Indole derivatives as potent inhibitors of 5-lipoxygenase: Design, synthesis, biological evaluation, and molecular modeling
文献类型：期刊论文
| 作者 | Zheng, Mingfang; Zheng, Mingyue ; Ye, Deju; Deng, Yangmei; Qiu, Shuifeng; Luo, Xiaomin; Chen, Kaixian; Liu, Hong; Jiang, Hualiang
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2007-05-01 |
| 卷号 | 17期号:9页码:2414-2420 |
| 关键词 | indole derivatives 5-lipoxygenase inhibitor molecular modeling |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2007.02.038 |
| 文献子类 | Article |
| 英文摘要 | A series of novel indole derivatives was designed, synthesized and evaluated by cell-based assays for their inhibitory activities against 5-LOX in rat peritoneal leukocytes. Most of them (30 out of 35) showed an inhibitory potency higher than the initial screening hit 1a (IC50 = 74 mu M). Selected compounds for concentration-response studies showed prominent inhibitory activities with IC50 values ranging from 0.74 mu M to 3.17 mu M. Four compounds (1m, 1s, 4a, and 6a) exhibited the most potent inhibitory activity compared to that of the reference drug (Zileuton), with IC50 values less than I mu M. Molecular modeling studies for compounds 1a, 3a, 4a, and 6a were also presented. The excellent in vitro activities of this class of compounds may possess potential for the treatment of LT-related diseases. (C) 2007 Published by Elsevier Ltd. |
| WOS关键词 | CYCLOOXYGENASE-2 COX-2 ; DOCKING ; DRUGS ; LEUKOTRIENES ; INSIGHTS ; TARGET ; CANCER ; 5-LOX |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000246087900004 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273265]  |
| 专题 | 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 药物发现与设计中心 |
| 通讯作者 | Liu, Hong |
| 作者单位 | 1.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, State Key Lab Drug Res,Drug Discovery & Design Ct, Shanghai 201203, Peoples R China 3.Zhejiang Univ, Sch Med, Zhejiang Resp Drugs Res Lab, State Drugs Adm China, Hangzhou 310031, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zheng, Mingfang,Zheng, Mingyue,Ye, Deju,et al. Indole derivatives as potent inhibitors of 5-lipoxygenase: Design, synthesis, biological evaluation, and molecular modeling[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2007,17(9):2414-2420. |
| APA | Zheng, Mingfang.,Zheng, Mingyue.,Ye, Deju.,Deng, Yangmei.,Qiu, Shuifeng.,...&Jiang, Hualiang.(2007).Indole derivatives as potent inhibitors of 5-lipoxygenase: Design, synthesis, biological evaluation, and molecular modeling.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,17(9),2414-2420. |
| MLA | Zheng, Mingfang,et al."Indole derivatives as potent inhibitors of 5-lipoxygenase: Design, synthesis, biological evaluation, and molecular modeling".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 17.9(2007):2414-2420. |
入库方式： OAI收割
来源：上海药物研究所
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