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Title: CXCR4 chemokine receptor antagonists: nickel(ii) complexes of configurationally restricted macrocycles
Authors: Smith, Rachel ×
Huskens, Dana
Daelemans, Dirk
Mewis, Ryan E
Garcia, Courtney D
Cain, Amy N
Freeman, Tarynn N Carder
Pannecouque, Christophe
De Clercq, Erik
Schols, Dominique
Hubin, Timothy J
Archibald, Stephen J #
Issue Date: Oct-2012
Publisher: Royal Society of Chemistry
Series Title: Dalton Transactions vol:41 issue:37 pages:11369-11377
Abstract: Tetraazamacrocyclic complexes of transition metals provide useful units for incorporating multiple coordination interactions into a single protein binding molecule. They can be designed with available sites for protein interactions via donor atom-containing amino acid side chains or labile ligands, such as H(2)O, allowing facile exchange. Three configurationally restricted nickel(ii) cyclam complexes with either one or two macrocyclic rings were synthesised and their ability to abrogate the CXCR4 chemokine receptor signalling process was assessed (IC(50) = 8320, 194 and 14 nM). Analogues were characterised crystallographically to determine the geometric parameters of the acetate binding as a model for aspartate. The most active nickel(ii) compound was tested in several anti-HIV assays against representative viral strains showing highly potent EC(50) values down to 13 nM against CXCR4 using viruses, with no observed cytotoxicity (CC(50) > 125 μM).
URI: 
ISSN: 1477-9226
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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