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Synthesis,SAR, and Biological Evaluation of α‐Sulfonylphosphonic Acids as Selective Matrix Metalloproteinase Inhibitors
Authors:Maria Teresa Rubino Dr.  Mariangela Agamennone Dr.  Cristina Campestre Dr.  Giuseppe Fracchiolla Dr.  Antonio Laghezza Dr.  Fulvio Loiodice Prof.  Elisa Nuti Dr.  Armando Rossello Prof.  Paolo Tortorella Prof.
Affiliation:1. Dipartimento Farmaco‐Chimico, Università degli Studi di Bari, Via Orabona 4, 70126 Bari (Italy), Fax: (+39)?080‐5442231;2. Dipartimento di Scienze del Farmaco, Università “G. d'Annunzio”, Via dei Vestini 31, 66013 Chieti (Italy);3. Dipartimento di Scienze Farmaceutiche, Università degli Studi di Pisa, Via Bonanno 6, 56126 Pisa (Italy)
Abstract:Selective MMP inhibitors : Eleven α‐sulfonylphosphonates were synthesized and tested as MMP inhibitors. The IC50 values for most of them are in the nanomolar range against MMP‐2, ‐8, ‐13, and ‐14, with an interesting selectivity profile versus MMP‐9.
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Keywords:inhibitors  matrix metalloproteinases  molecular modeling  phosphonic acids  zinc binding groups
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