具有抗心肌纤维化作用的ATX抑制剂的发现、优化与作用机制探索研究

81872751
2018
H3401.合成药物化学
翟鑫
面上项目
教授
沈阳药科大学
57万元
药物设计合成;心肌纤维化;ATX抑制剂;分子机制;生物活性评价
2019-01-01到2022-12-31
  • 中英文摘要
  • 结题摘要
  • 结题报告
  • 项目成果
  • 项目参与人
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序号 标题 类型 作者
1 A Novel Synthetic Strategy of First-in-Class ATX Inhibitor Ziritaxestat (GLPG-1690) 会议论文 Hongrui Lei;Fang Jia;Yu Yang;Changtao Li;Ming Guo;Xin Zhai
2 首届全国药学专业学位研究生教育教学成果奖二等奖 奖励 翟鑫;严中平;李岩;杨建军;顾丽娜
3 Structure guided design of imidazo[1,2-a] pyridine analogues bearing carbamate moiety as potent ATX inhibitors for treatment of fibrotic diseases 会议论文 Hongrui Lei;Fang Jia;Ming Guo;Xin Zhai
4 Optimization and evaluation of novel tetrahydropyrido[4,3-d] pyrimidine derivatives as ATX inhibitors for cardiac and hepatic fibrosis 期刊论文 Nan Jiang;Yuhong Zhou;Minglin Zhu;Junlong Zhang;Meng Cao;Hongrui Lei;Ming Guo;Ping Gong;Guangyue Su;Xin Zhai
5 An updated patent review of autotaxin inhibitors (2017–present) 期刊论文 Zehui Tan;Hongrui Lei;Ming Guo;Yuxiang Chen;Xin Zhai
6 辽宁省首届优秀研究生导师团队 奖励 翟鑫
7 Discovery of novel tetrahydropyrido[4,3- d ]pyrimidine analogs as potent autotaxin regulators with impressive tumor suppression effects 期刊论文 Huinan Wu;Hongrui Lei;Zehui Tan;Deyi Ma;Tong Li;Fuyi Wang;Mengrao Guo;Nan Jiang;Xin Zhai
8 四氢吡啶并[4,3-d]嘧啶类衍生物及其用途 专利 翟鑫;周宇宏;宫平;荆同飞;类红瑞;郭明;荆同飞
9 辽宁省研究生教学成果一等奖:行业特色高校研究生教育“一体两翼,四轮驱动”现代化治理模式的创新与实践 奖励 程卯生;翟鑫;武晓娜;严中平;杨建军;顾丽娜
10 《地方行业特色高校研究生教育治理现代化改革与实践》在2021年第二届“双一流”建设与评价学术研讨会上评为优秀论文奖 奖励 翟鑫;严中平;武晓娜
11 Investigation of novel ATX inhibitor metabolites by UHPLC-orbitrap-MS/MS and molecular docking studies 期刊论文 Hongjin Wang;Yuxiang Chen;Xinjie Qi;Hao Zhang;Xin Zhai;Lixin Sun
12 Catalyst-Free Cyclization- and Curtius Rearrangement-Induced Functional Group Transformation: An Improved Synthetic Strategy of First-in-Class ATX Inhibitor Ziritaxestat (GLPG-1690) 期刊论文 Hongrui Lei;Yu Yang;Changtao Li;Fang Jia;Nan Jiang;Ping Gong;Xin Zhai
13 Novel imidazo[1,2-a]pyridine derivatives as potent ATX allosteric inhibitors: Design, synthesis and promising in vivo anti-fibrotic efficacy in mice lung model 期刊论文 Hongrui Lei;Zhen Li;Tong Li;Huinan Wu;Jing Yang;Xinlian Yang;Yu Yang;Nan Jiang;Xin Zhai
14 辽宁省“兴辽英才计划”科技创新领军人才 奖励 翟鑫
15 辽宁省学位与研究生教育“先进个人” 奖励 翟鑫
16 2019创新药物成药性评价高层学术论坛优秀论文三等奖 奖励 翟鑫
17 2021年辽宁省优秀博士学位论文指导教师 奖励 翟鑫
18 Structure guided design of indole derivatives as potent ATX inhibitors for treatment of fibrotic diseases 会议论文 Lei Hongrui;Cui Youbao;Li Tong;Zhai Xin
19 辽宁省研究生教学成果二等奖:深化产教融合培养体系建设,培养新药研发高端应用型人才 奖励 赵临襄;翟鑫;刘丹;赵燕芳;张达盼;关奇;黄敏;许佑君
20 Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects 期刊论文 Hongrui Lei;Changtao Li;Yu Yang;Fang Jia;Ming Guo;Minglin Zhu;Nan Jiang;Xin Zhai
21 Structural and PK-guided identification of indole-based non-acidic autotaxin (ATX) inhibitors exhibiting high invivo anti-fibrosis efficacy in rodent model 期刊论文 Hongrui Lei;Zhi Cao;Huinan Wu;Tong Li;Xinyu Wang;Yuxiang Chen;Enlong Ma;Lixin Sun;Xin Zhai
22 Hybrid imidazo[1,2‐ a ]pyridine analogs as potent ATX inhibitors with concrete in vivo antifibrosis effect 期刊论文 Tong Li;Hongrui Lei;Juanjuan Yang;Zhi Cao;Yu Yang;Zimeng Liu;Ruonan Sun;Xinlian Yang;Xin Zhai
23 辽宁省首届优秀研究生导师 奖励 翟鑫
24 Discovery of Novel Indole-Based Allosteric Highly Potent ATX Inhibitors with Great In Vivo Efficacy in a Mouse Lung Fibrosis Model 期刊论文 Hongrui Lei;Ming Guo;Xiaopeng Li;Fang Jia;Changtao Li;Yu Yang;Meng Cao;Nan Jiang;Enlong Ma;Xin Zhai
25 Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors 期刊论文 Hongrui Lei;Xinyu Wang;Guolong Zhao;Tong Li;Youbao Cui;Huinan Wu;Jing Yang;Nan Jiang;Xin Zhai
26 Structure-based linker exploration: Discovery of 1-ethyl-1H-indole analogs as novel ATX inhibitors 期刊论文 Fang Jia;Hongrui Lei;Yuxiang Chen;Tong Li;Lingyun Xing;Zhi Cao;Xin Zhai
27 Design, synthesis and anti-fibrosis evaluation of imidazo[1,2–a]pyridine derivatives as potent ATX inhibitors 期刊论文 Yuxiang Chen;Hongrui Lei;Tong Li;Youbao Cui;Xinyu Wang;Zhi Cao;Huinan Wu;Xin Zhai
28 咪唑并[1,2-a]吡啶衍生物及其制备方法和应用 专利 翟鑫;类红瑞;马恩龙;郭明;贾芳
29 沈阳市优秀研究生导师 奖励 翟鑫
30 第四届全国药学专业学位优秀教学案例:连续流微反应技术:“冰箱式”迷你制药工厂的诞生 奖励 翟鑫
31 一种ATX抑制剂Ziritaxestat的合成方法 专利 翟鑫;类红瑞;姜楠;贾芳;杨宇;李长涛
32 基于吲哚母核的ATX抑制剂及其制备方法和应用 专利 翟鑫;类红瑞;马恩龙;姜楠;贾芳;郭明
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