EnglishEleven simple a-sulfonylphosphonates, new analogues of previously reported a-sulfonylaminophosphonates, were prepared and tested as MMP inhibitors. The IC50 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 (IC50=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
| Autori: | |
| Autori: | RUBINO M T; AGAMENNONE M; CAMPESTRE C; FRACCHIOLLA G; LAGHEZZA A; LOIODICE F; NUTI E; ROSSELLO A; TORTORELLA P |
| Titolo: | Synthesis, SAR, and biological evaluation of alpha-sulfonylphosphonic acids as selective matrix metalloproteinase inhibitors |
| Anno del prodotto: | 2009 |
| Digital Object Identifier (DOI): | 10.1002/cmdc.200800324 |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
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