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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 8, Issue 5, 2011

Page: [401 - 405] Pages: 5

DOI: 10.2174/157018011795514258

Price: $65

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.

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

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