Discovery of a New Class of Potent MMP Inhibitors by Structure-Based Optimization of the Arylsulfonamide Scaffold (Articolo in rivista)

Type
Label
  • Discovery of a New Class of Potent MMP Inhibitors by Structure-Based Optimization of the Arylsulfonamide Scaffold (Articolo in rivista) (literal)
Anno
  • 2013-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1021/ml300446a (literal)
Alternative label
  • Mori, Mattia; Massaro, Assunta; Calderone, Vito; Fragai, Marco; Luchinat, Claudio; Mordini, Alessandro (2013)
    Discovery of a New Class of Potent MMP Inhibitors by Structure-Based Optimization of the Arylsulfonamide Scaffold
    in ACS medicinal chemistry letters; AMER CHEMICAL SOC, WASHINGTON (Stati Uniti d'America)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Mori, Mattia; Massaro, Assunta; Calderone, Vito; Fragai, Marco; Luchinat, Claudio; Mordini, Alessandro (literal)
Pagina inizio
  • 565 (literal)
Pagina fine
  • 569 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 4 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali
  • 5 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
  • 6 (literal)
Note
  • Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • ProtEra Srl Università di Firenze ICCOM-CNR (literal)
Titolo
  • Discovery of a New Class of Potent MMP Inhibitors by Structure-Based Optimization of the Arylsulfonamide Scaffold (literal)
Abstract
  • A new class of potent matrix metalloproteinase (MMP) inhibitors designed by structure-based optimization of the well-known arylsulfonamide scaffold is presented. Mols. show an ethylene linker connecting the sulfonamide group with the P1' arom. portion and a D-proline residue bearing the zinc-binding group. The affinity improvement provided by these modifications led us to discover a nanomolar MMP inhibitor bearing a carboxylate moiety as zinc-binding group, which might be a promising lead mol. Notably, a significant selectivity for MMP-8, MMP-12, and MMP-13 was obsd. with respect to MMP-1 and MMP-7. (literal)
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