title: MMP-13 selective alpha-sulfone hydroxamates: identification of selective P1' amides.
abstract: Continuing our interest in designing compounds preferentially potent and selective for MMP-13, we report on a series of hydroxamic acids with a flexible amide P1' substituents. We identify an amide which spares both MMP-1 and -14, and shows >500 fold selectivity for MMP-13 versus MMP-2 and -8.
authors.affiliation: Department of Medicinal Chemistry, Pfizer Research & Development, 700 Chesterfield Village Parkway, St. Louis, MO 63198, USA.
authors.forename: Yvette M
authors.initials: YM
authors.lastname: Fobian
authors.forename: John N
authors.initials: JN
authors.lastname: Freskos
authors.forename: Thomas E
authors.initials: TE
authors.lastname: Barta
authors.forename: Louis J
authors.initials: LJ
authors.lastname: Bedell
authors.forename: Robert
authors.initials: R
authors.lastname: Heintz
authors.forename: Darren J
authors.initials: DJ
authors.lastname: Kassab
authors.forename: James R
authors.initials: JR
authors.lastname: Kiefer
authors.forename: Brent V
authors.initials: BV
authors.lastname: Mischke
authors.forename: John M
authors.initials: JM
authors.lastname: Molyneaux
authors.forename: Patrick
authors.initials: P
authors.lastname: Mullins
authors.forename: Grace E
authors.initials: GE
authors.lastname: Munie
authors.forename: Daniel P
authors.initials: DP
authors.lastname: Becker
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry; D020128:Inhibitory Concentration 50; D061965:Matrix Metalloproteinase Inhibitors; D015394:Molecular Structure; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D000577:Amides; D006877:Hydroxamic Acids; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors