Aryloxy Pivaloyloxymethyl Prodrugs as Nucleoside Monophosphate Prodrugs,Journal of Medicinal Chemistry

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Aryloxy Pivaloyloxymethyl Prodrugs as Nucleoside Monophosphate Prodrugs
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2021-11-04 , DOI: 10.1021/acs.jmedchem.1c01490
Ashwag S Alanazi ₁ , Ageo Miccoli ₁ , Youcef Mehellou ₁

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Intracellular phosphorylation of therapeutic nucleoside analogues into their active triphosphate metabolites is a prerequisite for their pharmacological activity. However, the initial phosphorylation of these unnatural nucleosides into their monophosphate derivatives can be a rate-limiting step in their activation. To address this, we herein report the development of the aryloxy pivaloyloxymethyl prodrugs (POMtides) as a novel and effective nucleoside monophosphate prodrug technology and its successful application to the anticancer nucleoside analogue 5-fluoro-2′-deoxyuridine (FdUR).

中文翻译：

芳氧基新戊酰氧基甲基前药作为核苷单磷酸前药

治疗性核苷类似物的细胞内磷酸化为其活性三磷酸代谢物是其药理活性的先决条件。然而，这些非天然核苷初始磷酸化为其单磷酸盐衍生物可能是其活化的限速步骤。为了解决这个问题，我们在此报告了芳氧基新戊酰氧基甲基前药 (POMtides) 作为一种新型有效的单磷酸核苷前药技术的开发及其在抗癌核苷类似物 5-氟-2'-脱氧尿苷 (FdUR) 中的成功应用。

更新日期：2021-11-25

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