Design,synthesis and antiproliferative activity of 3-hydroxy-4-quinolone compounds

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药物发现与设计中心

	Design,synthesis and antiproliferative activity of 3-hydroxy-4-quinolone compounds
	Wang Fenghua 2; Wang Kai 1; Shen Jianhua1 ; Chen Kaixian2
刊名	Journal of China Pharmaceutical University
	2014
卷号	45 期号:3 页码:286-292
关键词	3-hydroxy-4-quinolone combination synthesis antiproliferative activity structural-activity relationship
ISSN号	1000-5048
其他题名	3-羟基-4-喹诺酮类化合物的设计、合成及其抗增殖活性
文献子类	Article
英文摘要	A combination of the structural features of dihydromyricetin and quinolone antineoplastic compounds gave rise to 3-hydroxy-4-quinolone motif. Starting from 3,5-dimethoxyaniline,the target compounds were prepared through a reaction cascade,including reductive amination,Friedel-Crafts reaction,microwave assisted ring closure,BBr_3 catalyzed demethylation and Mannich reaction. Sixteen novel compounds were synthesized,and their structures were confirmed by IR,MS and ~1H NMR. The antiproliferative activities of the compounds against A549 and NCI-H 460 cells were tested in MTT assay. Several compounds exhibited moderate antiproliferative activities against both cell lines,of which,compound 11b displayed the most robust inhibition towards NCI-H 460. Preliminary structural-activity relationships indicated that introduction of isopentenyl into the N-1 position of 3-hydroxy-4-quinolone motif would significantly improve the potency of the compounds.
WOS研究方向	Pharmacology & Pharmacy (provided by Clarivate Analytics)
语种	中文
CSCD记录号	CSCD:5178677
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/269333]
专题	药物发现与设计中心
通讯作者	Chen Kaixian
作者单位	1.State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences, Shanghai 201203, China. 2.College of Traditional Chinese Medicine,Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.;
推荐引用方式 GB/T 7714	Wang Fenghua,Wang Kai,Shen Jianhua,et al. Design,synthesis and antiproliferative activity of 3-hydroxy-4-quinolone compounds[J]. Journal of China Pharmaceutical University,2014,45(3):286-292.
APA	Wang Fenghua,Wang Kai,Shen Jianhua,&Chen Kaixian.(2014).Design,synthesis and antiproliferative activity of 3-hydroxy-4-quinolone compounds.Journal of China Pharmaceutical University,45(3),286-292.
MLA	Wang Fenghua,et al."Design,synthesis and antiproliferative activity of 3-hydroxy-4-quinolone compounds".Journal of China Pharmaceutical University 45.3(2014):286-292.