Conjugates of betulin derivatives with AZT as potent anti-HIV agents |
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| Authors: | Juan Xiong Yoshiki Kashiwada Chin-Ho Chen Keduo Qian Susan L. Morris-Natschke Kuo-Hsiung Lee Yoshihisa Takaishi |
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| Affiliation: | 1. Graduate School of Pharmaceutical Sciences, University of Tokushima, Tokushima 770-8505, Japan;2. Medical Center, Duke University, Durham, NC 27710, USA;3. Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599-7568, USA |
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| Abstract: | Fourteen novel conjugates of 3,28-di-O-acylbetulins with AZT were prepared as anti-HIV agents, based on our previously reported potent anti-HIV triterpene leads, including 3-O-acyl and 3,28-di-O-acylbetulins. Nine of the conjugates (49–53, 55, 56, 59, and 60) exhibited potent anti-HIV activity at the submicromolar level, with EC50 values ranging from 0.040 to 0.098 μM in HIV-1NL4-3 infected MT-4 cells. These compounds were equipotent or more potent than 3-O-(3′,3′-dimethylsuccinyl)betulinic acid (2), which is currently in Phase IIb anti-AIDS clinical trial. |
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