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Ni M.H.,Istituto di Ricerche Chimiche e Biochimiche G. Ronzoni | Esposito E.,Istituto di Ricerche Chimiche e Biochimiche G. Ronzoni | Castorina M.,Research and Development Sigma Tau | Pozzo A.D.,Istituto di Ricerche Chimiche e Biochimiche G. Ronzoni
Letters in Drug Design and Discovery | Year: 2011

Ten new RGD (Arginine-Glycine-Aspartic acid) peptidomimetics have been synthesized and screened for their affinity to α vβ 3 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. © 2011 Bentham Science Publishers Ltd. Source

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