Artemisinin-indole and artemisinin-imidazole hybrids: Synthesis, cytotoxic evaluation and reversal effects on multidrug resistance in MCF-7/ADR cells

Bioorg Med Chem Lett. 2019 May 1;29(9):1138-1142. doi: 10.1016/j.bmcl.2019.02.021.

Yanping Hu ¹, Na Li ¹, Jiayao Zhang ¹, Ying Wang ¹, Li Chen ², Jianbo Sun ³

Affiliations

1 State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, School of Traditional Chinese Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China.
2 State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, School of Traditional Chinese Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China. Electronic address: chenli627@cpu.edu.cn.
3 State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, School of Traditional Chinese Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China. Electronic address: sjbcpu@gmail.com.

PMID: 30837097 DOI: 10.1016/j.bmcl.2019.02.021

Abstract

A series of artemisinin derivatives with MDR reversal activity were designed and synthesized. All hybrids were screened to Anticancer activities against four human Cancer cell lines (A549, MCF-7, HepG-2, MDA-MB-231) and normal human hepatic cell (L02) in vitro. Most of the new compounds showed higher Anticancer activities than artemisinin, among which compounds 11a and 11c displayed superior potency with IC₅₀ 6.78 μM and 5.25 μM against MCF-7, respectively. The further research indicated that the most potent 11c induced cell cycle arrest at G2 phase in MCF-7. Additionally, compound 11c showed remarkable MDR reversal activity which reversed adriamycin against MCF-7/ADR cells with IC₅₀ 0.76 μM.

Keywords

Anticancer activities; Artemisinin; Imidazole; Indole; MDR reversal activity.

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