGF(1alpha).

PMID:
20144869
DOI:
10.1016/j.bmcl.2010.01.060
[Indexed for MEDLINE]

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