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学科主题: 药学
题名:
Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors
作者: Wang, Jie1; Tan, Hailiang1; Sun, Qi1; Ge, Zemei1; Wang, Xin1; Wang, Yinye2; Li, Runtao1
关键词: PARP-1 inhibitor ; Pyridazino[3,4,5-de]quinazolin-3(2H)-one ; Combination strategy ; Neuroprotectivity ; Molecular docking
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2015-06-01
DOI: 10.1016/j.bmcl.2015.04.013
卷: 25, 期:11, 页:2340-2344
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: POLY(ADP-RIBOSE) POLYMERASE-1 INHIBITOR ; DNA-REPAIR ; IN-VITRO ; DERIVATIVES ; SYNTHETASE ; DISEASE
英文摘要:

A series of pyridazino[3,4,5-de]quinazolin-3(2H)-one derivatives were designed and synthesized as PARP-1 inhibitors. Most of the synthesized compounds showed good inhibitory activities of PARP-1 and four of them achieved at the IC50 values ranging from 0.0914 mu M to 0.244 mu M. Two compounds, 1a and 1b, were further tested for their neuroprotective effect in the PC12 cell model injured by H2O2 and both of them exhibited excellent activities. (C) 2015 Elsevier Ltd. All rights reserved.

语种: 英语
所属项目编号: 81172915
项目资助者: National Natural Science Foundation of China
WOS记录号: WOS:000354115400015
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56543
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Dept Mol & Cellular Pharmacol, Beijing 100191, Peoples R China

Recommended Citation:
Wang, Jie,Tan, Hailiang,Sun, Qi,et al. Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2015,25(11):2340-2344.
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