Cardiff University | Prifysgol Caerdydd ORCA
Online Research @ Cardiff 
WelshClear Cookie - decide language by browser settings

Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside

McGuigan, Christopher, Murziani, Paola, Slusarczyk, Magdalena, Gonczy, Blanka, Vande Voorde, Johan, Liekens, Sandra and Balzarini, Jan 2011. Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside. Journal of Medicinal Chemistry 54 (20) , pp. 7247-7258. 10.1021/jm200815w

Full text not available from this repository.

Abstract

The fluorinated pyrimidine family of nucleosides continues to represent major current chemotherapeutic agents for treating solid tumors. We herein report their phosphate prodrugs, ProTides, as promising new derivatives, which partially bypass the dependence of the current drugs on active transport and nucleoside kinase-mediated activation. They are also resistant to metabolic deactivation by phosphorolytic enzymes. We report 39 ProTides of the fluorinated pyrimidine FUDR with variation in the aryl, ester, and amino acid regions. Notably, only certain ProTide motifs are successful in delivering the nucleoside monophosphate into intact cells. We also find that the ProTides retain activity in mycoplasma infected cells, unlike FUDR. Data suggest these compounds to be worthy of further progression.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Systems Immunity Research Institute (SIURI)
Subjects: Q Science > QD Chemistry
R Medicine > RS Pharmacy and materia medica
Publisher: ACS Publications
ISSN: 0022-2623
Last Modified: 02 Apr 2019 14:34
URI: http://orca.cf.ac.uk/id/eprint/11977

Citation Data

Cited 29 times in Google Scholar. View in Google Scholar

Cited 63 times in Scopus. View in Scopus. Powered By Scopus® Data

Actions (repository staff only)

Edit Item Edit Item