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

文献类型：期刊论文

作者Wang, Liang-Liang2,3,4; Kong, Lingmei2,3,4; Liu, Hui1; Zhang, Yunqin2,3,4; Zhang, Li1; Liu, Xingyong1; Yuan, Feng2,3,4; Li, Yan2,3,4; Zuo, Zhili1,2,3,4
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2019-11-15
卷号182页码:10
关键词Artemisinin Quinazoline Hybridization Colorectal cancer Chemotherapy
ISSN号0223-5234
DOI10.1016/j.ejmech.2019.111665
通讯作者Li, Yan(liyanb@mail.kib.ac.cn) ; Zuo, Zhili(zuozhili@mail.kib.ac.cn)
英文摘要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.
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000496896600070
源URL[http://ir.kib.ac.cn/handle/151853/70101]  
专题昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室
通讯作者Li, Yan; Zuo, Zhili
作者单位1.Sichuan Univ Sci & Engn, Sch Chem Engn, Zigong, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
3.Yunnan Key Lab Nat Med Chem, Kunming 650201, Yunnan, Peoples R China
4.Chinese Acad Sci, Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
推荐引用方式
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.

入库方式： OAI收割

来源：昆明植物研究所

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