中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Simple and Efficient Synthesis of Anithiactins A-C, Thiasporine A and Their Potent Antitumor 2,4-Linked Oligothiazole Derivatives

文献类型:期刊论文

作者Liu, Yi; Ma, Zhanwei; Zhao, Xiangyun; Shan, Qiuli; He, Peng; Du, Yuguo; Wang, Yibin
刊名CHEMISTRYSELECT
出版日期2019-01-17
卷号4期号:2页码:742-746
关键词2,4 '-linked oligothiazole 2-phenylthiazole thiasporine A anithiactins A-C antitumor activity
ISSN号2365-6549
英文摘要Directly 2,4-linked oligothiazoles are not only broadly applied in drug discovery but also are the core structural motif of many biological natural products. With this background, we reported a simple and efficient route for the synthesis of four 2-phenylthiazole natural products anithiactins A-C, thiasporine A, and series of their novel 2,4-linked oligothiazole derivatives relies on the one-pot cascade reaction of beta-azido disulfides and commercially carboxyl acids. This approach also represented a remarkably direct and simple route for 2,4-linked oligothiazoles synthesis. By doing so, ten bisthiazoles and terthiazoles were effectively obtained in only 3 similar to 6 linear steps with good to moderate yields. The bioassay results demonstrated that all the phenyl-based oligothiazoles show potent antitumor activities. Among them, terthiazole 28 was the most potent compound with IC50 values of 4.4 mu M, 4.8 mu M against HCT116 and A549 cell lines, respectively.
源URL[http://ir.rcees.ac.cn/handle/311016/43014]  
专题生态环境研究中心_环境化学与生态毒理学国家重点实验室
作者单位1.Univ Jinan, Sch Biol Sci & Technol, Jinan 250022, Shandong, Peoples R China
2.State Ocean Adm, Inst Oceanog 1, Key Lab Marine Ecol & Environm Sci & Engn, Qingdao 266061, Peoples R China
3.Yantai Univ, Sch Chem & Chem Engn, Yantai 264005, Peoples R China
4.Chinese Acad Sci, State Key Lab Environm Chem & Ecotoxicol, Res Ctr Ecoenvironm Sci, Beijing 100085, Peoples R China
推荐引用方式
GB/T 7714
Liu, Yi,Ma, Zhanwei,Zhao, Xiangyun,et al. Simple and Efficient Synthesis of Anithiactins A-C, Thiasporine A and Their Potent Antitumor 2,4-Linked Oligothiazole Derivatives[J]. CHEMISTRYSELECT,2019,4(2):742-746.
APA Liu, Yi.,Ma, Zhanwei.,Zhao, Xiangyun.,Shan, Qiuli.,He, Peng.,...&Wang, Yibin.(2019).Simple and Efficient Synthesis of Anithiactins A-C, Thiasporine A and Their Potent Antitumor 2,4-Linked Oligothiazole Derivatives.CHEMISTRYSELECT,4(2),742-746.
MLA Liu, Yi,et al."Simple and Efficient Synthesis of Anithiactins A-C, Thiasporine A and Their Potent Antitumor 2,4-Linked Oligothiazole Derivatives".CHEMISTRYSELECT 4.2(2019):742-746.

入库方式: OAI收割

来源:生态环境研究中心

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