3'-叠氮基-3'-脱氧胸苷（AZT）甾体前药的合成及抗HIV活性

Synthesis and anti-HIV activity of steroidal prodrugs of 3'-azido-3'-deoxythymidine (AZT).

作者信息

Balagopala M I, Ollapally A P, Lee H J

机构信息

Department of Chemistry, Florida A. & M. University, Tallahassee 32307, USA.

出版信息

Cell Mol Biol (Noisy-le-grand). 1995;41 Suppl 1:S1-7.

PMID:8574137

Abstract

A total of seven steroidal prodrugs of AZT were synthesized and tested in vitro for their anti-HIV activity. Three of them were steroidal carboxylic esters prepared from steroidal 17 beta-carboxylic acids and AZT. The remaining four were alkyl steroidal phospho-triesters of AZT. These prodrugs were synthesized using known procedures. Preliminary results of in vitro anti-HIV activity screening showed that all of these prodrugs were active against HIV. While carboxylic esters showed comparable anti-HIV activity to that of AZT, phosphotriesters were less active than AZT. The therapeutic indices of all these prodrugs are comparable to that of AZT.

摘要

共合成了七种齐多夫定的甾体前药，并在体外测试了它们的抗HIV活性。其中三种是由甾体17β - 羧酸与齐多夫定制备的甾体羧酸酯。其余四种是齐多夫定的烷基甾体磷酸三酯。这些前药采用已知方法合成。体外抗HIV活性筛选的初步结果表明，所有这些前药均具有抗HIV活性。虽然羧酸酯显示出与齐多夫定相当的抗HIV活性，但磷酸三酯的活性低于齐多夫定。所有这些前药的治疗指数与齐多夫定相当。