1221971-48-7Relevant articles and documents
Selective inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from an oxicam template
Wang, Jane,Limburg, David,Carter, Jeff,Mbalaviele, Gabriel,Gierse, James,Vazquez, Michael
scheme or table, p. 1604 - 1609 (2010/07/04)
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 PGE2 inhibition in a cell-based assay (0.42 μM) and had over 238-fold selectivity for mPGES-1 over COX-2 and over 200-fold selectivity for mPGES-1 over 6-keto PGF1α.