radiation- and photo-induced activation of 5-fluorouracil prodrugs as a strategy for the selective treatment of solid tumors辐射和photo-induced激活5 -氟尿嘧啶高活性化合物作为实体肿瘤的选择性治疗的策略.pdfVIP

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radiation- and photo-induced activation of 5-fluorouracil prodrugs as a strategy for the selective treatment of solid tumors辐射和photo-induced激活5 -氟尿嘧啶高活性化合物作为实体肿瘤的选择性治疗的策略.pdf

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radiation- and photo-induced activation of 5-fluorouracil prodrugs as a strategy for the selective treatment of solid tumors辐射和photo-induced激活5 -氟尿嘧啶高活性化合物作为实体肿瘤的选择性治疗的策略

Molecules 2008, 13, 2370-2384; DOI: 10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /molecules Review Radiation- and Photo-induced Activation of 5-Fluorouracil Prodrugs as a Strategy for the Selective Treatment of Solid Tumors Takeo Ito, Kazuhito Tanabe, Hisatsugu Yamada, Hiroshi Hatta and Sei-ichi Nishimoto * Department of Energy and Hydrocarbon Chemistry, Graduate School of Engineering, Kyoto University, Kyoto 615-8510, Japan * Author to whom correspondence should be addressed; E-mail: nishimot@scl.kyoto-u.ac.jp. Received: 8 September 2008; in revised form: 22 September 2008 / Accepted: 22 September 2008 / Published: 1 October 2008 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 ch