2. Academic Validation
  3. Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo

Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo

  • Eur J Med Chem. 2019 Nov 15:182:111665. doi: 10.1016/j.ejmech.2019.111665.
Liang-Liang Wang 1,  Lingmei Kong 1,  Hui Liu 2,  Yunqin Zhang 1,  Li Zhang 2,  Xingyong Liu 2,  Feng Yuan 1,  Yan Li 3,  Zhili Zuo 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Phytochemistry and Plant Resources in West China, Institute of Botany, Chinese Academy of Sciences, Kunming, 650201, PR China; Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming, 650201, PR China; University of Chinese Academy of Sciences, Beijing, 100049, PR China.
  • 2 School of Chemical Engineering, Sichuan University of Science & Engineering, Zigong, China.
  • 3 State Key Laboratory of Phytochemistry and Plant Resources in West China, Institute of Botany, Chinese Academy of Sciences, Kunming, 650201, PR China; Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming, 650201, PR China; University of Chinese Academy of Sciences, Beijing, 100049, PR China. Electronic address: liyanb@mail.kib.ac.cn.
  • 4 State Key Laboratory of Phytochemistry and Plant Resources in West China, Institute of Botany, Chinese Academy of Sciences, Kunming, 650201, PR China; Yunnan Key Laboratory of Natural Medicinal Chemistry, Kunming, 650201, PR China; University of Chinese Academy of Sciences, Beijing, 100049, PR China; School of Chemical Engineering, Sichuan University of Science & Engineering, Zigong, China. Electronic address: zuozhili@mail.kib.ac.cn.
PMID: 31494469 DOI: 10.1016/j.ejmech.2019.111665
Abstract

A series of novel derivatives of artemisinin-4-(arylamino)quinazoline have been designed and synthesized, and most of them showing potent in vitro cytotoxic activity against HCT116 and WM-266-4 cell lines. Compound 32 was the most active derivative against HCT116 cell line with an IC50 of 110 nM, and significantly improved the antitumor activity of the parent compounds dihydroartemisinin (DHA) (IC50 = 2.85 μM) and Gefitinib (IC50 = 19.82 μM). In vivo HCT116 xenografts assay showed that compound 32 exhibited potent antitumor activity with obvious tumor growth delay and tumor shrunken after 18 days treatment on xenografted mice, and especially without loss of body weight. Our results indicate that compounds 32 may represent a safe, novel structural lead for developing new chemotherapy of colorectal Cancer.

Keywords

Artemisinin; Chemotherapy; Colorectal cancer; Hybridization; Quinazoline.

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