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![]() ![]() | |
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
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ISSN | 0223-5234 |
Volume | 182Pages: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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