Novel Betulinic Acid–Nucleoside Hybrids with Potent Anti-HIV Activity

Abstract

Novel betulinic/betulonic acid-nucleoside hybrids were synthesized as possible new anti-HIV agents. Among the synthesized hybrids, two compounds were highly effective against HIV. Compared with AZT and DSB, compounds <b>10a</b> (IC₅₀ = 0.0078 μM, CC₅₀ = 9.6 μM) and <b>10b</b> (IC₅₀ = 0.020 μM, CC₅₀ = 23.8 μM) showed more potent or equipotent, respectively, anti-HIV activity but displayed lower cytotoxicity.