Enhancing the divergent activities of betulinic acid via neoglycosylation.

Enhancing the divergent activities of betulinic acid via neoglycosylation.
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DOI:
10.1021/ol8025704
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发表时间:
2009-01-15
期刊:
影响因子:
5.2
通讯作者:
Thorson JS
Thorson JS
中科院分区:
化学1区
文献类型:
--
作者:
Goff RD;Thorson JS

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使用neoglycosylation,差异糖基化的影响后,不同的抗癌和抗艾滋病毒的三萜桦木酸(BA)的性质进行了检查。对来自37个差异糖基化BA变体的文库的每个成员进行抗癌和抗HIV活性测试。发现了两种所需活性的增强的类似物,其中相应的抗肿瘤或抗病毒增强作用基于附加的糖而分成两个不同的化合物子集。
Using neoglycosylation, the impact of differential glycosylation upon the divergent anticancer and anti-HIV properties of the triterpenoid betulinic acid (BA) was examined. Each member from a library of 37 differentially glycosylated BA variants was tested for anticancer and anti-HIV activities. Enhanced analogs for both desired activities were discovered with the corresponding antitumor or antiviral enhancements diverging, based upon the appended sugar, into two distinct compound subsets.
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