The fundamental importance alpha-v-beta-3 integrin in a diverse range of biological processes, makes the search for new ligands of this receptors a significant therapeutic goal. We report herein our initial results in the synthesis of 5,6-dihydropyridin-2-one based ligands, containing a rigid heterocyclic core and two appendages mimicking arginine and aspartic acid moieties. In particular we explored herein the influence of the scaffold stereochemistry on bioactivity, performing SK-MEL-24 cell-fibronectin adhesion tests on diastereoisomers, that differ for the configuration at C6.

Synthesis of Enantiomerically Pure alpha-v-beta-3 Integrin ligands Based on a 5,6-Dihydropyridin-2-one Scaffold.

F. Benfatti;G. Cardillo;S. Fabbroni;L. Gentilucci;R. Perciaccante;A. Tolomelli;M. Baiula;S. Spampinato
2006

Abstract

The fundamental importance alpha-v-beta-3 integrin in a diverse range of biological processes, makes the search for new ligands of this receptors a significant therapeutic goal. We report herein our initial results in the synthesis of 5,6-dihydropyridin-2-one based ligands, containing a rigid heterocyclic core and two appendages mimicking arginine and aspartic acid moieties. In particular we explored herein the influence of the scaffold stereochemistry on bioactivity, performing SK-MEL-24 cell-fibronectin adhesion tests on diastereoisomers, that differ for the configuration at C6.
F. Benfatti; G. Cardillo; S. Fabbroni; L. Gentilucci; R. Perciaccante; A. Tolomelli; M. Baiula; S.Spampinato
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/27383
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