Novel RGD Peptidomimetics Embedding 1,2,3-Triazole as Central Scaffold; Synthesis and αvβ3 Integrin Affinity
Ming Hong Ni, Emiliano Esposito, Massimo Castorina and Alma Dal Pozzo
Affiliation: Istituto di Ricerche Chimiche e Biochimiche G. Ronzoni, via G. Colombo, 81, 20133, Milano, Italy.
Keywords: RGD peptidomimetics, αvβ3 integrin, Osteoporosis, 1,2,3-Triazole, Click chemistry, RGD, v 3 Integrin Affinity, peptide, aspartic acid, heterocyclic scaffolds, cycloaddition
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.
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