Simple and Efficient Synthesis of Anithiactins A-C, Thiasporine A and Their Potent Antitumor 2,4-Linked Oligothiazole Derivatives | |
Liu, Yi1; Ma, Zhanwei1; Zhao, Xiangyun1; Shan, Qiuli4; He, Peng3; Du, Yuguo3; Wang, Yibin2 | |
刊名 | CHEMISTRYSELECT |
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 |
DOI | 10.1002/slct.201803664 |
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. |
资助项目 | State Key Laboratory of Environmental Chemistry and Ecotoxicology[KF2015-07] |
WOS研究方向 | Chemistry |
语种 | 英语 |
出版者 | WILEY-V C H VERLAG GMBH |
WOS记录号 | WOS:000456211600043 |
内容类型 | 期刊论文 |
源URL | [http://ir.fio.com.cn:8080/handle/2SI8HI0U/10916] |
专题 | 业务部门_海洋生态研究中心 |
通讯作者 | Liu, Yi; Wang, Yibin |
作者单位 | 1.Yantai Univ, Sch Chem & Chem Engn, Yantai 264005, Peoples R China 2.State Ocean Adm, Inst Oceanog 1, Key Lab Marine Ecol & Environm Sci & Engn, Qingdao 266061, Peoples R China 3.Chinese Acad Sci, State Key Lab Environm Chem & Ecotoxicol, Res Ctr Ecoenvironm Sci, Beijing 100085, Peoples R China 4.Univ Jinan, Sch Biol Sci & Technol, Jinan 250022, Shandong, 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. |
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