Title : Discovery of N-amido-phenylsulfonamide derivatives as novel microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors.

Pub. Date : 2021 Jun 1

PMID : 33775835






3 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 Discovery of N-Amido-Phenylsulfonamide Derivatives as Novel Microsomal Prostaglandin E2 Synthase-1 (mPGES-1) Inhibitors. Dinoprostone prostaglandin E synthase Mus musculus
2 Among them, MPO-0186 (scaffold C) inhibited the production of PGE2 (IC50: 0.24 muM) in A549 cells via inhibition of mPGES-1 (IC50: 0.49 muM in a cell-free assay) and was found to be approximately 9- and 8-fold more potent than MK-886 as a reference inhibitor, respectively. Dinoprostone prostaglandin E synthase Mus musculus
3 A molecular docking study theoretically suggests that MPO-0186 could inhibit PGE2 production by blocking the PGH2 binding site of mPGES-1 enzyme. Dinoprostone prostaglandin E synthase Mus musculus