SYNTHESIS AND ANTI-HIV EVALUATION OF D4T AND D4T 5'-MONOPHOSPHATE PRODRUGS

被引：41

作者：

SERGHERAERT, C ^{[1
]}

PIERLOT, C ^{[1
]}

TARTAR, A ^{[1
]}

HENIN, Y ^{[1
]}

LEMAITRE, M ^{[1
]}

机构：

[1] CRVA,RHONE POULENC RORER,DEPT BIOL,F-94403 VITRY,FRANCE

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 07期

关键词：

D O I：

10.1021/jm00059a006

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several 5-monophosphate D4T derivatives and their analogues were synthesized as potential lipophilic prodrugs of D4T. Cholesteryl D4T phosphate diester and bis-5'-D4T phosphate inhibited HIV replication in CEM-Cl13 cells more efficiently than D4T itself as measured by the inhibition of cytopathic effect based on MTT assay or reverse transcriptase activity. The two compounds were devoid of toxicity on CEM-Cl13 cells at doses equal to 50 and 100 muM, respectively, which brought the selectivity index into the same range as AZT.

引用

页码：826 / 830

页数：5

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