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Synthesis and anti-HIV activity of oleanolic acid derivatives
1Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 294 Taiyuan Road, 200031, Shanghai, China.
Bioorganic & Medicinal Chemistry Letters
|November 27, 2001
Abstract:
Thirteen oleanolic acid derivatives were prepared and evaluated for anti-HIV activity in H9 lymphocytes. Saturating the C(12)-C(13) double bond and converting the C(17)-carboxyl group to an aminomethyl group led to compounds 13-15 and 19-20, respectively, which showed improved anti-HIV activity. Compound 15 was the most potent derivative with EC(50)=0.0039 microg/mL and TI=3570.