Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication

  • Bioorg Med Chem Lett. 2011 Mar 1;21(5):1414-8. doi: 10.1016/j.bmcl.2011.01.021.
Renato Skerlj  1 ,  Gary Bridger ,  Ernest McEachern ,  Curtis Harwig ,  Chris Smith ,  Alan Kaller ,  Duane Veale ,  Helen Yee ,  Krystyna Skupinska ,  Rossana Wauthy ,  Letian Wang ,  Ian Baird ,  Yongbao Zhu ,  Kate Burrage ,  Wen Yang ,  Michael Sartori ,  Dana Huskens ,  Erik De Clercq ,  Dominique Schols
Affiliations
PMID: 21295470 DOI: 10.1016/j.bmcl.2011.01.021
Abstract

A novel series of CXCR4 antagonists were identified based on the substantial redesign of AMD070. These compounds possessed potent anti-HIV-1 activity and showed excellent pharmacokinetics in rat and dog.