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Aryloxy pivaloyloxymethyl prodrugs as nucleoside monophosphate prodrugs

Alanazi, Ashwag S., Miccoli, Ageo and Mehellou, Youcef ORCID: 2021. Aryloxy pivaloyloxymethyl prodrugs as nucleoside monophosphate prodrugs. Journal of Medicinal Chemistry 64 (22) , 16703–16710. 10.1021/acs.jmedchem.1c01490

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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).

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Publisher: American Chemical Society
ISSN: 0022-2623
Date of First Compliant Deposit: 30 November 2021
Date of Acceptance: 21 October 2021
Last Modified: 10 Nov 2023 17:33

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