http://www.cnr.it/ontology/cnr/individuo/prodotto/ID16660
Synthesis of Bicyclic Molecular Scaffolds (BTAa). An Investigation Towards New Selective MMP-12 Inhibitors (Articolo in rivista)
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- Synthesis of Bicyclic Molecular Scaffolds (BTAa). An Investigation Towards New Selective MMP-12 Inhibitors (Articolo in rivista) (literal)
- Anno
- 2006-01-01T00:00:00+01:00 (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
- 10.1016/j.bmc.2006.07.028 (literal)
- Alternative label
Mannino, Claudia; Nievo, Marco; Machetti,Fabrizio; Papakyriakou, A.; Calderone, V.: Fragai, Marco; Guarna, Antonio (2006)
Synthesis of Bicyclic Molecular Scaffolds (BTAa). An Investigation Towards New Selective MMP-12 Inhibitors
in Bioorganic & medicinal chemistry (Print); Pergamon-Elsevier Science Ltd., Oxford (Regno Unito)
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- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
- Mannino, Claudia; Nievo, Marco; Machetti,Fabrizio; Papakyriakou, A.; Calderone, V.: Fragai, Marco; Guarna, Antonio (literal)
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- http://www.sciencedirect.com/science/article/pii/S0968089606005827 (literal)
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- ISI Web of Science (WOS) (literal)
- PubMe (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
- Istituto di chimica dei composti organometallici del CNR
Dipartimento di chimica Organica 'Ugo Schiff' dell'Università di Firenze (literal)
- Titolo
- Synthesis of Bicyclic Molecular Scaffolds (BTAa). An Investigation Towards New Selective MMP-12 Inhibitors (literal)
- Abstract
- Starting from 3-aza-6,8-dioxa-bicyclo[3.2.1]octane scaffold (BTAa) a virtual library of molecules was generated and
screened in silico against the crystal structure of the Human Macrophage Metalloelastase (MMP-12). The molecules obtaining high
score were synthesized and the affinity for the catalytic domain of MMP-12 was experimentally proved by NMR experiments. A
BTAa scaffold 20 having a N-hydroxyurea group in position 3 and a p-phenylbenzylcarboxy amide in position 7 showed a fair inhibition
potency (IC50 = 149 lM) for MMP-12 and some selectivity towards five different MMPs. These results, taken together with
the X-ray structure of the adduct between MMP-12, the inhibitor 20 and the acetohydroxamic acid (AHA), suggest that bicyclic
scaffold derivatives may be exploited for the design of new selective matrix metalloproteinase inhibitors (MMPIs). (literal)
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