Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377167 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
3-O-3′(or 2′)-Methylsuccinyl-betulinic acid (MSB) derivatives were separated by using recycle HPLC. The structures of four isomers were assigned by NMR and asymmetric synthesis. 3-O-3′S-Methylsuccinyl-betulinic acid (3′S-MSB, 4) exhibited potent anti-HIV activity with an EC50 value of 0.0087 μM and a TI value of 6.3 × 103, which is comparable to the data for bevirimat (DSB, PA-457), a current clinical trials drug that was also derived from betulinic acid. The anti-HIV potency of 4 was slightly better than that of AZT.
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Related Topics
Physical Sciences and Engineering
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Organic Chemistry
Authors
Keduo Qian, Kyoko Nakagawa-Goto, Donglei Yu, Susan L. Morris-Natschke, Theodore J. Nitz, Nicole Kilgore, Graham P. Allaway, Kuo-Hsiung Lee,