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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

Novel Artemisinin-Derived Dimers: Synthesis and Evaluation of Anti-cancer Activities

Author(s): Vu Tuan Kien, Le Huy Binh, Phan Hai Phong, Doan Thi Hien, Nguyen Thi Thuy My, Nguyen Hai Nam, Do Thi Thao, Michael Baltas and Tran Khac Vua

Volume 14, Issue 1, 2017

Page: [102 - 111] Pages: 10

DOI: 10.2174/1570180813666160810155354

Price: $65


In continuation of our study on anticancer compounds, a series of novel artemisinin dimers have been synthesized and evaluated for their cytotoxic effects against three human cancer cell lines, including HepG2 (liver cancer), MCF-7(breast cancer) and HL-60 (leukemia cancer). The assay results showed that most of the compounds displayed inhibitory effects against all three human cancer cell lines tested, and seemed to be more cytotoxic toward the blood cancer cells (HL-60) than liver (HepG2), and breast (MCF-7) cancer cells. Among the synthesized artemisinin dimers, the compound 10d with a double bond bridge exhibited the most potent cytotoxicity with IC50 values of 5.08, 4.82 and 1.32 µg/mL against the HepG2, MCF-7, and HL-60 cell lines, respectively.

Keywords: Artemisinin, cytotoxicity, antimalarial, cancer, dimer.

Graphical Abstract

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