Synthetic derivatives of the natural product 13-amino 2-desoxy-4-epi-pulchellin inhibit STAT3 signaling and induce G2/M arrest and death of colon cancer cells

doi:10.1016/j.bmcl.2019.01.030

	Synthetic derivatives of the natural product 13-amino 2-desoxy-4-epi-pulchellin inhibit STAT3 signaling and induce G2/M arrest and death of colon cancer cells
	Niu, Junxing 2,4; Huang, Hui 3,4; Wang, Fei 3,4; Zhang, Xianjing 2,4; Liu, Yi 2,4; Yu, Qiang 3,4; Hu, Lihong 1
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2019-03-15
卷号	29 期号:6 页码:782-785
关键词	Sesquiterpene-lactone JAK2/STAT3 Michael addition reaction Antitumor Colorectal carcinoma
ISSN号	0960-894X
DOI	10.1016/j.bmcl.2019.01.030
通讯作者	Yu, Qiang(qyu@sibs.ac.cn) ; Hu, Lihong(lhhu@njucm.edu.cn)
英文摘要	2-Desoxy-4-epi-puchellin (PCL) is a sesquiterpene-lactone, which naturally occurs in many traditional Chinese medicinal plants, and has antitumor and anti-inflammatory activities. In this work, a series of 13-amino derivatives of PCL were synthesized through Michael addition reaction. Inhibition of IL-6-induced STAT3 signaling pathway and in vitro cytotoxicity of these compounds were evaluated, and their effect on the cell cycle was also studied. The methyl hydroxyethylamine derivatives showed higher potency than PCL, which could induce significant mitotic arrest via G2/M arrest in HCT116 cancer cells, indicating that these derivatives have the potential to be developed into anti-colon cancer drugs.
资助项目	National Natural Science Foundation of China[81673465] ; China Ministry of Science and Technology Key New Drug Creation and Manufacturing Program[2014ZX9102001002] ; Natural science foundation of Jiangsu Higher Education Institutions[17KJA360004] ; Program for Outstanding Scientific and Technological Innovation Team of Jiangsu Higher Education Institutions ; Priority Academic Program Development of Jiangsu Higher Education Institutions
WOS关键词	SESQUITERPENOIDS ; CYTOTOXICITY ; INFLAMMATION
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000458623500003
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/290516]
专题	中国科学院上海药物研究所
通讯作者	Yu, Qiang; Hu, Lihong
作者单位	1.Nanjing Univ Chinese Med, Jiangsu Key Lab Funct Subst Chinese Med, Sch Pharm, Nanjing 210023, Jiangsu, Peoples R China 2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Meteria Med, 501 Haike Rd, Shanghai 201203, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Mediu, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 4.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
推荐引用方式 GB/T 7714	Niu, Junxing,Huang, Hui,Wang, Fei,et al. Synthetic derivatives of the natural product 13-amino 2-desoxy-4-epi-pulchellin inhibit STAT3 signaling and induce G2/M arrest and death of colon cancer cells[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2019,29(6):782-785.
APA	Niu, Junxing.,Huang, Hui.,Wang, Fei.,Zhang, Xianjing.,Liu, Yi.,...&Hu, Lihong.(2019).Synthetic derivatives of the natural product 13-amino 2-desoxy-4-epi-pulchellin inhibit STAT3 signaling and induce G2/M arrest and death of colon cancer cells.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,29(6),782-785.
MLA	Niu, Junxing,et al."Synthetic derivatives of the natural product 13-amino 2-desoxy-4-epi-pulchellin inhibit STAT3 signaling and induce G2/M arrest and death of colon cancer cells".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 29.6(2019):782-785.