中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
首页 机构 成果 学者
  
  1. CAS IR Grid
  2. 上海药物研究所
  3. 中国科学院上海药物研究所
  4. 天然药物化学研究室
Synthesis and Activity Evaluation of Novel 3,4-Dihydro-benzo[b]-oxazepin-5(2H)-one Derivatives as Protein Kinases Inhibitors

文献类型：期刊论文

作者Hou Guige1,2; Jiang Chengshi1,3; Liu Hongchun1; Tong Linjiang1; Peng Xia1; Ji Yinchun1; Geng Meiyu1; Xiao Wei4; Gong Jingxu1; Guo Yuewei1
刊名CHINESE JOURNAL OF ORGANIC CHEMISTRY
出版日期2017-06
卷号37期号:6页码:1463-1472
关键词3,4-dihydro-benzo[b]oxazepin-5(2H)-one derivatives synthesis protein-tyrosine kinases inhibitors ErbB1 ErbB2
ISSN号0253-2786
DOI10.6023/cjoc201611005
文献子类Article
英文摘要A series of novel 3,4-dihydro-benzo[b]oxazepin-5(2H)-one derivatives were designed and synthesized as potent protein-tyrosine kinases (PTKs, e.g. ErbBl, ErbB2, c-Met, ALK, FGFR1, RET, KDR) inhibitors. All compounds were characterized by NMR and MS. E-7-[(2,5-dihydroxy)phenylmethylene]amino-3,4-dihydro-benzo[b]oxazepin-5(213)-one (8k) and E-7-[(2,3,4-trihydroxy)phenylmethylene]amino-3,4-dihydro-benzo[b]oxazepin-5(2H)-one (8n) were further characterized by X-ray single-crystal analysis. The synthesized compounds were further tested for their inhibitory activity on PTKs. The results display compounds with catechol-substitution display the most potent inhibitory activities toward PTKs. The IC50 values for E-7-[(3,4-dihydroxy)phenylmethylene]amino-3,4-dihydro-benzo[b]oxazepin-5(213)-one (8i) against ErbB1, ErbB2 are 1.0 and 0.33 mu mol/L, respectively. The IC50 value for 8n against RET is 0.7 mu mol/L, while the IC50 value for 7-[(3,4-dihydroxyphenyl)methyl]amino-2,3,4,5-tetrahydro-benzo[b]oxazepin-5-ol (10b) against ErbB2 is 1.02 mu mol/L.
WOS关键词CELL LUNG-CANCER ; NATURAL-PRODUCTS ; RECEPTOR
资助项目National Natural Science Foundation of China[81520108028] ; National Natural Science Foundation of China[81273430] ; National Natural Science Foundation of China[21402010] ; National Natural Science Foundation of China[21672230] ; National Natural Science Foundation of China[41506187] ; National Natural Science Foundation of China[81302692] ; National Natural Science Foundation of China[41476063] ; National Natural Science Foundation of China[4167060562] ; National Natural Science Foundation of China[8160131016] ; National Natural Science Foundation of China-Shandong Joint Fund for Marine Science Research Centers[U1406402] ; Shanghai Science and Technology Committee Project[14431901100] ; Shanghai Science and Technology Committee Project[15431901000] ; State Key Laboratory of Drug Research/Shanghai Institute of Materia Medica Projects[SIMM1501ZZ-03] ; Institutes for Drug Discovery and Development, Chinese Academy of Sciences[CASIMM0120152039]
WOS研究方向Chemistry
语种中文
CSCD记录号CSCD:6021387
WOS记录号WOS:000406824700017
出版者SCIENCE PRESS
源URL[http://119.78.100.183/handle/2S10ELR8/272625]  
专题天然药物化学研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Xiao Wei; Gong Jingxu
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
2.Binzhou Med Univ, State Adm Tradit Chinese Med China, Key Lab Prescript Effect & Clin Evaluat, Yantai 264003, Peoples R China;
3.Jinan Univ, Sch Biol Sci & Technol, Jinan 250022, Shandong, Peoples R China;
4.Jiangsu Kanion Pharmaceut Co Ltd, Lianyungang 222001, Peoples R China
推荐引用方式
GB/T 7714		 Hou Guige,Jiang Chengshi,Liu Hongchun,et al. Synthesis and Activity Evaluation of Novel 3,4-Dihydro-benzo[b]-oxazepin-5(2H)-one Derivatives as Protein Kinases Inhibitors[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2017,37(6):1463-1472.
APA Hou Guige.,Jiang Chengshi.,Liu Hongchun.,Tong Linjiang.,Peng Xia.,...&Guo Yuewei.(2017).Synthesis and Activity Evaluation of Novel 3,4-Dihydro-benzo[b]-oxazepin-5(2H)-one Derivatives as Protein Kinases Inhibitors.CHINESE JOURNAL OF ORGANIC CHEMISTRY,37(6),1463-1472.
MLA Hou Guige,et al."Synthesis and Activity Evaluation of Novel 3,4-Dihydro-benzo[b]-oxazepin-5(2H)-one Derivatives as Protein Kinases Inhibitors".CHINESE JOURNAL OF ORGANIC CHEMISTRY 37.6(2017):1463-1472.

入库方式： OAI收割

来源：上海药物研究所

浏览0
下载0
收藏0
其他版本

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。