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Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors
Wang, Jie1; Tan, Hailiang1; Sun, Qi1; Ge, Zemei1; Wang, Xin1; Wang, Yinye2; Li, Runtao1
关键词Parp-1 Inhibitor Combination Strategy Pyridazino[3 Neuroprotectivity 4 Molecular Docking 5-de]Quinazolin-3(2h)-one
刊名BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
2015-06-01
DOI10.1016/j.bmcl.2015.04.013
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
WOS记录号WOS:000354115400015
项目编号81172915
资助机构National Natural Science Foundation of China
引用统计
被引频次:4[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/400002259/56543
专题北京大学药学院
北京大学药学院_化学生物学系
北京大学药学院_分子与细胞药理学系
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
推荐引用方式
GB/T 7714
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.
APA Wang, Jie.,Tan, Hailiang.,Sun, Qi.,Ge, Zemei.,Wang, Xin.,...&Li, Runtao.(2015).Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,25(11),2340-2344.
MLA Wang, Jie,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".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 25.11(2015):2340-2344.
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