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

University of Liverpool
Weizmann Institute of Science
Liverpool School of Tropical Medicine

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

62 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.",

keywords = "Antimalarial agents, Chalcones, Combination chemotherapy, Cysteine protease inhibitors, Endoperoxides",

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doi = "10.1002/anie.200453859",

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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.

PY - 2004/8/13

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KW - Antimalarial agents

KW - Chalcones

KW - Combination chemotherapy

KW - Cysteine protease inhibitors

KW - Endoperoxides

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Design and synthesis of endoperoxide antimalarial prodrug models

Abstract

Keywords

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