Synthesis and in vitro cytotoxic evaluation of novel -(3,4,5-trimethoxyphenyl)pyridin-2()-one derivatives

doi:10.1007/s11030-013-9442-1

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	Synthesis and in vitro cytotoxic evaluation of novel -(3,4,5-trimethoxyphenyl)pyridin-2()-one derivatives
	Chen, Taijie 1; Luo, Yu 1; Sheng, Li 3; Li, Jia3 ; Hu, Youhong3 ; Lu, Wei 2
刊名	MOLECULAR DIVERSITY
	2013-08
卷号	17 期号:3 页码:435-444
关键词	Pyridin-2(1H)-one Combretastatin A-4 Chan-Lam coupling reaction Buchwald-Hartwig coupling reaction HCT-116 Cytotoxicity Cell cycle
ISSN号	1381-1991
DOI	10.1007/s11030-013-9442-1
文献子类	Article
英文摘要	A series of novel -(3,4,5-trimethoxyphenyl)pyridin-2()-one derivatives were designed, synthesized, and evaluated for their in vitro cytotoxicity against human colon cancer cells HCT-116. The key steps involved consecutive Chan-Lam- and Buchwald-Hartwig couplings. Most of these C-6 substituted pyridone derivatives showed moderate antiproliferative activity. The preliminary SAR indicated that the conformationally restricted pyridones exhibited more potent cytotoxicity than the flexible counterparts. In addition, cell cycle analysis of the selected compounds 4b and e showed a G2/M arrest, suggesting a possible antitubulin mechanism for these novel pyridone derivatives.
资助项目	National Natural Science Foundation of China[81172936] ; National Natural Science Foundation of China[21102046] ; Fundamental Research Funds for the Central Universities[00000000] ; Laboratory of Organic Functional Molecules, the Sino-French Institute of ECNU[00000000]
WOS关键词	COMBRETASTATIN A-4 DERIVATIVES ; 2-PYRIDONE DERIVATIVES ; ANTIMITOTIC AGENTS ; INHIBITORS ; DISCOVERY ; RECEPTOR ; POTENT ; PYRIDIN-2(1H)-ONE ; ANALOGS ; MOIETY
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	SPRINGER
WOS记录号	WOS:000321912600003
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277523]
专题	国家新药筛选中心药物化学研究室药物安全性评价中心
通讯作者	Luo, Yu
作者单位	1.E China Normal Univ, Dept Chem, Shanghai 200062, Peoples R China; 2.E China Normal Univ, Inst Drug Discovery & Dev, Shanghai 200062, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Chen, Taijie,Luo, Yu,Sheng, Li,et al. Synthesis and in vitro cytotoxic evaluation of novel -(3,4,5-trimethoxyphenyl)pyridin-2()-one derivatives[J]. MOLECULAR DIVERSITY,2013,17(3):435-444.
APA	Chen, Taijie,Luo, Yu,Sheng, Li,Li, Jia,Hu, Youhong,&Lu, Wei.(2013).Synthesis and in vitro cytotoxic evaluation of novel -(3,4,5-trimethoxyphenyl)pyridin-2()-one derivatives.MOLECULAR DIVERSITY,17(3),435-444.
MLA	Chen, Taijie,et al."Synthesis and in vitro cytotoxic evaluation of novel -(3,4,5-trimethoxyphenyl)pyridin-2()-one derivatives".MOLECULAR DIVERSITY 17.3(2013):435-444.