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

doi:10.1016/j.ejmech.2019.111665

	Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo
	Wang, Liang-Liang 1,2,3; Kong, Lingmei 1,2,3; Liu, Hui 4; Zhang, Yunqin 1,2,3; Zhang, Li 4; Liu, Xingyong 4; Yuan, Feng 1,2,3; Li, Yan1,2,3 ; Zuo, Zhili1,2,3,4
Corresponding Author	Li, Yan(liyanb@mail.kib.ac.cn) ; Zuo, Zhili(zuozhili@mail.kib.ac.cn)
	2019-11-15
Source Publication	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN	0223-5234
Volume	182 Pages:10
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 mu M) and Gefitinib (IC50 = 19.82 mu M). 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. (C) 2019 Elsevier Masson SAS. All rights reserved.
Keyword	Artemisinin Quinazoline Hybridization Colorectal cancer Chemotherapy
DOI	10.1016/j.ejmech.2019.111665
Indexed By	SCI ; SCI
Language	英语
WOS ID	WOS:000496896600070
Citation statistics
Document Type	期刊论文
Identifier	http://ir.kib.ac.cn/handle/151853/70102
Collection	植物化学与西部植物资源持续利用国家重点实验室
Corresponding Author	Li, Yan; Zuo, Zhili
Affiliation	1.Chinese Acad Sci, Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China 2.Yunnan Key Lab Nat Med Chem, Kunming 650201, Yunnan, Peoples R China 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 4.Sichuan Univ Sci & Engn, Sch Chem Engn, Zigong, Peoples R China
Recommended Citation GB/T 7714	Wang, Liang-Liang,Kong, Lingmei,Liu, Hui,et al. Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2019,182:10.
APA	Wang, Liang-Liang.,Kong, Lingmei.,Liu, Hui.,Zhang, Yunqin.,Zhang, Li.,...&Zuo, Zhili.(2019).Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,182,10.
MLA	Wang, Liang-Liang,et al."Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 182(2019):10.

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