In Vitro Antioxidant and Pancreatic Anticancer Activity of Novel 5-Fluorouracil-Coumarin Conjugates

Author:

López Sonia,Gracia Ignacio,Plaza-Pedroche Rodrigo,Rodríguez Juan FranciscoORCID,Pérez-Ortiz José ManuelORCID,Rodríguez-López JuliánORCID,Ramos María JesúsORCID

Abstract

Molecular hybridization consists of the combination of two or more non-identical pharmacophores in a single molecule. It has emerged as a promising strategy that allows the design of molecular frameworks with enhanced activity and affinity compared to their parent drugs. In this work, two novel hybrids that combine the well-known anticancer chemotherapeutic agent 5-fluorouracil with antioxidant coumarin derivatives have been synthesized and characterized by means of a copper-catalyzed azide-alkyne cycloaddition (CuAAC). The conjugates showed good antioxidant properties and a high tendency to aggregate and form stable nanoparticles in aqueous media, with regular shape and uniform size. These materials have proven to be preferential cytotoxic agents in vitro against human pancreatic cancer cells PANC-1, with an activity superior to free 5-fluorouracil. These results open up the possibility of exploiting the synergistic combination between 5-fluorouracil and coumarin derivatives and warrant further investigation of these hybrids as promising pancreatic anticancer agents.

Funder

Ministerio de Economía y Competitividad/Agencia Estatal de Investigación/FEDER

Publisher

MDPI AG

Subject

Pharmaceutical Science

Reference60 articles.

1. Latest Global Cancer Data: Cancer Burden Rises to 18.1 Million New Cases and 9.6 Million Deaths in 2018;World Health Organization (WHO),2018

2. World Cancer Report 2014,2014

3. Cancer prevention from the perspective of global cancer burden patterns

4. Global Cancer Statistics 2020: GLOBOCAN Estimates of Incidence and Mortality Worldwide for 36 Cancers in 185 Countries

5. Drug Combination in Cancer Treatment—From Cocktails to Conjugated Combinations

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