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  • Title: New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1.
    Author: Dang Z, Ho P, Zhu L, Qian K, Lee KH, Huang L, Chen CH.
    Journal: J Med Chem; 2013 Mar 14; 56(5):2029-37. PubMed ID: 23379607.
    Abstract:
    Bevirimat (1, BVM) is an anti-HIV agent that blocks HIV-1 replication by interfering with HIV-1 Gag-SP1 processing at a late stage of viral maturation. However, clinical trials of 1 have revealed a high baseline drug resistance that is attributed to naturally occurring polymorphisms in HIV-1 Gag. To overcome the drug resistance, 28 new derivatives of 1 were synthesized and tested against compound 1-resistant (BVM-R) HIV-1 variants. Among them, compound 6 exhibited much improved activity against several HIV-1 strains carrying BVM-R polymorphisms. Compound 6 was at least 20-fold more potent than 1 against the replication of NL4-3/V370A, which carries the most prevalent clinical BVM-R polymorphism in HIV-1 Gag-SP1. Thus, compound 6 merits further development as a potential anti-AIDS clinical trial candidate.
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