872584-92-4Relevant academic research and scientific papers
Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents
Yu, Donglei,Sakurai, Yojiro,Chen, Chin-Ho,Chang, Fang-Rong,Huang, Li,Kashiwada, Yoshiki,Lee, Kuo-Hsiung
, p. 5462 - 5469 (2006)
In a continuing structure-activity relationship study of potent anti-HIV agents, seven new triterpene derivatives were designed, synthesized, and evaluated for in vitro antiviral activity. Among them, moronic acid derivatives 19, 20, and 21 showed significant activity in HIV-1 infected H9 lymphocytes. Compounds 19 and 20 were also evaluated against HIV-1 NL4-3 and drug resistant strains in the MT-4 cell line. Compounds 19 and 20 showed better antiviral profiles than the betulinic acid analogue 8 (PA-457), which has successfully completed a Phase IIa clinical trial. Compound 20 showed potent anti-HIV activity with EC50 values of 0.0085 μM against NL4-3, 0.021 μM against PI-R (a multiple protease inhibitor resistant strain), and 0.13 μM against FHR-2 (an HIV strain resistant to 8). Promising compound 20 has become a new lead for modification, and further development of 20-related compounds as clinical trial candidates is warranted.
