1169880-18-5Relevant articles and documents
New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1
Dang, Zhao,Ho, Phong,Zhu, Lei,Qian, Keduo,Lee, Kuo-Hsiung,Huang, Li,Chen, Chin-Ho
, p. 2029 - 2037 (2013/05/08)
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.
Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors
Dang, Zhao,Lai, Weihong,Qian, Keduo,Ho, Phong,Lee, Kuo-Hsiung,Chen, Chin-Ho,Huang, Li
experimental part, p. 7887 - 7891 (2010/04/30)
Wepreviously reported that [[N-[3β-hydroxyllup-20(29)-en-28-oyl]-7- aminoheptyl]carbamoyl]methane (A43D, 4) was a potent HIV-1 entry inhibitor. However, 4 was inactive against HIV-2 virus, suggesting the structural requirements for targeting these two ret
