Design and synthesis of novel artemisinin derivatives with potent activities against colorectal cancer in vitro and in vivo
Wang, Liang-Liang1,2,3; Kong, Lingmei1,2,3; Liu, Hui4; Zhang, Yunqin1,2,3; Zhang, Li4; Liu, Xingyong4; Yuan, Feng1,2,3; Li, Yan1,2,3; Zuo, Zhili1,2,3,4
Corresponding AuthorLi, Yan(liyanb@mail.kib.ac.cn) ; Zuo, Zhili(zuozhili@mail.kib.ac.cn)
2019-11-15
Source PublicationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
Volume182Pages:10
AbstractA 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.
KeywordArtemisinin Quinazoline Hybridization Colorectal cancer Chemotherapy
DOI10.1016/j.ejmech.2019.111665
Indexed BySCI ; SCI
Language英语
WOS IDWOS:000496896600070
Citation statistics
Document Type期刊论文
Identifierhttp://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 AuthorLi, Yan; Zuo, Zhili
Affiliation1.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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