Novel highly potent, structurally simple gamma-trifluoromethyl gamma-sulfone hydroxamate inhibitor of stromelysin-1 (MMP-3) (Articolo in rivista)

Type
Label
  • Novel highly potent, structurally simple gamma-trifluoromethyl gamma-sulfone hydroxamate inhibitor of stromelysin-1 (MMP-3) (Articolo in rivista) (literal)
Anno
  • 2005-01-01T00:00:00+01:00 (literal)
Alternative label
  • Sani M., Candiani G., Pecker F., Malpezzi L., Zanda M. (2005)
    Novel highly potent, structurally simple gamma-trifluoromethyl gamma-sulfone hydroxamate inhibitor of stromelysin-1 (MMP-3)
    in Tetrahedron letters
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Sani M., Candiani G., Pecker F., Malpezzi L., Zanda M. (literal)
Pagina inizio
  • 2393 (literal)
Pagina fine
  • 2396 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 46 (literal)
Rivista
Note
  • ISI Web of Science (WOS) (literal)
Titolo
  • Novel highly potent, structurally simple gamma-trifluoromethyl gamma-sulfone hydroxamate inhibitor of stromelysin-1 (MMP-3) (literal)
Abstract
  • The gamma-trifluoromethyl gamma-sulfone hydroxamate 1 was synthesized both in racemic and enantiomerically pure forms by means of a thia-Michael reaction of p-methoxythiophenol on achiral and chiral 3,3,3-trifluorocrotonoyl Michael acceptors. The (R)-1 enantiomer was the most potent inhibitor of MMP-3 (stromelysin-1), showing an IC50 = 3.2 nM, as well as the most selective with respect to MMP-9 (65-fold). (c) 2005 Elsevier Ltd. All rights reserved. (literal)
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