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.
Rachel Smith, Dana Huskens, Dirk Daelemans, Ryan E. Mewis, Courtney D. Garcia, Amy N. Cain, TaRynn N. Carder Freeman, Christophe Pannecouque, De Clercq Erik, Dominique Schols, Timothy J. Hubin, Stephen J. Archibald
Graeme McRobbie, Gina C. Valks, Christopher J. Empson, Abid Khan, J.D. Silversides, Christophe Pannecouque, De Clercq Erik, Steven G. Fiddy, Adam J. Bridgeman, Nigel A. Young, Stephen J. Archibald
Abid Khan, Gary Nicholson, John Greenman, Leigh A. Madden, Graeme McRobbie, Christophe Pannecouque, De Clercq Erik, Robert Ullom, D.L. Maples, Randall D. Maples, J.D. Silversides, Timothy J. Hubin, Stephen J. Archibald
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