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EnglishEleven 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.
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.
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| Titolo: | Synthesis, SAR, and Biological Evaluation of alpha-Sulfonylphosphonic Acids as Selective Matrix Metalloproteinase Inhibitors |
| Autori: | |
| Data di pubblicazione: | 2009 |
| Rivista: | |
| 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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