Title: Configurationally restricted bismacrocyclic CXCR4 receptor antagonists
Authors: Valks, Gina C ×
McRobbie, Graeme
Lewis, Elizabeth A
Hubin, Timothy J
Hunter, Tina M
Sadler, Peter J
Pannecouque, Christophe
De Clercq, Erik
Archibald, Stephen J #
Issue Date: Oct-2006
Series Title: Journal of Medicinal Chemistry vol:49 issue:21 pages:6162-5
Abstract: A zinc(II) containing configurationally restricted analogue of bismacrocyclic cyclam-type CXCR4 chemokine receptor antagonists has been synthesized and shown to adopt only one configuration in solution. The single crystal X-ray structure reveals favorable binding to acetate via a bidentate chelation that can be related to the proposed interaction with aspartate on the receptor protein surface. The zinc(II) complex is highly active against HIV infection in vitro.
ISSN: 0022-2623
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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