Design, Synthesis, and Antitumor Activities of Isomers of Artemisinin Dimer Derivatives.
Chem Biodivers
; 20(7): e202300615, 2023 Jul.
Article
em En
| MEDLINE
| ID: mdl-37256824
ABSTRACT
In recent years, numerous studies have reported on the anti-tumor properties of artemisinin and its derivatives. However, the relationship between their artemisinin chirality and activity remains unknown. In this study, we synthesized a series of artemisinin dimer derivatives with three different chiral structures and tested their antiproliferative activity in MCF-7 and HepG2 cells using the CCK-8 assay. Interestingly, we discovered that artemisinin dimer derivatives with ß, ß and α, ß conformations at C-10 exhibited stronger anti-tumor activity than those with an α, α configuration in MCF-7 and HepG2 cells. Notably, compound 4 showed an activity of 0.06â
µM in MCF-7 cells. This study demonstrates the relationship between the conformation and activity of artemisinin dimer derivatives, and these derivatives have the potential to be developed into anti-cancer drugs.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Artemisininas
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Antimaláricos
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Antineoplásicos
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article