Synthesis and anti-HIV-1 activities of novel podophyllotoxin derivatives

Synthesis and anti-HIV-1 activities of novel podophyllotoxin derivatives
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新型鬼臼毒素衍生物的合成及其抗HIV-1活性

DOI:
10.1016/j.bmcl.2006.11.070
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发表时间:
2007-04-01
影响因子:
2.7
通讯作者:
Tu, Yong-Qiang
Tu, Yong-Qiang
中科院分区:
医学4区
文献类型:
--
作者:
Chen, Shi-Wu;Wang, Yun-Hua;Tu, Yong-Qiang

文献摘要

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为了探索鬼臼毒素类化合物的生物活性范围,设计、合成了一系列新的鬼臼毒素衍生物,它们是由司他夫定和不同结构的鬼臼毒素类似物偶联而成的,并对它们的体外抗hiv -1活性进行了评价。其中,119d和19c的抗hiv -1活性最高,EC50分别为0.17和0.29 μ M, TI分别为466.9和354.5。(c) 2007年Elsevier Ltd.出版
In order to explore the range of biological activities of the podophyllotoxin compound class, a novel series of derivatives of podophyllotoxin, which were conjugates containing stavudine and different structural podophyllotoxin analogues, were designed, synthesized, and evaluated for their anti-HIV-1 activities in vitro. Among these compounds, 119d and 19c showed the highest anti-HIV-1 activities with EC50 values of 0.17 and 0.29 mu M and TI values of 466.9 and 354.5, respectively. (c) 2007 Published by Elsevier Ltd.