Novel RGD Peptidomimetics Embedding 1,2,3-Triazole as Central Scaffold; Synthesis and αvβ3 Integrin Affinity

Title: Novel RGD Peptidomimetics Embedding 1,2,3-Triazole as Central Scaffold; Synthesis and αvβ3 Integrin Affinity

Volume: 8 Issue: 5

Author(s): Ming Hong Ni, Emiliano Esposito, Massimo Castorina and Alma Dal Pozzo

Affiliation:

Keywords: RGD peptidomimetics, αvβ3 integrin, Osteoporosis, 1,2,3-Triazole, Click chemistry, RGD, v 3 Integrin Affinity, peptide, aspartic acid, heterocyclic scaffolds, cycloaddition

Abstract: Ten new RGD (Arginine-Glycine-Aspartic acid) peptidomimetics have been synthesized and screened for their affinity to αvβ3 integrin receptor. Arginine and Aspartic acid mimetic subunits were connected through 1,2,3-triazole as central scaffold by click chemistry, affording the final products with good yields. Among them, compounds 3f-j exhibited high affinity to the receptor,with IC50 in the low nanomolar range, comparable to that of the reference compound Cilengitide.

Cite this article as:

Hong Ni Ming, Esposito Emiliano, Castorina Massimo and Dal Pozzo Alma, Novel RGD Peptidomimetics Embedding 1,2,3-Triazole as Central Scaffold; Synthesis and αvβ3 Integrin Affinity, Letters in Drug Design & Discovery 2011; 8 (5) . https://dx.doi.org/10.2174/157018011795514258