Anticancer Activity of Chalcones and Its Derivatives: Review and In Silico Studies

Author:

Leite Fernando Ferreira1,de Sousa Natália Ferreira1,de Oliveira Bruno Hanrry Melo1ORCID,Duarte Gabrielly Diniz2ORCID,Ferreira Maria Denise Leite1,Scotti Marcus Tullius1ORCID,Filho José Maria Barbosa1,Rodrigues Luís Cezar2,de Moura Ricardo Olímpio3,Mendonça-Junior Francisco Jaime Bezerra4ORCID,Scotti Luciana1ORCID

Affiliation:

1. Post-Graduate Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, João Pessoa 58051-900, Brazil

2. Post-Graduate Program in Development and Innovation of Drugs and Medicines, Federal University of Paraíba, João Pessoa 58051-900, Brazil

3. Post-Graduate Program in Pharmaceuticals Sciences Paraiba State University, Campina Grande 58429-500, Brazil

4. Laboratory of Synthesis and Drug Delivery, Department of Biological Science, Paraiba State University, João Pessoa 58071-160, Brazil

Abstract

Chalcones are direct precursors in the biosynthesis of flavonoids. They have an α,β-unsaturated carbonyl system which gives them broad biological properties. Among the biological properties exerted by chalcones, their ability to suppress tumors stands out, in addition to their low toxicity. In this perspective, the present work explores the role of natural and synthetic chalcones and their anticancer activity in vitro reported in the last four years from 2019 to 2023. Moreover, we carried out a partial least square (PLS) analysis of the biologic data reported for colon adenocarcinoma lineage HCT-116. Information was obtained from the Web of Science database. Our in silico analysis identified that the presence of polar radicals such as hydroxyl and methoxyl contributed to the anticancer activity of chalcones derivatives. We hope that the data presented in this work will help researchers to develop effective drugs to inhibit colon adenocarcinoma in future works.

Funder

Coordination of Improvement of Higher Education Personnel—Brazil

Conselho Nacional de Desenvolvimento Científico e Tecnológico

Paraíba State Research Foundation

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

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