Literature

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 EC(50) value of 0.0087microM and a TI value of 6.3x10(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.

DOI： 10.1016/j.bmcl.2007.09.081

Anti-AIDS agents 73: Structure–activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives

Bioorganic & Medicinal Chemistry Letters 2007.0

3,28-Di-O-(dimethylsuccinyl)-betulin isomers as anti-HIV agents1

Bioorganic & Medicinal Chemistry Letters 2001.0

Anti-AIDS Agents 81. Design, Synthesis, and Structure−Activity Relationship Study of Betulinic Acid and Moronic Acid Derivatives as Potent HIV Maturation Inhibitors

Journal of Medicinal Chemistry 2010.0

3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents

Bioorganic & Medicinal Chemistry Letters 2004.0

Anti-AIDS agents. 32.1 synthesis and anti-HIV activity of betulin derivatives

Bioorganic & Medicinal Chemistry Letters 1998.0

Anti-AIDS Agents. 78. Design, Synthesis, Metabolic Stability Assessment, and Antiviral Evaluation of Novel Betulinic Acid Derivatives as Potent Anti-Human Immunodeficiency Virus (HIV) Agents