Design and synthesis of endoperoxide antimalarial prodrug models

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; Mario D. Bachi

doi:10.1002/anie.200453859

Design and synthesis of endoperoxide antimalarial prodrug models

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, Mario D. Bachi

Research output: Contribution to journal › Article › peer-review

61 Scopus citations

Abstract

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-FC ₆H₄, p-ClC₆H₄.

Original language	English
Pages (from-to)	4193-4197
Number of pages	5
Journal	Angewandte Chemie - International Edition
Volume	43
Issue number	32
DOIs	https://doi.org/10.1002/anie.200453859
State	Published - 13 Aug 2004
Externally published	Yes

Keywords

Antimalarial agents
Chalcones
Combination chemotherapy
Cysteine protease inhibitors
Endoperoxides

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10.1002/anie.200453859

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abstract = "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-FC 6H4, p-ClC6H4.",

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AU - Stocks, Paul A.

AU - Pugh, Matthew D.

AU - Araujo, Nuna C.

AU - Korshin, Edward E.

AU - Bickley, Jamie F.

AU - Ward, Stephen A.

AU - Bray, Patrick G.

AU - Pasini, Erica

AU - Davies, Jill

AU - Verissimo, Edite

AU - Bachi, Mario D.

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KW - Combination chemotherapy

KW - Cysteine protease inhibitors

KW - Endoperoxides

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Design and synthesis of endoperoxide antimalarial prodrug models

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