Abstract
Increased attention has centered on exploiting hypoxia in tumors for targeting the design of selective antitumor agents. This review presents an update of the principal families of compounds under study and in clinical trials, such as Noxide derivatives, nitro compounds and quinone derivatives. Especially promising for bioreductive activation is the reduction of some moieties able to trigger a mechanism that releases cytotoxic antitumor drugs. The most remarkable redox-activated triggers are presented, N-oxide, nitro, azido, quinone, metal ions, 1,2-benzisoxazolyl and sulfoxide moieties.
Keywords: prodrug activation, antineoplastic drugs, Benzotriazine derivatives, QdNO derivatives, Redox-Activated Trigger
Medicinal Chemistry
Title: Development of Hypoxia Selective Cytotoxins for Cancer Treatment: An Update
Volume: 2 Issue: 3
Author(s): Hugo Cerecetto, Mercedes Gonzalez and Maria L. Lavaggi
Affiliation:
Keywords: prodrug activation, antineoplastic drugs, Benzotriazine derivatives, QdNO derivatives, Redox-Activated Trigger
Abstract: Increased attention has centered on exploiting hypoxia in tumors for targeting the design of selective antitumor agents. This review presents an update of the principal families of compounds under study and in clinical trials, such as Noxide derivatives, nitro compounds and quinone derivatives. Especially promising for bioreductive activation is the reduction of some moieties able to trigger a mechanism that releases cytotoxic antitumor drugs. The most remarkable redox-activated triggers are presented, N-oxide, nitro, azido, quinone, metal ions, 1,2-benzisoxazolyl and sulfoxide moieties.
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Cite this article as:
Cerecetto Hugo, Gonzalez Mercedes and Lavaggi L. Maria, Development of Hypoxia Selective Cytotoxins for Cancer Treatment: An Update, Medicinal Chemistry 2006; 2 (3) . https://dx.doi.org/10.2174/157340606776930808
DOI https://dx.doi.org/10.2174/157340606776930808 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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