Design of Selectively Activated Anticancer Prodrugs: Elimination and Cyclization Strategies

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Design of Selectively Activated Anticancer Prodrugs: Elimination and Cyclization Strategies

Anti-Cancer Agents in Medicinal Chemistry, 2(2): 155-185.

Author(s): S. Papot, I. Tranoy, F. Tillequin, J. -C. Florent and J -P Gesson.

Affiliation: UMR 6514, Faculte des Sciences, 40 avenue du recteur Pineau, 86022 Poitiers, France


Cancer chemotherapy is associated with severe side effects which may be reduced by selective liberation, at the tumour site, of a cytotoxic agent from a non-toxic prodrug. Several strategies are used to achieve the required selective activation : with enzymes which are present in higher concentration in, or close, to the tumour (β-glucuronidase, plasmin), with enzymes covalently linked to a macromolecular carrier able to recognize antigen positive cancer cells (ADEPT : Antibody Directed Enzyme Prodrug Therapy) or with reductive processes which are favoured in an hypoxic environment. Most of the prodrugs include a linker (or spacer) between the trigger and the drug (or effector). The design of such linkers is crucial in order to achieve a fast drug liberation under physiological conditions. The linker groups may be classified in two categories based on elimination or cyclization processes. The advantages and the limitations of each strategy are discussed.


Anticancer Prodrugs, Phenol Based Linkers, hydroxylamine, glutamine antimetabolite, Cephalosporin-Based, deacetylvinblastine (DAVLB), 4-hydroxyanisole.

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Article Details

Volume: 2
Issue Number: 2
First Page: 155
Last Page: 185
Page Count: 31
DOI: 10.2174/1568011023354173
Price: $58
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