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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Development of Hypoxia Selective Cytotoxins for Cancer Treatment: An Update

Author(s): Hugo Cerecetto, Mercedes Gonzalez and Maria L. Lavaggi

Volume 2, Issue 3, 2006

Page: [315 - 327] Pages: 13

DOI: 10.2174/157340606776930808

Price: $65

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

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