Design, synthesis, and evaluation of potential prodrugs of DFMO for reductive activation

descriptionPublicationkeyboard_double_arrow_right Article 01 Nov 2012 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 22, pages 6,583-6,586 (issn: 0960-894X,

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Authors: Yanhui, Yang; Andrew, Voak; Shane R, Wilkinson; Longqin, Hu;

doi: 10.1016/j.bmcl.2012.09.005

pmid: 23031595

Design, synthesis, and evaluation of potential prodrugs of DFMO for reductive activation

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Abstract

A series of potential DFMO prodrugs was designed through the incorporation of 4-nitrobenzyl ester or carbamate groups for potential activation by trypanosomal nitroreductase. It was found that only modification of N(ε)-amino group of DFMO by 4-nitro-2-fluorobenzyloxycarbonyl resulted in significant trypanocidal activity and could serve as a lead for further investigation.

Related Organizations

Queen Mary University of London
United Kingdom
Rutgers Cancer Institute
United States
Rutgers, The State University of New Jersey
United States

Keywords

Trypanosoma, Binding Sites, Drug Design, Prodrugs, Nitroreductases, Models, Biological, Oxidation-Reduction, Trypanocidal Agents

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