DESIGN AND SYNTHESIS OF NOVEL THREOSYL-5′-DEOXYPHOSPHONIC ACID PURINE ANALOGUES AS POTENT ANTI-HIV AGENTS

被引：5

作者：

Liu, Lian Jin ^{[1
]}

Kim, Eunae ^{[1
]}

Hong, Joon Hee ^{[1
]}

机构：

[1] Chosun Univ, Coll Pharm, Project Team BK 21, Kwangju 501759, South Korea

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2012年 / 31卷 / 05期

关键词：

Antiviral agent; threosyl nucleoside phosphonic acid; Vorbruggen reaction; PHOSPHONATE ANALOGS; ANTIVIRAL ACTIVITY; NUCLEOSIDES; DNA;

D O I：

10.1080/15257770.2012.670349

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The discovery of threosyl phosphonate nucleoside (PMDTA, EC50 = 2.53 mu M) as a potent anti-HIV agent has led to the synthesis and biological evaluation of 5 5'-deoxyversions of threosyl phosphonate nucleosides from 1,4-dihydroxy-2-butene. The synthesized nucleoside phosphonic acid analogues 14 and 19 were tested for anti-HIV activity as well as cytotoxicity. The adenine analogue 14 exhibits moderate in vitro anti-HIV-1 activity (EC50 = 12.6 mu M).

引用

页码：411 / 422

页数：12

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