
Bioorganic and Medicinal Chemistry Letters p. 1604 - 1609 (2010)
Update date:2022-07-30
Topics:
Wang, Jane
Limburg, David
Carter, Jeff
Mbalaviele, Gabriel
Gierse, James
Vazquez, Michael
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.
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Doi:10.1002/chem.201600535
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