Synthesis and structure-activity relationships of boswellic acid derivatives as potent VEGFR-2 inhibitors
文献类型：期刊论文
| 作者 | Shen, Sida; Xu, Xingyu; Liu, Zhulong; Liu, Junhua; Hu, Lihong |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2015-05-01 |
| 卷号 | 23期号:9页码:1982-1993 |
| 关键词 | Acetyl-11-keto-beta-boswellic acid VEGFR-2 Synthesis Structure-activity relationship |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2015.03.022 |
| 文献子类 | Article |
| 英文摘要 | A series of AKBA derivatives were synthesized, and evaluated as potent VEGFR-2 inhibitors. The initial biological evaluation indicated that the introduction of C-24 amide group or a heterocycle at C-2,3 position effectively improved the potency. Further structure-activity relationship analysis showed that amide (7, 23, 25, and 26) and heterocycle (19, 34, and 36) substituted AKBA derivatives displayed more potential anti-proliferation activities than AKBA (1) on HUVECs that express high levels of VEGFR-2. Among all tested compounds, compounds 7 and 19 exhibited the best potency (IC50: 2.36 and 2.13 mu M) and obvious inhibitory activities with VEGFR-2 inhibition rates of 96% and 94% at 50 mu M, respectively. (C) 2015 Elsevier Ltd. All rights reserved. |
| WOS关键词 | GROWTH IN-VIVO ; NATURAL-PRODUCT ; TUMOR-GROWTH ; ANGIOGENESIS ; CANCER |
| 资助项目 | National Science Foundation of China[81273397] ; National Science Foundation of China[81473110] ; National Science Foundation of China[81402811] ; Chinese National Science & Technology Major Project 'Key New Drug Creation and Manufacturing Program'[2013ZX09508104] ; Chinese Postdoctoral Science Foundation[2014M550255] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000352698700008 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276559]  |
| 专题 | 上海中药现代化研究中心 |
| 通讯作者 | Liu, Junhua |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Shen, Sida,Xu, Xingyu,Liu, Zhulong,et al. Synthesis and structure-activity relationships of boswellic acid derivatives as potent VEGFR-2 inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2015,23(9):1982-1993. |
| APA | Shen, Sida,Xu, Xingyu,Liu, Zhulong,Liu, Junhua,&Hu, Lihong.(2015).Synthesis and structure-activity relationships of boswellic acid derivatives as potent VEGFR-2 inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,23(9),1982-1993. |
| MLA | Shen, Sida,et al."Synthesis and structure-activity relationships of boswellic acid derivatives as potent VEGFR-2 inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 23.9(2015):1982-1993. |
入库方式： OAI收割
来源：上海药物研究所
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