Aryloxy pivaloyloxymethyl prodrugs as nucleoside monophosphate prodrugs

Alanazi, Ashwag S., Miccoli, Ageo and Mehellou, Youcef ORCID: https://orcid.org/0000-0001-5720-8513 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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Abstract

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:	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:	19 Nov 2024 12:30
URI:	https://orca.cardiff.ac.uk/id/eprint/145823

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