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Aryloxy Pivaloyloxymethyl Prodrugs as Nucleoside Monophosphate Prodrugs
Journal of Medicinal Chemistry  (IF7.446),  Pub Date : 2021-11-04, DOI: 10.1021/acs.jmedchem.1c01490
Ashwag S. Alanazi, Ageo Miccoli, Youcef Mehellou

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).