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  • Title: Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.
    Author: Skerlj R, Bridger G, McEachern E, Harwig C, Smith C, Wilson T, Veale D, Yee H, Crawford J, Skupinska K, Wauthy R, Yang W, Zhu Y, Bogucki D, Di Fluri M, Langille J, Huskens D, De Clercq E, Schols D.
    Journal: Bioorg Med Chem Lett; 2011 Jan 01; 21(1):262-6. PubMed ID: 21109432.
    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.
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