Simple and Efficient Synthesis of Anithiactins A-C, Thiasporine A and Their Potent Antitumor 2,4-Linked Oligothiazole Derivatives

doi:10.1002/slct.201803664

	Simple and Efficient Synthesis of Anithiactins A-C, Thiasporine A and Their Potent Antitumor 2,4-Linked Oligothiazole Derivatives
	Liu, Yi 1; Ma, Zhanwei 1; Zhao, Xiangyun 1; Shan, Qiuli 4; He, Peng 3; Du, Yuguo 3; Wang, Yibin 2
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关键词	2,4-DISUBSTITUTED THIAZOLES ; FERMENTATION ; CYCLOPEPTIDE ; ANTIBIOTICS
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/26152]
专题	自然资源部第一海洋研究所
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.