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Molecules 2008, 13(10), 2370-2384; doi:10.3390/molecules13102370
Review

Radiation- and Photo-induced Activation of 5-Fluorouracil Prodrugs as a Strategy for the Selective Treatment of Solid Tumors

, , ,  and *
Department of Energy and Hydrocarbon Chemistry, Graduate School of Engineering, Kyoto University, Kyoto 615-8510, Japan
* Author to whom correspondence should be addressed.
Received: 8 September 2008 / Revised: 22 September 2008 / Accepted: 22 September 2008 / Published: 1 October 2008
(This article belongs to the Special Issue 5-Fluorouracil)
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Abstract

5-Fluorouracil (5-FU) is used widely as an anticancer drug to treat solid cancers, such as colon, breast, rectal, and pancreatic cancers, although its clinical application is limited because 5-FU has gastrointestinal and hematological toxicity. Many groups are searching for prodrugs with functions that are tumor selective in their delivery and can be activated to improve the clinical utility of 5-FU as an important cancer chemotherapeutic agent. UV and ionizing radiation can cause chemical reactions in a localized area of the body, and these have been applied in the development of site-specific drug activation and sensitization. In this review, we describe recent progress in the development of novel 5-FU prodrugs that are activated site specifically by UV light and ionizing radiation in the tumor microenvironment. We also discuss the chemical mechanisms underlying this activation.
Keywords: 5-Fluorouracil; Prodrugs; Hypoxia; Hydrated Electrons; Radiolysis; Photolysis 5-Fluorouracil; Prodrugs; Hypoxia; Hydrated Electrons; Radiolysis; Photolysis
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Ito, T.; Tanabe, K.; Yamada, H.; Hatta, H.; Nishimoto, S.-I. Radiation- and Photo-induced Activation of 5-Fluorouracil Prodrugs as a Strategy for the Selective Treatment of Solid Tumors. Molecules 2008, 13, 2370-2384.

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