Phosphoramidate derivatives of d4T with improved anti-HIV efficacy retain full activity in thymidine kinase-deficient cells

被引：61

作者：

McGuigan, C

Cahard, D

Sheeka, HM

DeClercq, E

Balzarini, J

机构：

[1] UNIV SOUTHAMPTON,DEPT CHEM,SOUTHAMPTON SO9 5NH,HANTS,ENGLAND

[2] KATHOLIEKE UNIV LEUVEN,REGA INST MED RES,B-3000 LOUVAIN,BELGIUM

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 10期

关键词：

D O I：

10.1016/0960-894X(96)00195-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New phosphate derivatives of the anti-HIV nucleoside analogue d4T were prepared as potential membrane-soluble pro-drugs of the bio-active free nucleotide. Some of the derivatives appear to have enhanced antiviral efficacy relative to the parent nucleoside analogue. Moreover, the derivatives appear to by-pass the dependence of the nucleoside on thymidine kinase-mediated activation, retaining full activity in thymidine kinase-deficient cells. The new analogues show particular promise for further pre-clinical development. (C) 1996 Elsevier Science Ltd

引用

页码：1183 / 1186

页数：4

共 18 条

[1] ESTIMATION OF THE LIPOPHILICITY OF ANTI-HIV NUCLEOSIDE ANALOGS BY DETERMINATION OF THE PARTITION-COEFFICIENT AND RETENTION TIME ON A LICHROSPHER-60 RP-8 HPLC COLUMN [J].