Recognition and inhibition of HIV integrase by novel dinucleotides

被引：45

作者：

Taktakishvili, M

Neamati, N

Pommier, Y

Pal, S

Nair, V ^{[1
]}

机构：

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

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

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2000年 / 122卷 / 24期

关键词：

D O I：

10.1021/ja992528d

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

HIV integrase is involved in the integration of viral DNA into chromosomal DNA, a biological process that occurs by a sequence involving HIV DNA splicing and subsequent integration steps. in the quest for small nucleotide systems with nuclease stability of the internucleotide phosphate bond and critical structural features for recognition and inhibition of HIV-1 integrase, we have discovered novel, nuclease-resistant dinucleotides with defined base sequences that are inhibitors of this key viral enzyme. Synthetic methodologies utilized for the syntheses of the novel dinucleotides include an excellent new phosphorylating agent.

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页码：5671 / 5677

页数：7

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