Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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, Alma Dal Pozzo.

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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Article Details

VOLUME: 8
ISSUE: 5
Year: 2011
Page: [401 - 405]
Pages: 5
DOI: 10.2174/157018011795514258
Price: $58