Synthesis, SAR, and Biological Evaluation of alpha-Sulfonylphosphonic Acids as Selective Matrix Metalloproteinase Inhibitors

RUBINO M., T; Agamennone, M; Campestre, C; Fracchiolla, Giuseppe; Laghezza, Antonio; Loiodice, Fulvio; Nuti, E; Rossello, A; Tortorella, Paolo

doi:10.1002/cmdc.200800324

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Eleven simple alpha-sulfonylphosphonates, new analogues of previously reported alpha-sulfonylaminophosphonates, were prepared and tested as MMP inhibitors. The IC(50) values of most of these compounds are in the nanomolar range against MMP-2, -8, -13, and -14. Compound 11 proved to be the most effective inhibitor of MMP-2 (IC(50) = 60 nM), with interesting selectivity versus the antitarget enzymes MMP-3 and MMP-9. The mode of binding of the new phosphonates in the active site of MMP-2 was studied, and variations in inhibition was explained by means of molecular modeling.

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Titolo:	Synthesis, SAR, and Biological Evaluation of alpha-Sulfonylphosphonic Acids as Selective Matrix Metalloproteinase Inhibitors
Autori:	RUBINO M. T AGAMENNONE M CAMPESTRE C FRACCHIOLLA, GIUSEPPE LAGHEZZA, ANTONIO LOIODICE, Fulvio NUTI E ROSSELLO A TORTORELLA, Paolo mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	2009
Rivista:	CHEMMEDCHEM
Citazione:	Synthesis, SAR, and Biological Evaluation of alpha-Sulfonylphosphonic Acids as Selective Matrix Metalloproteinase Inhibitors / RUBINO M.T; AGAMENNONE M; CAMPESTRE C; FRACCHIOLLA G; LAGHEZZA A; LOIODICE F; NUTI E; ROSSELLO A; TORTORELLA P. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 4:3(2009), pp. 352-362.
Abstract:	Eleven simple alpha-sulfonylphosphonates, new analogues of previously reported alpha-sulfonylaminophosphonates, were prepared and tested as MMP inhibitors. The IC(50) values of most of these compounds are in the nanomolar range against MMP-2, -8, -13, and -14. Compound 11 proved to be the most effective inhibitor of MMP-2 (IC(50) = 60 nM), with interesting selectivity versus the antitarget enzymes MMP-3 and MMP-9. The mode of binding of the new phosphonates in the active site of MMP-2 was studied, and variations in inhibition was explained by means of molecular modeling.
Handle:	http://hdl.handle.net/11586/133617
Appare nelle tipologie:	1.1 Articolo in rivista

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