THE PROOLIGONUCLEOTIDE APPROACH .1. ESTERASE-MEDIATED REVERSIBILITY OF DITHYMIDINE-S-ALKYL-PHOSPHOROTHIOLATES TO DITHYMIDINE PHOSPHOROTHIOATES

被引：45
作者：
BARBER, I [1 ]
RAYNER, B [1 ]
IMBACH, JL [1 ]
机构：
[1] UNIV MONTPELLIER 2,CHIM BIOORGAN LAB,CNRS,URA 488,F-34095 MONTPELLIER 5,FRANCE
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 06期
关键词：
D O I：
10.1016/0960-894X(95)00074-4
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Alkylation of dithymidine phosphorothioate and phosphorodithioate with various iodoalkyl acylates afforded the corresponding uncharged S-alkyl phosphoromono- and di-thioates respectively. Upon incubation of these triesters in CEM cell extracts, the bioreversible alkyl acylate masking groups were selectively and rapidly removed by carboxyesterases present in the milieu, yielding the starting dinucleoside diesters.
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页码：563 / 568
页数：6
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