title: Synthesis and SAR of alpha-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors.
abstract: A series of novel carboxylic acid-based alpha-sulfone MMP inhibitors have been synthesized and the in vitro enzyme SAR is discussed. A potential binding mode in the active site of the MMP-9 homology model was highlighted. These compounds are potent MMP-9 inhibitors and are selective over MMP-1.
authors.affiliation: Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, 1000 Route 202, Raritan, NJ 08869, USA. xufangymz@yahoo.com
authors.forename: Yue-Mei
authors.initials: YM
authors.lastname: Zhang
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Fan
authors.forename: Bangping
authors.initials: B
authors.lastname: Xiang
authors.forename: Devraj
authors.initials: D
authors.lastname: Chakravarty
authors.forename: Robert
authors.initials: R
authors.lastname: Scannevin
authors.forename: Sharon
authors.initials: S
authors.lastname: Burke
authors.forename: Prabha
authors.initials: P
authors.lastname: Karnachi
authors.forename: Kenneth
authors.initials: K
authors.lastname: Rhodes
authors.forename: Paul
authors.initials: P
authors.lastname: Jackson
mesh_terms: D000818:Animals; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D061965:Matrix Metalloproteinase Inhibitors; D020782:Matrix Metalloproteinases / Q000737:chemistry / Q000378:metabolism; D008958:Models, Molecular; D015394:Molecular Structure; D011480:Protease Inhibitors / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship; D013455:Sulfur / Q000737:chemistry*
chemical_list: D002264:Carboxylic Acids; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D013455:Sulfur; D020782:Matrix Metalloproteinases