期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 23, 页码 6553-6557出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.09.081
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资金
- NIAID NIH HHS [R01 AI033066-16, AI-33066, R01 AI033066] Funding Source: Medline
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 mu M and a TI value of 6.3 x 10(3), 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. (c) 2007 Elsevier Ltd. All rights reserved.
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