Design and Synthesis of Endoperoxide Antimalarial Prodrug Models (pages 4193–4197)
Paul M. O'Neill, Paul A. Stocks, Matthew D. Pugh, Nuna C. Araujo, Edward E. Korshin, Jamie F. Bickley, Stephen A. Ward, Patrick G. Bray, Erica Pasini, Jill Davies, Edite Verissimo and Mario D. Bachi
Article first published online: 9 AUG 2004 | DOI: 10.1002/anie.200453859
A masked combination chemotherapy which relies on the embedding of a number of active components, in a latent form, within a single endoperoxidic chemical entity is the aim of the research presented. The approach is illustrated by means of purposely designed bicyclic endoperoxide prodrug prototypes 1 and subsequently validated through the study of model compounds 2 (Ar=Ph, p-FC6H4, p-ClC6H4).