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, et al. (2006). Synthesis of Enantiomerically Pure alpha-v-beta-3 Integrin ligands Based on a 5,6-Dihydropyridin-2-one Scaffold. TETRAHEDRON-ASYMMETRY, 17, 167-170 [10.1016/j.tetasy.2005.12.006].
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
