Inhibition of HIV integrase by novel nucleotides bearing tricyclic bases

被引：12

作者：

Zhang, JZ

Neamati, N

Pommier, Y

Nair, V ^{[1
]}

机构：

[1] Univ Iowa, Dept Chem, Iowa City, IA 52242 USA

[2] NCI, Mol Pharmacol Lab, NIH, Bethesda, MD 20892 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(98)00327-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5'-Monophosphates of several novel dideoxynucleosides bearing tricyclic nucleobases were synthesized. Both linear and angular ring-extended analogs of isomeric dideoxyadenosine 5'-monophosphate were discovered to have moderate to good inhibition of the viral-encoded enzyme, HIV integrase. The results suggest that the nucleotide binding site of HIV integrase can accommodate major modifications in the nucleobase, which is in stark contrast to the nucleotide binding site on HIV reverse transcriptase, (C) 1998 Elsevier Science Ltd. All rights reserved.

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页码：1887 / 1890

页数：4

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