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Review
. 2023 May 10;28(10):4009.
doi: 10.3390/molecules28104009.

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

Fernando Ferreira Leite  1 , Natália Ferreira de Sousa  1 , Bruno Hanrry Melo de Oliveira  1 , Gabrielly Diniz Duarte  2 , Maria Denise Leite Ferreira  1 , Marcus Tullius Scotti  1 , José Maria Barbosa Filho  1 , Luís Cezar Rodrigues  2 , Ricardo Olímpio de Moura  3 , Francisco Jaime Bezerra Mendonça-Junior  4 , Luciana Scotti  1
Affiliations
Review

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

Fernando Ferreira Leite et al. Molecules. .

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.

Keywords: anticancer activity; chalcones; drug discovery; in vitro; natural products; synthesis.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Chemical structure of a chalcone.
Figure 2
Figure 2
Chemical structure of benzocoumarin-chalcones.
Figure 3
Figure 3
Chemical structure of chalcones, MIPP and MOMIPP.
Figure 4
Figure 4
Chemical structure of TNF-α inhibitor compounds.
Figure 5
Figure 5
Chemical structure of colon cancer inhibitor compounds.
Figure 6
Figure 6
Chemical structure of lung cancer inhibitor compounds.
Figure 7
Figure 7
Chemical structure of breast cancer inhibitor compounds.
Figure 8
Figure 8
Chemical structure of oral cancer inhibitor compounds.
Figure 9
Figure 9
Chemical structure of leukemia inhibitor compounds.
Figure 10
Figure 10
Chemical structure of hepatocarcinoma inhibitor compounds.
Figure 11
Figure 11
Chemical structure of cervical cancer inhibitor compounds.
Figure 12
Figure 12
Chemical structure of glioblastoma inhibitor compounds.
Figure 13
Figure 13
Chemical structure of melanoma inhibitor compounds.
Figure 14
Figure 14
Chemical structure of the series of compounds submitted to PLS analysis. (A) Active compounds; (B) inactive compounds.
Figure 14
Figure 14
Chemical structure of the series of compounds submitted to PLS analysis. (A) Active compounds; (B) inactive compounds.
Figure 15
Figure 15
Arrangement of objects in relation to the activity of compounds.
Figure 16
Figure 16
Coefficient graph generated from the PLS model.
See this image and copyright information in PMC

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