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

THE PROOLIGONUCLEOTIDE APPROACH .1. ESTERASE-MEDIATED REVERSIBILITY OF DITHYMIDINE-S-ALKYL-PHOSPHOROTHIOLATES TO DITHYMIDINE PHOSPHOROTHIOATES
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DOI:
10.1016/0960-894x(95)00074-4
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发表时间:
1995-03-16
影响因子:
2.7
通讯作者:
IMBACH, JL
IMBACH, JL
中科院分区:
医学4区
文献类型:
--
作者:
BARBER, I;RAYNER, B;IMBACH, JL

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二胸苷硫代酸磷和二硫代酸磷与不同的碘烷基酰化产物烷基化后,分别得到不带电的s -烷基磷单硫代和二硫代。这些三聚酯在CEM细胞提取物中孵育后,生物可逆的烷基酰基掩盖基团被环境中存在的羧酶选择性地快速去除,产生起始的二核苷二酯。
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.