Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity
文献类型：期刊论文
| 作者 | Yang, Chao2; Chen, Hui3; Lu, Shihai2; Zhang, Meng2; Tian, Wei2; Wang, Mingping1,2; Zhang, Ling2; Song, Yunlong2; Shen, Aijun4 ; Zhou, Youjun2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2016-08-01 |
| 卷号 | 26期号:15页码:3464-3467 |
| 关键词 | Luteolin Flos Chrysanthemi Structural modification Bcl-2 protein Anti-tumor |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2016.06.043 |
| 文献子类 | Article |
| 英文摘要 | The luteolin from Flos Chrysanthemi was found to directly bind to the Bcl-2 protein and inhibit the tumor cell growth in our previous study. However, it has been shown to possess wide and week biological activities. In this study, a series of derivatives of luteolin were designed and synthesized, and their tumor cell growth inhibitory activities were evaluated against human leukemia cell line HL-60. The results showed that compounds 1B-2, 2A-3, and 2B-5, with hydrophobic substituted benzyl groups introduced to B ring and hydrogen or methyl introduced to 7-OH group of luteolin, exhibited the strongest inhibitory activity with the IC50 lower than 10 mu M, which were significantly more potent than luteolin. The studies presented here offer a good example for modifications of flavones to improve their tumor cell growth inhibitory activities. (C) 2016 Elsevier Ltd. All rights reserved. |
| WOS关键词 | FLAVONOID LUTEOLIN |
| 资助项目 | Shanghai Municipal Education Commission[00000000] ; Shanghai Education Development Foundation of China[12CG42] ; State Key laboratory of Drug Research of China[SIMM1601KF-01] ; National Natural Science Foundation of China[21172260] ; National Natural Science Foundation of China[21572266] ; Shanghai Rising-Star Program of China[16QA1404800] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000380574100014 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275941]  |
| 专题 | 药理学第一研究室 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 | Zhou, Youjun; Zhu, Ju; Zheng, Canhui |
| 作者单位 | 1.China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China; 2.Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China; 3.Second Mil Med Univ, Changhai Hosp, Shanghai 200433, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Chao,Chen, Hui,Lu, Shihai,et al. Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2016,26(15):3464-3467. |
| APA | Yang, Chao.,Chen, Hui.,Lu, Shihai.,Zhang, Meng.,Tian, Wei.,...&Zheng, Canhui.(2016).Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,26(15),3464-3467. |
| MLA | Yang, Chao,et al."Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 26.15(2016):3464-3467. |
入库方式： OAI收割
来源：上海药物研究所
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