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Oxorhenium-mediated assembly of noncyclic selective integrin antagonists: a combinatorial approach.

Chembiochem : a European journal of chemical biology (2011-02-10)
Marie Aufort, Marta Gonera, Julien Le Gal, Bertrand Czarny, Loïc Le Clainche, Robert Thai, Christophe Dugave
ABSTRACT

The parallel oxorhenium-mediated assembly of 288 noncyclic RGD analogues is reported. All complexes contain a NS(2) +S chelating motif that enables the unambiguous coordination of the oxorhenium and oxotechnetium cores. In this study, "modules S" contain a variety of pending guanidinium groups whereas the "NS(2) modules" are made of a series of N-acylated amino acids. Combination of sets of "NS(2) " and "S modules" together with tetrabutylammonium tetrachlorooxorhenate gave the corresponding oxorhenium complexes in good yields and satisfactory purities. Evaluation of these metalloconstructs towards integrins α(V) β(3) , α(IIb) β(3) , and α(V) β(5) led to the identification of micromolar and submicromolar antagonists of theses integrins. These compounds exhibit interesting selectivities and promise attractive applications for the molecular imaging of integrin-dependent pathologies.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Sodium perrhenate, 99.99% trace metals basis
Sigma-Aldrich
Ammonium perrhenate, ≥99%
Sigma-Aldrich
Potassium perrhenate, 99%
Sigma-Aldrich
Potassium perrhenate, 99.98% trace metals basis
Sigma-Aldrich
Ammonium perrhenate, 99.999% trace metals basis