Special Issue on "5-Fluorouracil" of the Molecules journal

Introduction

Although 5-fluorouracil (5-FU) was first introduced in 1957, it remains one of the most important anticancer agents. In 5-FU, the hydrogen atom at the 5-position of uracil is replaced by a fluorine atom and the molecule was designed to occupy the active sites of enzyme targets, thereby blocking metabolism in malignant cells. Although this antimetabolite is toxic, its efficacy makes it one of the most widely used agents against solid tumors. Numerous reports by the scientific community have been devoted to 5-FU, covering a wide range of topics: preparation of innovative formulations, synthesis of 5-FU derivatives, mechanism of action studies, etc. This special issue of Molecules aims to provide an overview of the current knowledge on this important chemotherapeutic agent, as well as focus on current strategies to improve therapeutic effectiveness of this drug in the treatment of advanced disease.

Guest Editor for this Special Issue
Dr Francesco Puoci

Review manuscripts: Before writing their manuscripts, potential authors of review articles should forward the title and a short abstract to the Guest Editor. The Guest Editor will then provide feedback on the suitability of the topic upon consultation with other editors and/or members of the Editorial Board. Authors are encouraged to write reviews that provide a critical appraisal of areas of 5-fluorouracil research.

Manuscript ID: fluorouracil-20071109-Campos-es
Type of the paper: review
Title: Acyclonucleosides, salicyl- and catechol-derived acyclic 5-fluorouracil O,N-acetals: Antiproliferative activities, apoptosis and cellular differentiation
Authors: Juan A. Marchal,a Antonia Aránega,a Miguel A. Gallo,b Antonio Espinosa,b Joaquín M. Campos
E-mail: jmcampos@ugr.es
a Instituto de Biopatología y Medicina Regenerativa (IBIMER). Departamento de Anatomía y Embriología Humana. Facultad de Medicina, Avenida de Madrid s/n, 18071 Granada (Spain)
b Departamento de Química Farmacéutica y Orgánica. Facultad de Farmacia, c/ Campus de Cartuja s/n, 18071 Granada (Spain)
Abstract available at http://www.mdpi.org/molecules/specialissues/fluorouracil.htm
Paper received: 13 May 2008

Manuscript ID: fluorouracil-20080415-Nishimoto-jp
Title: Radiation- and photo-induced activation of 5-fluorouracil prodrugs as a strategy for selective treatment of solid tumors
Authors: Sei-ichi Nishimoto, Kazuhito Tanabe, Takeo Ito, Hisatsugu Yamada,and Hiroshi Hatta
Corresponding author: Sei-ichi Nishimoto, Ph.D. Professor of Excited-State Hydrocarbon Chemistry, Graduate School of Engineering, Kyoto University, Katsura Campus, Kyoto 615-8530, Japan
Tel: +81-75-383-2500/FAX: +81-75-383-2501
E-mail: nishimot@scl.kyoto-u.ac.jp
URL: http://www.ehcc.kyoto-u.ac.jp/eh32/home/web-content/index-e.htm
Abstract: Nowadays, 5-fluorouracil (5FU) is widely used as an anticancer drug to treat solid cancers, such as colon, breast, rectal, and pancreatic cancers, although its clinical application is limited because 5FU shows gastrointestinal and hematological toxicities. A great deal of efforts have been made in the search for prodrugs with functions that are
tumor-selectively delivered and activated to improve the clinical utility of 5FU as an important cancer chemotherapeutic agent. Since UV-light and ionizing radiations can cause chemical reactions in a localized area of the body,their applications into site-specific drug activation and sensitization have been thus developed. In this review, we describe recent progress in
The development of novel 5FU prodrugs that are site-specifically activated by UV-light and ionizing radiations under tumor microenvironments, and discuss chemical mechanisms of the activation.

Francesco Puoci ^1,*, Francesca Iemma ¹, Giuseppe Cirillo ¹, Nevio Picci ¹, Pietro Matricardi ² and Franco Alhaique ²
1 Dipartimento di Scienze Farmaceutiche, Università della Calabria, Edificio Polifunzionale, Arcavacata di Rende (CS) 87036, Italy
2 Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, University “La Sapienza”, P.le A. Moro 5, 00185 Roma, Italy
* Author to whom correspondence should be addressed; email: francesco.puoci@unical.it; Tel. (+39) 0984493151, fax (+39) 0984493151
Received: 21 March 2007; in revised form: 13 March 2007 / Accepted: 16 April 2007 / Published: 18 April 2007
Full Paper: Molecularly Imprinted Polymers for 5-Fluorouracil Release in Biological Fluids
Molecules 2007, 12, 805-814 (PDF format 69 K)