Synthesis and anti-HIV activity of oleanolic acid derivatives

Synthesis and anti-HIV activity of oleanolic acid derivatives
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DOI:
10.1016/s0960-894x(01)00647-3
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发表时间:
2001-12-17
影响因子:
2.7
通讯作者:
Lee, KH
Lee, KH
中科院分区:
医学4区
文献类型:
--
作者:
Zhu, YM;Shen, JK;Lee, KH

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制备了十三种油酸衍生物,并在H9淋巴细胞中评价了其抗HIV活性。使C-12-C-13双键饱和并将C-17-羧基转化为氨甲基得到化合物13-15和19-20。分别,其显示出改善的抗HIV活性。化合物15是最有效的衍生物,EC 50 =0.0039 μ g/mL,TI = 3570。(C)2001爱思唯尔科技有限公司版权所有。
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 EC50=0.0039 mug/mL and TI = 3570. (C) 2001 Elsevier Science Ltd. All rights reserved.