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Updated: Jun 2, 2026

Modification and Functionalization of the Guanidine Group by Tailor-made Precursors
Published on: April 27, 2017
Chelate oxorhenium to assemble new integrin antagonists
Julien Le Gal1, Marta Gonera, Marie-Anne Lelait
1CEA/Saclay, iBiTec-S/SIMOPRO, Bâtiment 152, 91191 Gif-sur-Yvette, France.
Abstract:
Assembly of independent chemical modules through oxorhenium coordination by a NS(2)+S chelation motif was applied to the synthesis of RGD (Arg-Gly-Asp) analogs. Modules were assembled through oxorhenium chelation to give a series of 18 metal complexes in good yields and satisfactory purities. Screening of these oxorhenium coordinates as antagonists of integrins αVβ3, αIIbβ3 and αVβ5 led to the identification of 3 bioactive compounds that exhibit submicromolar affinities for the 3 integrins. Preliminary studies showed that the corresponding oxotechnetium complexes are stable in mice plasma and therefore could be proposed for the molecular imaging of pathologies that overexpress integrins αVβ3 and αVβ5.
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