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Bioorg Med Chem Lett. 2011 Jan 1;21(1):262-6. doi: 10.1016/j.bmcl.2010.11.023. Epub 2010 Nov 6.

Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.

Author information

1
Genzyme Corp, 153 Second Avenue, Waltham, MA 02451, USA. renato.skerlj@genzyme.com

Abstract

An early lead from the AMD070 program was optimized and a structure-activity relationship was developed for a novel series of heterocyclic containing compounds. Potent CXCR4 antagonists were identified based on anti-HIV-1 activity and Ca(2+) flux inhibition that displayed good pharmacokinetics in rat and dog.

PMID:
21109432
DOI:
10.1016/j.bmcl.2010.11.023
[Indexed for MEDLINE]

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