SYNTHESIS AND ANTI-HIV ACTIVITY OF ALKYL STEROIDAL 3'-AZIDO-3'-DEOXYTHYMIDIN-5'-YL PHOSPHOTRIESTERS AS PRODRUGS OF AZT

被引：8

作者：

BALAGOPALA, MI

OLLAPALLY, AP

LEE, HJ

机构：

[1] FLORIDA A&M UNIV,COLL PHARM & PHARMACEUT SCI,TALLAHASSEE,FL 32307

[2] FLORIDA A&M UNIV,DEPT CHEM,TALLAHASSEE,FL 32307

来源：

NUCLEOSIDES & NUCLEOTIDES | 1994年 / 13卷 / 09期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1080/15257779408010667

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：

Alkyl steroidal AZT 5'-monophosphate triesters are designed as lipophilic prodrugs of AZT to improve its therapeutic efficiency. We have synthesized four phosphotriesters of AZT, in one-pot, using phosphoramidite-phosphite triester methodology. This method afforded the desired prodrugs in high yields under mild conditions. The in vitro evaluation of anti-HIV activity of these prodrugs is also reported.

引用

页码：1843 / 1853

页数：11

共 31 条

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