Molecular Hybridization as a Strategy for Developing Artemisinin-Derived Anticancer Candidates.

Autor: Marchesi E; Department of Environmental and Prevention Sciences, University of Ferrara, 44121 Ferrara, Italy., Perrone D; Department of Environmental and Prevention Sciences, University of Ferrara, 44121 Ferrara, Italy., Navacchia ML; Institute for Organic Synthesis and Photoreactivity (ISOF), National Research Council of Italy (CNR), 40129 Bologna, Italy.
Jazyk: angličtina
Zdroj: Pharmaceutics [Pharmaceutics] 2023 Aug 23; Vol. 15 (9). Date of Electronic Publication: 2023 Aug 23.
DOI: 10.3390/pharmaceutics15092185
Abstrakt: Artemisinin is a natural compound extracted from Artemisia species belonging to the Asteraceae family. Currently, artemisinin and its derivatives are considered among the most significant small-molecule antimalarial drugs. Artemisinin and its derivatives have also been shown to possess selective anticancer properties, however, there are several limitations and gaps in knowledge that retard their repurposing as effective anticancer agents. Hybridization resulting from a covalent combination of artemisinin with one or more active pharmacophores has emerged as a promising approach to overcome several issues. The variety of hybridization partners allows improvement in artemisinin activity by tuning the ability of conjugated artemisinin to interact with various molecule targets involved in multiple biological pathways. This review highlights the current scenario of artemisinin-derived hybrids with potential anticancer activity. The synthetic approaches to achieve the corresponding hybrids and the structure-activity relationships are discussed to facilitate further rational design of more effective candidates.
Databáze: MEDLINE
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