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Novel 2-substituted nitronyl nitroxides as free radical scavengers: Synthesis, biological evaluation and structure-activity relationship
Wu, Yihui1; Bi, Lanrong1; Bi, Wei1; Li, Zeng1; Zhao, Ming1; Wang, Chao1; Ju, Jingfang1; Peng, Shiqi1
关键词Nitronyl Nitroxide Derivatives Free Radical Scavenger Structure-activity Relationship
刊名BIOORGANIC & MEDICINAL CHEMISTRY
2006-08-15
DOI10.1016/j.bmc.2006.04.016
14期:16页:5711-5720
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
关键词[WOS]OXIDATIVE STRESS ; NITRIC-OXIDE ; ANTIOXIDANTS ; DISEASE ; MOLECULE ; CANCER ; CELLS
英文摘要

To develop more potent small molecules with enhanced free radical scavenger properties, we designed and synthesized a series of nitronyl nitroxide derivatives 4a-h. A lead compound 4f was discovered based on Ach-induced vascorelaxation assay. Further chemical modification based on this scaffold provided a new series of 2-substituted phenylnitronyl nitroxide derivatives 6a-s. The newly synthesized compounds 6a-s possess improved radical scavenger′s activity based on PC12 cell survival assay. Compounds 6g,n,o, and s are some of the most potent compounds in terms of NO, H2O2, and OH scavenging ability. 2-Substitued phenylnitronyl nitroxides had a higher radical scavenging activity with the electron-donating group (EDG). In contrast, the introduction of electron-withdrawing group (EWG) to the aromatic ring led to a dramatic decrease in its radical scavenging activity. These results suggest that the electron-donating group (EDG) of the aromatic ring may be an important factor influencing the radical scavenging behavior of these compounds, and the potency of free radical scavenging activity largely depended on the position and electronic properties of the phenyl ring substituents. The enhanced radical scavenging capacities of the novel 2-substituted nitronyl nitroxides may be potential drug leads against the deleterious action of ROS (reactive oxygen species)/RNS (reactive nitrogen species). (c) 2006 Elsevier Ltd. All rights reserved.

语种英语
WOS记录号WOS:000239472700032
引用统计
被引频次:30[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/52928
专题北京大学药学院
作者单位1.Univ S Alabama, Mitchell Canc Inst, Mobile, AL 36688 USA
2.Capital Univ Med Sci, Coll Pharmaceut Sci, Beijing 100054, Peoples R China
3.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
4.Hebei Med Univ, Affiliated Hosp 2, Dept Surg, Shijiazhuang 050000, Peoples R China
推荐引用方式
GB/T 7714
Wu, Yihui,Bi, Lanrong,Bi, Wei,et al. Novel 2-substituted nitronyl nitroxides as free radical scavengers: Synthesis, biological evaluation and structure-activity relationship[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2006,14(16):5711-5720.
APA Wu, Yihui.,Bi, Lanrong.,Bi, Wei.,Li, Zeng.,Zhao, Ming.,...&Peng, Shiqi.(2006).Novel 2-substituted nitronyl nitroxides as free radical scavengers: Synthesis, biological evaluation and structure-activity relationship.BIOORGANIC & MEDICINAL CHEMISTRY,14(16),5711-5720.
MLA Wu, Yihui,et al."Novel 2-substituted nitronyl nitroxides as free radical scavengers: Synthesis, biological evaluation and structure-activity relationship".BIOORGANIC & MEDICINAL CHEMISTRY 14.16(2006):5711-5720.
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