Selective synthesis of an elusive C-functional bis-cyclam and study of its inhibition of the CXCR4 chemokine receptor

Author:

Le Roy Marie M.1ORCID,Claes Sandra2,Saffon-Merceron Nathalie3,Schols Dominique2ORCID,Troadec Thibault1ORCID,Tripier Raphaël1ORCID

Affiliation:

1. Univ Brest, UMR CNRS 6521 CEMCA, 6 Avenue Victor le Gorgeu, 29200 Brest, France

2. Rega Institute for Medical Research, KU Leuven, Herestraat 49, 3000 Leuven, Belgium

3. Institut de Chimie de Toulouse (FR 2599), 118 route de Narbonne, 31062 Toulouse Cedex 9, France

Abstract

A rare example of C,C′-linked bis-cyclam has been synthesized with controlled manner in mild conditions thanks to the “bis-aminal” tool, and its good CXCR4-recognition properties could be demonstated in vitro.

Funder

Ligue Contre le Cancer

Région Bretagne

Publisher

Royal Society of Chemistry (RSC)

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