Chemistry and Anticancer Activity of Hybrid Molecules and Derivatives based on 5-Fluorouracil

Title:Chemistry and Anticancer Activity of Hybrid Molecules and Derivatives based on 5-Fluorouracil

Volume: 28 Issue: 27

Author(s): Wilson Cardona-G*, Angie Herrera-R, Wilson Castrillón-L and Howard Ramírez-Malule

Affiliation:

• Quimica de Plantas Colombianas, Institute of Chemistry, Faculty of Exact and Natural Sciences, University of Antioquia UdeA, Calle 70 No. 52-21, A.A 1226 Medellin,Colombia

Keywords: 5-fluorouracil, cancer, anticancer activity, hybrid compounds, conjugate, structure-activity relationship (SAR).

Abstract:

Considering that cancer continues to be an important cause of death worldwide, several conventional anticancer treatments are widely used. However, most of them display low selectivity against malignant cells and induce many adverse side effects. Among these, the use of therapies based on 5-Fluorouracil (5-FU) has been one of the most efficient, with a broad-spectrum. Due to these circumstances, various modifications of 5-FU have been developed to improve drug delivery and reduce side effects. Among the optimization strategies, modifications of 5-FU at N1 or N3 position are made, usually including the incorporation of pharmacologically active compounds with anticancer activity (called hybrid molecule) and functionalization with other groups of compounds (called conjugates).

Several studies have been conducted in the search for new alternative therapies against cancer. Many of them have evidenced that hybrid compounds exhibit good anticancer activity, which has emerged as a promising strategy in this field of drug discovery and development. Furthermore, the binding of 5-FU to amino acids, peptides, phospholipids, polymers, among others, improves metabolic stability and absorption.

This review highlights the potential of hybrids and derivatives based on 5-FU as a scaffold for the development of antitumor agents. Besides, it also presents a detailed description of the different strategies employed to design and synthesized these compounds, together with their biological activities and structure-activity relationship (SAR) analysis.

Cite this article as:

Cardona-G Wilson *, Herrera-R Angie , Castrillón-L Wilson and Ramírez-Malule Howard , Chemistry and Anticancer Activity of Hybrid Molecules and Derivatives based on 5-Fluorouracil, Current Medicinal Chemistry 2021; 28 (27) . https://dx.doi.org/10.2174/0929867328666210211164314