Design, Synthesis, and Antitumor Activities of Isomers of Artemisinin Dimer Derivatives

Author:

Yue Lingyun1,Pan Yanna2,Wang Jiaoying2,Yue Lin23,Luo Yuxuan2,Lv Fang2,Lv Jiagang2,Chen Jianping2,Zhao Qingjie2ORCID,Lin Haixia1

Affiliation:

1. Department of Chemistry College of Sciences Shanghai University 99 Shangda Road, Baoshan District Shanghai 200444 China

2. Innovation Research Institute of Traditional Chinese Medicine Shanghai University of Traditional Chinese Medicine Shanghai 201203 China

3. College of Life Sciences Shanghai Normal University Shanghai 201418 China

Abstract

AbstractIn 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 β, β and α, β 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 0.06 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.

Funder

National Natural Science Foundation of China

Shanghai University of Traditional Chinese Medicine

Publisher

Wiley

Subject

Molecular Biology,Molecular Medicine,General Chemistry,Biochemistry,General Medicine,Bioengineering

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