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

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

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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