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Cardioprotective mechanism of SGLT2 inhibitor against myocardial infarction is through reduction of autosis被引量:35收藏 分享
作者:Kai Jiang Yue Xu Dandan Wang Feng Chen Zizhuo Tu Jie Qian Sheng Xu Yixiang Xu John Hwa Jian Li Hongcai Shang Yaozu Xiang
机构:Shanghai East Hospital;State Key Laboratory of Bioreactor Engineering;Section of Cardiovascular Medicine;Key Laboratory of Chinese Internal Medicine of Ministry of Education and Beijing
来源:蛋白质与细胞(英文版)  2022
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Repurposing antimycotic ciclopirox olamine as a promising anti-ischemic stroke agent被引量:8收藏 分享
作者:Hongxuan Feng Linghao Hu Hongwen Zhu Lingxue Tao Lei Wu Qinyuan Zhao Yemi Gao Qi Gong Fei Mao Xiaokang Li Hu Zhou Jian Li Haiyan Zhang
机构:CAS Key Laboratory of Receptor Research;State Key Laboratory of Bioreactor Engineering;Shanghai Key Laboratory of New Drug Design;University of Chinese Academy of Sciences
来源:药学学报(英文版)  2020
关键词:Blood-brain barrier  Brain ischemia  Cell cycle  Inflammation  Neuroprotection  
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Anti-aging effects of chlorpropamide depend on mitochondrial complex-Ⅱ and the production of mitochondrial reactive oxygen species被引量:7收藏 分享
作者:Zhifan Mao Wenwen Liu Yunyuan Huang Tianyue Sun Keting Bao Jiali Feng Alexey Moskalev Zelan Hu Jian Li
机构:State Key Laboratory of Bioreactor Engineering;Laboratory of Geroprotective and Radioprotective Technologies;Yunnan Key Laboratory of Screening and Research on Anti-pathogenic Plant Resources from West Yunnan;Clinical Medicine Scientific and Technical Innovation Center
来源:药学学报(英文版)  2022
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Nitazoxanide,an anti-parasitic drug,efficiently ameliorates learning and memory impairments in AD model mice被引量:6收藏 分享
作者:Lei Fan Xiao-xia Qiu Zhi-yuan Zhu Jian-lu Lv Jian Lu Fei Mao Jin Zhu Jia-ying Wang Xiao-wei Guan Jing Chen Jin Ren Ji-ming Ye Yong-hua Zhao Jian Li Xu Shen
机构:Center for Drug Safety Evaluation and Research;University of Chinese Academy of Sciences;Shanghai Key Laboratory of New Drug Design;School of Medicine and Life Sciences;School of Health and Biomedical Sciences
来源:中国药理学报(英文版)  2019
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红花籽粕对小鼠的急性毒性及抗溃疡性结肠炎作用研究被引量:5收藏 分享
作者:戚曼 王文萱 付向磊 姜超 张亮 MD HASAN ALI 李剑 楚生辉 刘敏
机构:石河子大学药学院;华东理工大学药学院
来源:《中草药》  2024
关键词:红花籽粕  急性毒性  溃疡性结肠炎  炎症  肠道屏障  
摘要:目的评价红花籽粕(红花Carthamus tinctorius的种子经过压榨提取红花籽油后的副产品)对小鼠的急性毒性及抗溃疡性结肠炎(ulcerative colitis,UC)作用。方法C57BL/6小鼠ig不同剂量的...
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Cucurbitacin B-induced G2/M cell cycle arrest of conjunctival melanoma cells mediated by GRP78-FOXM1-KIF20A pathway被引量:5收藏 分享
作者:Jinlian Wei Xin Chen Yongyun Li Ruoxi Li Keting Bao Liang Liao Yuqing Xie Tiannuo Yang Jin Zhu Fei Mao Shuaishuai Ni Renbing Jia Xiaofang Xu Jian Li
机构:State Key Laboratory of Bioreactor Engineering;Department of Ophthalmology;Cancer Institute;Yunnan Key Laboratory of Screening and Research on Anti-pathogenic Plant Resources from West Yunnan;Clinical Medicine Scientific and Technical Innovation Center
来源:药学学报(英文版)  2022
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Structural repurposing of SGLT2 inhibitor empagliflozin for strengthening anti-heart failure activity with lower glycosuria被引量:3收藏 分享
作者:Yixiang Xu Chao Zhang Kai Jiang Xinchun Yang Feng Chen Zhiyang Cheng Jinlong Zhao Jiaxing Cheng Xiaokang Li Xin Chen Luoyifan Zhou Hao Duan Yunyuan Huang Yaozu Xiang Jian Li
机构:State Key Laboratory of Bioreactor Engineering;Shanghai East Hospital;East China University of Science and Technology-Tengbai Pharmaceutical Innovative Drugs Joint Research Institute;Hubei Key Laboratory of Genetic Regulation and Integrative Biology;Yunnan Key Laboratory of Screening and Research on Anti-pathogenic Plant Resources from West Yunnan
来源:药学学报(英文版)  2023
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Policresulen, a novel NS2B/NS3 protease inhibitor, effectively inhibits the replication of DENV2 virus in BHK-21 cells被引量:3收藏 分享
作者:Deng-wei WU Fei MAO Yan YE Jian LI Chuan-lian XU Xiao-min LUO Jing CHEN Xu SHEN
机构:College of Life Sciences;Shanghai Key Laboratory of New Drug Design;CAS Key Laboratory of Receptor Research
来源:中国药理学报(英文版)  2015
关键词:Dengue virus   antiviral drug   NS2B/NS3 protease   policresulen   molecular docking   molecular modeling  
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Discovery of synergistic activity of fluoroquinolones in combination with antimicrobial peptides against clinical polymyxin-resistant Pseudomonas aeruginosa DK2被引量:2收藏 分享
作者:Xinyu Zheng Qiao Cao Qin Cao Fei Mao Xiaokang Li Jin Zhu Lefu Lan Jian Li
机构:State Key Laboratory of Bioreactor Engineering;State Key Laboratory of Drug Research
来源:中国化学快报(英文版)  2020
关键词:Polymyxin B  Pseudomonas aeruginosa  Fluoroquinolones  Synergy  Cystic fibrosis  Antimicrobial peptides  
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Discovery of nitazoxanide-based derivatives as autophagy activators for the treatment of Alzheimer’s disease被引量:2收藏 分享
作者:Xiaokang Li Jian Lu Yixiang Xu Jiaying Wang Xiaoxia Qiu Lei Fan Baoli Li Wenwen Liu Fei Mao Jin Zhu Xu Shen Jian Li
机构:State Key Laboratory of Bioreactor Engineering;School of Medicine and Life Sciences;Center for Drug Safety Evaluation and Research
来源:药学学报(英文版)  2020
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Pro-senescence neddylation inhibitor combined with a senescence activated β-galactosidase prodrug to selectively target cancer cells被引量:2收藏 分享
作者:Shuaishuai Ni Qian Liu Xin Chen Lele Ding Lili Cai Fei Mao Donglei Shi Robert M.Hoffman Jian Li Lijun Jia
机构:Cancer Institute;State Key Laboratory of Bioreactor Engineering;Department of Surgery
来源:信号转导与靶向治疗(英文)  2022
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2-咪唑基-戊-1,4-二烯-3-酮类衍生物的合成及其抗菌活性研究被引量:1收藏 分享
作者:刘春丽 史册 刘锦燕 魏冰 毛斐 项明洁 李剑
机构:华东理工大学药学院;上海交通大学医学院附属瑞金医院检验科;上海交通大学医学院附属瑞金医院卢湾分院放免检验科
来源:《中国药物化学杂志》  2015
关键词:2-咪唑基-戊-1,4-二烯-3-酮  衍生物  抗菌活性  金黄色葡萄球菌  表皮葡萄球菌  
摘要:目的设计合成2-咪唑基-戊-1,4-二烯-3-酮类衍生物,并进行抗菌活性测试。方法以不同取代的苯甲醛为起始原料,经过Aldol缩合、溴代、亲核取代和Knoevenagel缩合四步反应合成目标化合物;采用微量稀释法测定化合...
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扎那米韦的合成工艺研究(英文)被引量:1收藏 分享
作者:周宇 李剑 李建 赵临襄 蒋华良 柳红
机构:中国科学院上海药物研究所药物发现与设计中心;沈阳药科大学制药工程学院;华东理工大学药学院
来源:《中国药物化学杂志》  2008
关键词:工艺研究  禽流感  扎那米韦  
摘要:目的研究治疗禽流感药物扎那米韦的合成工艺。方法以N-乙酰神经氨酸作为起始原料,经过酯化、酰化、成环、开环、叠氮化、还原、水解及AIMSA取代等8步反应制备扎那米韦。结果与结论经过对合成工艺的改进得到了目标产物,其结构经1...
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抗耐药铜绿假单胞菌DK2增敏剂的结构优化与活性评价被引量:1收藏 分享
作者:曾茹 陆淘淘 吴铃钰 张庆 石东磊 李剑 宋施豪 刘文文 李宝力
机构:海南大学药学院热带生物资源教育部重点实验室;华东理工大学药学院
来源:《沈阳药科大学学报》  2023
关键词:铜绿假单胞菌DK2  多粘菌素B  增敏剂  苯甲酰胺类  结构优化  
摘要:目的发现有效增敏多粘菌素B抗耐药铜绿假单胞菌DK2,并且具有良好安全性和水溶性的化合物。方法将本课题组前期所发现的先导化合物B4进行苯甲酰胺类化合物的设计与合成,并且通过微量肉汤稀释法测试目标化合物对铜绿假单胞菌DK2的...
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脾酪氨酸激酶抑制剂的研究进展被引量:1收藏 分享
作者:张玲玲 王义永 蒋华良 李剑
机构:华东理工大学药学院;浙江医药股份有限公司新昌制药厂
来源:《中国药物化学杂志》  2014
关键词:脾酪氨酸激酶  自身免疫疾病  类风湿性关节炎  Syk抑制剂  
摘要:非受体型蛋白激酶—脾酪氨酸激酶(Syk)在免疫细胞信号的转导过程中发挥着关键作用,可作为治疗各种过敏性疾病和免疫性疾病的新靶点。本文就近年来文献中报道的小分子Syk抑制剂的结构类型进行分类归纳,对这些抑制剂的构效关系及作...
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TRPA1 channel mediates organophosphate-induced delayed neuropathy被引量:1收藏 分享
作者:Qiang DING Sui FANG Xue-qin CHEN You-Xin WANG Jian LI Fu-yun TIAN Xiang XU Bernard ATTALI Xin XIE Zhao-bing GAO
机构:CAS Key Laboratory of Receptor Research;University of Chinese Academy of Sciences;Shanghai Leado Pharmatech Co. Ltd;Shanghai Key Laboratory of New Drug Design;Department of Physiology & Pharmacology
来源:Chinese Journal of Pharmacology and Toxicology  2017
关键词:organophosphate malathion TOCP organophosphate-induced delayed neuropathy Transient receptor potential cation channel member A1  
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Repurposing of antitumor drug candidate Quisinostat lead to novel spirocyclic antimalarial agents被引量:1收藏 分享
作者:Ruoxi Li Dazheng Ling Tongke Tang Zhenghui Huang Manjiong Wang Fei Mao Jin Zhu Lubin Jiang Jian Li Xiaokang Li
机构:State Key Laboratory of Bioreactor Engineering;Key Laboratory of Molecular Virology and Immunology;College of Pharmacy and Chemistry;Frontiers Science Center for Materiobiology and Dynamic Chemistry;School of Life Science and Technology
来源:中国化学快报(英文版)  2021
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Specific tracking of monoamine oxidase A in heart failure models by a far-red fluorescent probe with an ultra large Stokes shift被引量:1收藏 分享
作者:Xinming Li Donglei Shi Yihe Song Yixiang Xu Ying Gao Wenjing Qiu Xin Chen Xiaokang Li Yunyuan Huang Yanjun Feng Baoli Li Yuan Guo Jian Li
机构:State Key Laboratory of Bioreactor Engineering;Key Laboratory of Synthetic and Natural Functional Molecule of the Ministry of Education;Frontiers Science Center for Materiobiology and Dynamic Chemistry;College of Pharmacy and Chemistry;Clinical Medicine Scientific and Technical Innovation Center
来源:中国化学快报(英文版)  2022
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Discovery of potent 2,4-difluoro-linker poly(ADPribose) polymerase i inhibitors with enhanced water solubility and in vivo anticancer efficacy被引量:0收藏 分享
作者:Wen-hua CHEN Shan-shan SONG Ming-hui QI Xia-juan HUAN Ying-qing WANG Hualiang JIANG Jian DING Guo-bin REN Ze-hong MIAO Jian LI
机构:Shanghai Key Laboratory of New Drug Design;Division of Antitumor Pharmacology;Laboratory of Pharmaceutical Crystal Engineering & Technology;State Key Laboratory of Drug Research
来源:中国药理学报(英文版)  2017
关键词:PARP-1 inhibitor   olaparib   breast cancer   BRCA-deficient tumors  
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Selective targeting p53^(WT) lung cancer cells harboring homozygous p53 Arg72 by an inhibitor of CypA被引量:0收藏 分享
作者:Wei-qiang LU Qian HU Jian LI Jin HUANG
机构:Shanghai Key Laboratory of New Drug Design
来源:Chinese Journal of Pharmacology and Toxicology  2017
关键词:non-small cell lung cancer Cyclophilin A inhibitor p53-72R polymorphsm  
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上市药物与中止药物理化性质差异探讨被引量:0收藏 分享
作者:倪炜 郑新羽 王熳炯 毛斐 李剑
机构:华东理工大学药学院
来源:《中国药物化学杂志》  2018
关键词:类药性质  理化性质  成药性  中止药物  
摘要:目的探讨上市及中止药物关键理化性质的相同与差异规律,用于指导药物研发工作者在新药开发早期阶段设计更易于成药的化合物,减少新药研发失败率,推动新药研发进程。方法基于上市及中止药物数据库药物的化学结构,对比分析上市及中止药物...
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Novel dual inhibitors against FP-2 and PfDHFR as potential antimalarial agents: Design, synthesis and biological evaluation被引量:0收藏 分享
作者:Wenhua Chen Xue Yao Zhenghui Huang Fei Mao Longfei Guan Yun Tang Hualiang Jiang Jian Li Jin Huang Lubin Jiang Jin Zhu
机构:Shanghai Key Laboratory of New Drug Design;Key Laboratory of Molecular Virology & Immunology
来源:中国化学快报(英文版)  2019
关键词:Antimalarial drug  Plasmodium falciparum  FP-2  PfDHFR  Dual inhibitor  
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Trilogy of drug repurposing for developing cancer and chemotherapy-induced heart failure co-therapy agent被引量:0收藏 分享
作者:Xin Chen Xianggang Mu Lele Ding Xi Wang Fei Mao Jinlian Wei Qian Liu Yixiang Xu Shuaishuai Ni Lijun Jia Jian Li
机构:State Key Laboratory of Bioreactor Engineering;Cancer Institute;College of Pharmacy
来源:药学学报(英文版)  2024
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Discovery and synthesis of N^2,N^4-substitued-cycloalkyl[d]pyrimidine-2,4-diamine analogs: The first examples of small-molecular FGFR-1 activator被引量:0收藏 分享
作者:Bao-Li Li Fang Xiao Wen-Chao Lu Yu-Yun Sun Jin Zhu Jian Li
机构:Shanghai Key Laboratory of New Drug Design;Department of Pharmacy;China Resources Double-Crane Pharmaceutical Co.
来源:中国化学快报(英文版)  2014
关键词:Cycloalkyl[d]pyrimidine derivatives  FGFR-1  Activator  Chemical probe  
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用氧化烯胺催化的方法从饱和的醛来高效制备反式烯醛(英文)被引量:0收藏 分享
作者:张士磊 谢贺新 宋爱国 吴德燕 朱进 赵思涵 李剑 虞心红 王卫
机构:Department of Chemistry&Chemical Biology;华东理工大学药学院
来源:《中国科学:化学》  2012
关键词:醛  烯醛  烯胺  IBX  氧化烯胺催化  
摘要:本文报道一种温和、高效的胺催化,用IBX作为氧化剂,简单的醛为原料,高产率、高(E)-选择性的制备α,β-不饱和醛.该反应涉及到一种新型的催化氧化烯胺到α,β-不饱和亚胺离子的转换过程.
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特拉万星合成工艺研究被引量:0收藏 分享
作者:熊伦 管栋梁 李剑 黄蔚
机构:华东理工大学药学院;中国科学院上海药物研究所药物化学研究室;中国科学院大学
来源:《中国药科大学学报》  2017
关键词:万古霉素  特拉万星  合成工艺  
摘要:对特拉万星工艺路线进行了研究,以癸醇为原料,经甲磺酰化、乙醇胺亲核取代、Fmoc保护和Parikh-Doering氧化得到N-(9-芴基-9-甲氧羰基)癸基氨基乙醛(5)。盐酸万古霉素与5通过还原胺化反应、脱Fmoc保护...
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