基本信息
周宇  男  博导  中国科学院上海药物研究所
电子邮件: zhouyu@simm.ac.cn
通信地址: 上海市浦东新区祖冲之路555号
邮政编码: 201203

招生信息

   
招生专业
100701-药物化学
招生方向
药物化学

教育背景

2003-09--2008-07   沈阳药科大学   博士
1999-09--2003-07   沈阳药科大学   学士学位

工作经历

   
工作简历
2023-07~2024-07,上海市浦东新区卫生健康委员会(卫健委), 副主任(挂职)
2020-01~现在, 国科大杭州高等研究院, 双聘教授、硕士生导师
2019-10~现在, 中国科学院上海药物研究所, 研究员、课题组长、博士生导师
2016-10~2019-09,中国科学院上海药物研究所, 研究员、博导(2018)
2010-09~2016-09,中国科学院上海药物研究所, 副研究员、硕导(2012)
2008-09~2010-08,中国科学院上海药物研究所, 博士后
2003-09~2008-07,沈阳药科大学, 博士
1999-09~2003-07,沈阳药科大学, 学士学位
社会兼职
2025-01-01-2026-12-31,《Chinese Chemical Letters》(中国化学快报)青年编委会委员, 青年编委
2023-12-30-2025-12-30,《中国药物化学杂志 》(Chinese Journal of Medicinal Chemistry)首届青年编委, 青年编委

教授课程

药物化学

专利与奖励

   
奖励信息
(1) 上海市东方英才计划拔尖项目(原上海市优秀学术带头人), 省级, 2024
(2) 国科大杭州高等研究院"教学奉献奖", 院级, 2024
(3) 第七届全国药学专业学位优秀教学案例奖, 部委级, 2024
(4) 上海市浦东新区“明珠计划”人才项目, 市地级, 2023
(5) 中国药学会科学技术奖, 一等奖, 专项, 2021
(6) 上海市科技进步奖, 一等奖, 省级, 2020
(7) 2019年度上海药学科技奖, 一等奖, 省级, 2020
(8) 上海药学科技奖, 一等奖, 省级, 2015
专利成果
( 1 ) 一类新型阿尔茨海默病检测探针及其生物应用, 2024, 第 3 作者, 专利号: CN114957296B

( 2 ) 一类多取代的四氢异喹啉化合物及制备方法、药物组合物和用途, 2024, 第 3 作者, 专利号: CN117510512A

( 3 ) 一类酰胺化合物及其制备方法、药物组合物和用途, 2024, 第 1 作者, 专利号: CN117402156A

( 4 ) 一类α,β-不饱和酰胺类化合物及其制备方法、药物组合物和用途, 2024, 第 3 作者, 专利号: CN117402123A

( 5 ) 一类并环吡唑啉酮甲酰胺类化合物及其制备方法、药物组合物和用途, 2023, 第 3 作者, 专利号: CN112236430B

( 6 ) 一类含氟异噁唑类化合物及其制备方法、药物组合物和用途, 2023, 第 3 作者, 专利号: CN110452235B

( 7 ) 一类新型阿尔茨海默病检测探针及其生物应用, 2022, 第 3 作者, 专利号: CN114957296A

( 8 ) 醛基类化合物及其制法和用途, 2022, 第 7 作者, 专利号: CN106928206B

( 9 ) 一种乙酰胆碱酯酶抑制剂的晶型及其制备方法和应用, 2021, 第 2 作者, 专利号: CN112939846A

( 10 ) 一类并环吡唑啉酮甲酰胺类化合物及其制备方法、药物组合物和用途, 2021, 第 3 作者, 专利号: CN112236430A

( 11 ) 一类并环吡唑啉酮甲酰胺类化合物及其制备方法、药物组合物和用途, 2019, 第 3 作者, 专利号: CN110511218A

( 12 ) 一类含氟异噁唑类化合物及其制备方法、药物组合物和用途, 2019, 第 3 作者, 专利号: CN110452235A

( 13 ) 五元杂环类化合物及其制备方法、药物组合物和用途, 2019, 第 5 作者, 专利号: CN109476650A

( 14 ) 五元杂环类化合物及其制备方法、药物组合物和用途, 2019, 第 5 作者, 专利号: CN109476649A

( 15 ) 5‑芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途, 2018, 第 2 作者, 专利号: CN107531633A

( 16 ) 一类含氟三氮唑并吡啶类化合物及其制备方法、药物组合物和用途, 2017, 第 2 作者, 专利号: CN107383002A

( 17 ) 醛基类化合物及其制法和用途, 2017, 第 7 作者, 专利号: CN106928206A

( 18 ) 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途, 2016, 第 2 作者, 专利号: CN106146391A

( 19 ) 一种1-(3-氨基丙基)取代环状胺类化合物、其制备方法、药物组合物及用途, 2016, 第 14 作者, 专利号: CN105873924A

( 20 ) 一种1-(3-氨基丙基)取代环状胺类化合物、其制备方法、药物组合物及用途, 2015, 第 14 作者, 专利号: CN104744451A

( 21 ) 一类二氢吲哚类化合物、其制备方法、药物组合物及应用, 2015, 第 8 作者, 专利号: CN104326963A

( 22 ) 一类吲哚类化合物、其制备方法、药物组合物及应用, 2014, 第 8 作者, 专利号: CN104211631A

( 23 ) 一种六氢二苯并a,g喹嗪类化合物的药物用途, 2014, 第 8 作者, 专利号: CN104127414A

( 24 ) 一类氟取代的环状胺类化合物及其制备方法、药物组合物和用途, 2014, 第 3 作者, 专利号: CN103787954A

( 25 ) 新型青蒿素衍生物及其制法和应用, 2014, 第 7 作者, 专利号: CN103570738A

( 26 ) 新型唾液酸衍生物及其制备方法,包含该衍生物的药物组合物,以及其用途, 2012, 第 8 作者, 专利号: CN102532080A

( 27 ) 环庚烷并吡啶类化合物、其制备方法、用途及包含此类化合物的药物组合物, 2011, 第 6 作者, 专利号: CN101284828B

( 28 ) 一类5-脂氧酶抑制剂及其制备方法、药物组合物和应用, 2010, 第 3 作者, 专利号: CN101684098A

( 29 ) 新颖的吡唑类5-脂氧酶小分子抑制剂及其制备方法、药物组合物和应用, 2009, 第 3 作者, 专利号: CN101544631A

( 30 ) 四氢喹啉类化合物、其制备方法及药物组合物, 2008, 第 8 作者, 专利号: CN101245062A

( 31 ) 阻止阿尔茨海默氏症Aβ多肽纤维化的小分子抑制剂及其制备方法、药物组合物和应用, 2008, 第 4 作者, 专利号: CN101100416A

( 32 ) N,N'-二取代哌嗪类衍生物及其制备方法、药物组合物和用途, 2007, 第 7 作者, 专利号: CN101007794A

( 33 ) 取代1,3,5三嗪类化合物及其制备方法和应用, 2007, 第 9 作者, 专利号: CN1970552A

出版信息

   
发表论文
(1) Discovery and characterization of novel potent non-covalent small molecule inhibitors targeting papain-like protease from SARS-CoV-2, Discovery and characterization of novel potent non-covalent small molecule inhibitors targeting papain-like protease from SARS-CoV-2, ACTA PHARMACEUTICA SINICA B, 2024, 第 19 作者  通讯作者
(2) Discovery and Optimization of Tetrahydroisoquinoline Derivatives To Enhance Lysosome Biogenesis as Preclinical Candidates for the Treatment of Alzheimer's Disease, JOURNAL OF MEDICINAL CHEMISTRY, 2024, 第 12 作者  通讯作者
(3) Discovery of Novel Nonpeptidic and Noncovalent Small Molecule 3CL pro Inhibitors as anti-SARS-CoV-2 Drug Candidate, JOURNAL OF MEDICINAL CHEMISTRY, 2024, 第 17 作者  通讯作者
(4) Characterization and noncovalent inhibition of the K63-deubiquitinase activity of SARS-cov-2 PLpro, Antiviral Research, 2024, 
(5) Electrochemical oxidative cyclization of N -allylamides for the synthesis of CF 3 -containing benzoxazines and oxazolines ���, RSC ADVANCES, 2024, 第 5 作者
(6) Discovery and Optimization of Novel Nonbile Acid FXR Agonists as Preclinical Candidates for the Treatment of Inflammatory Bowel Disease, JOURNAL OF MEDICINAL CHEMISTRY, 2024, 第 19 作者  通讯作者
(7) Rh(III)-Catalyzed C-H Activation/Annulation for the Construction of Quinolizinones and Indolizines, ORGANIC LETTERS, 2024, 第 9 作者  通讯作者
(8) Identification and biological evaluation of fused tetrahydroisoquinoline derivatives as Wnt/��-catenin signaling inhibitors to suppress colorectal cancer, Eur. J. Med. Chem., 2024, 
(9) Substrate��� and Catalyst���Controlled C���H Bond Activation/Annulation for Construction of Pyrido[2,3,4���de]quinazolinones and Indolo[1,2���c]quinazolinones., Adv. Synth. Catal., 2024, 第 8 作者  通讯作者
(10) A Ru(ii)-catalyzed C���H activation and annulation cascade for the construction of highly coumarin-fused benzo[a]quinolizin-4-ones and pyridin-2-ones, Organic Chemistry Frontiers, 2023, 第 9 作者  通讯作者
(11) Discovery of novel non-peptidic and non-covalent small-molecule 3CLpro inhibitors as potential candidate for COVID-19 treatment, Signal Transduction and Targeted Therapy, 2023, 第 10 作者  通讯作者
(12) Copper-Catalyzed Synthesis of alpha-Keto Amides from Sulfoxonium Ylides, The Journal of Organic Chemistry, 2023, 第 5 作者  通讯作者
(13) Rh(III)-Catalyzed Successive C-H Activations of 2-Phenyl-3H-indoles and Cyclization Cascades to Construct Highly Fused Indole Heteropolycycles, Organic Letters, 2023, 第 6 作者  通讯作者
(14) Synthesis of maleimide-braced peptide macrocycles and their potential anti-SARS-CoV-2 mechanisms, CHEMICAL COMMUNICATIONS, 2023, 第 10 作者
(15) LYECs: lysosome-enhancing compounds as potential therapeutic approaches for Alzheimer disease, AUTOPHAGY, 2023, 第 2 作者  通讯作者
(16) Smart Nanosensitizers for Activatable Sono-Photodynamic Immunotherapy of Tumors by Redox-Controlled Disassembly, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2023, 第 12 作者
(17) Structure-based drug discovery of novel fusedpyrazolone carboxamide derivatives as potent and selective AXL inhibitors, Structure-based drug discovery of novel fused-pyrazolone carboxamide derivatives as potent and selective AXL inhibitors, ACTA PHARMACEUTICA SINICA B, 2023, 第 17 作者  通讯作者
(18) The synthesis of spirocyclopropane skeletons enabled by Rh(III)-catalyzed enantioselective C���H activation/4+ 2 annulation, CHEM CATALYSIS, 2023, 第 14 作者  通讯作者
(19) Inhibition of the dopamine transporter promotes lysosome biogenesis and ameliorates Alzheimer's disease-like symptoms in mice, ALZHEIMERS & DEMENTIA, 2022, 第 10 作者  通讯作者
(20) A Facile Electrochemical Strategy for the Azidation of Benzylic C(sp(3))-H Bonds, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, 2022, 第 8 作者  通讯作者
(21) Recyclable rhodium-catalyzed C-H activation/4+2 annulation with unconventional regioselectivity at ambient temperature: experimental development and mechanistic insight, GREEN CHEMISTRY, 2022, 第 6 作者  通讯作者
(22) A substrate-controlled Ru(ii)-catalyzed C-H activation/5+2 annulation cascade and unusual acyl migration to synthesize diverse indoline scaffolds, ORGANIC CHEMISTRY FRONTIERS, 2022, 第 10 作者  通讯作者
(23) Rh(III)-Catalyzed C-H Activation and 4+1+1 Sequential Cyclization Cascade to Give Highly Fused Indano1,2-bazirines, ORGANIC LETTERS, 2022, 第 9 作者  通讯作者
(24) LYECs: lysosome-enhancing compounds as potential therapeutic approaches for Alzheimer disease, AUTOPHAGY, 2022, 第 2 作者  通讯作者
(25) Engineering of donor-acceptor-donor curcumin analogues as near-infrared fluorescent probes for in vivo imaging of amyloid-�� species, THERANOSTICS, 2022, 第 6 作者
(26) Discovery of Novel Pyrrolo2,3-dpyrimidine-based Derivatives as Potent JAK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors, JOURNAL OF MEDICINAL CHEMISTRY, 2022, 第 10 作者
(27) A metal-free method for the facile synthesis of indanones via the intramotecular hydroacylation of 2-vinytbenzaldehyde, GREEN CHEMISTRY, 2021, 第 6 作者  通讯作者
(28) A Rh(iii)-catalyzed C-H activation/regiospecific annulation cascade of benzoic acids with propargyl acetates to unusual 3-alkylidene-isochromanones, ORGANIC CHEMISTRY FRONTIERS, 2021, 第 7 作者  通讯作者
(29) Catalytic System-Controlled Divergent Reaction Strategies for the Construction of Diversified Spiropyrazolone Skeletons from Pyrazolidinones and Diazopyrazolones, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2021, 第 7 作者  通讯作者
(30) I-2-induced cascade cyclization and dearomatization of indoles for the highly efficient synthesis of iodinated and vinylic spiroindolenines, GREEN CHEMISTRY, 2021, 第 6 作者  通讯作者
(31) Rhodium-Catalyzed C-H Activation/Annulation Cascade of Aryl Oximes and Propargyl Alcohols to Isoquinoline N-Oxides, ADVANCED SYNTHESIS & CATALYSIS, 2021, 第 7 作者  通讯作者
(32) Rh(III)-Catalyzed 5+1 Annulation of Indole-enaminones with Diazo Compounds To Form Highly Functionalized Carbazoles, ORGANIC LETTERS, 2021, 第 5 作者  通讯作者
(33) Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate, JOURNAL OF MEDICINAL CHEMISTRY, 2021, 第 1 作者
(34) Structural optimization and biological evaluation for novel artemisinin derivatives against liver and ovarian cancers, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021, 第 1 作者
(35) A metal-free method for the facile synthesis of indanones via the intramolecular hydroacylation of 2-vinylbenzaldehyde, Green Chemistry, 2021, 第 6 作者  通讯作者
(36) Rh(III)-Catalyzed Dual C-H Functionalization/Cyclization Cascade by a Removable Directing Group: A Method for Synthesis of Polycyclic Fused PyranodeIsochromenes, JOURNAL OF ORGANIC CHEMISTRY, 2020, 第 7 作者  通讯作者
(37) Rhodium(III)-Catalyzed Redox-Neutral 3+3 Annulation of N -nitrosoanilines with Cyclopropenones: A Traceless Approach to Quinolin-4(1 H )-One Scaffolds, MOLECULES, 2020, 第 6 作者  通讯作者
(38) Ruthenium-Catalyzed C-H Activations for the Synthesis of Indole Derivatives, CATALYSTS, 2020, 第 3 作者
(39) A removable directing group-assisted Rh(iii)-catalyzed direct C-H bond activation/annulation cascade to synthesize highly fused isoquinolines, ORGANIC CHEMISTRY FRONTIERS, 2020, 第 4 作者  通讯作者
(40) Structures of Gi-bound metabotropic glutamate receptors mGlu2 and mGlu4, NATURE, 2020, 第 14 作者
(41) Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis, JOURNAL OF MEDICINAL CHEMISTRY, 2020, 第 14 作者  通讯作者
(42) Synthesis of Highly Fused Pyrano2,3-bpyridines via Rh(III)- Catalyzed C-H Activation and Intramolecular Cascade Annulation under Room Temperature, JOURNAL OF ORGANIC CHEMISTRY, 2020, 第 6 作者  通讯作者
(43) Ruthenium(ii)-catalyzed selective C-H bond activation of imidamides and coupling with sulfoxonium ylides: an efficient approach for the synthesis of highly functional 3-ketoindoles, ORGANIC CHEMISTRY FRONTIERS, 2019, 第 7 作者  通讯作者
(44) Rh(III)-Catalyzed C-H Bond Activation for the Construction of Heterocycles with sp(3)-Carbon Centers, CATALYSTS, 2019, 第 4 作者  通讯作者
(45) Highly selective C-H bond activation of N-arylbenzimidamide and divergent couplings with diazophosphonate compounds: a catalyst-controlled selective synthetic strategy for 3-phosphorylindoles and 4-phosphorylisoquinolines, ORGANIC CHEMISTRY FRONTIERS, 2019, 第 6 作者  通讯作者
(46) Gold-catalyzed Rapid Construction of Nitrogen-containing Heterocyclic Compound Library with Scaffold Diversity and Molecular Complexity, ADVANCED SYNTHESIS & CATALYSIS, 2019, 第 6 作者
(47) N-Heterocyclic Carbene Catalyzed Enantioselective 3+2 Dearomatizing Annulation of Saturated Carboxylic Esters with N-Iminoisoquinolinium Ylides, JOURNAL OF ORGANIC CHEMISTRY, 2018, 第 2 作者
(48) Rhodium(III)-Catalyzed C-H Activation of alpha-Iminonitriles or alpha-Imino Esters and Cyclization with Acrylates to 2H-Isoindoles, JOURNAL OF ORGANIC CHEMISTRY, 2018, 第 6 作者  通讯作者
(49) Rhodium(III)-Catalyzed C-H Activation of Benzoylacetonitriles and Cyclization with Sulfoxonium Ylides to Naphthols, ADVANCED SYNTHESIS & CATALYSIS, 2018, 第 6 作者  通讯作者
(50) Rh(III)-Catalyzed C-H Activation of Benzoylacetonitriles and Tandem Cyclization with Diazo Compounds to Substituted Benzodechromenes, ORGANIC LETTERS, 2018, 第 5 作者  通讯作者
(51) A Method for Synthesis of 3-Hydroxy-1-indanones via Cu-Catalyzed Intramolecular Annulation Reactions, JOURNAL OF ORGANIC CHEMISTRY, 2018, 第 6 作者
(52) Rhodium(III)-Catalyzed C-H Activation of alpha-Iminonitriles or alpha-Imino Esters and Cyclization with Acrylates to 2H-Isoindoles, JOURNAL OF ORGANIC CHEMISTRY, 2018, 第 6 作者  通讯作者
(53) Rh(III)���Catalyzed C���H Activation of Benzoylacetonitriles and Cyclization with Sulfoxonium Ylides to Naphthols., Advanced Synthesis & Catalysis, 2018, 第 1 作者  通讯作者
(54) Direct Synthesis of 3-Acylindoles through Rhodium(III)-Catalyzed Annulation of N-Phenylamidines with alpha-Cl Ketones, ORGANIC LETTERS, 2018, 第 7 作者  通讯作者
(55) Crystal structure of the human 5-HT1B serotonin receptor bound to an inverse agonist, CELL DISCOVERY, 2018, 第 13 作者
(56) Catalytic and catalyst-free diboration of alkynes, ORGANIC CHEMISTRY FRONTIERS, 2017, 第 5 作者
(57) 氮杂环卡宾催化有机反应的研究进展, Progress of Organic Reactions Catalyzed by N-Heterocyclic Carbenes, CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2017, 第 3 作者  通讯作者
(58) Propargyl Alcohols as One-Carbon Synthons: Redox-Neutral Rhodium(III)-Catalyzed C-H Bond Activation for the Synthesis of Isoindolinones Bearing a Quaternary Carbon, ORGANIC LETTERS, 2017, 第 3 作者
(59) Ruthenium-Catalyzed Redox-Neutral 4+1 Annulation of Benzamides and Propargyl Alcohols via C-H Bond Activation, ACS CATALYSIS, 2017, 第 4 作者  通讯作者
(60) Absolute Configuration of Periplosides C and F and Isolation of Minor Spiro-orthoester Group-Containing Pregnane-type Steroidal Glycosides from Periploca sepium and Their T-Lymphocyte Proliferation Inhibitory Activities, JOURNAL OF NATURAL PRODUCTS, 2017, 第 4 作者
(61) Construction of highly enantioenriched spirocyclopentaneoxindoles containing four consecutive stereocenters via thiourea-catalyzed asymmetric Michael���Henry cascade reactions, BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY, 2017, 第 5 作者  通讯作者
(62) 氮杂环卡宾催化有机反应的研究进展, Progress of Organic Reactions Catalyzed by N-Heterocyclic Carbenes, CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2017, 第 3 作者  通讯作者
(63) Recent Advances in the Synthesis of Heterocycles via Gold-catalyzed Cascade Reactions: A Review, CURRENT ORGANIC CHEMISTRY, 2017, 第 2 作者
(64) Rh(iii)-catalyzed c-h cyclization of arylnitrones with diazo compounds: access to 3-carboxylate substituted n-hydroxyindoles, JOURNAL OF ORGANIC CHEMISTRY, 2017, 第 4 作者  通讯作者
(65) Structural optimization and biological evaluation of 1,5-disubstituted pyrazole-3-carboxamines as potent inhibitors of human 5-lipoxygenase, ACTA PHARMACEUTICA SINICA B, 2016, 第 1 作者
(66) Enantioselective Assembly of Spirolactones through NHC-Catalyzed Remote gamma-Carbon Addition of Enals with Isatins, ACS COMBINATORIAL SCIENCE, 2016, 第 5 作者  通讯作者
(67) Enantioselective N-Heterocyclic Carbene-Catalyzed 3+3 Annulation of ,-Unsaturated Esters with Methyl Ketoimine, ADVANCED SYNTHESIS & CATALYSIS, 2016, 第 5 作者  通讯作者
(68) Enantioselective Assembly of Spirolactones through NHC-Catalyzed Remote ��-Carbon Activation of ��-Methyl Enals with Isatins., ACS Combinatorial Science, 2016, 第 1 作者  通讯作者
(69) Identification and biochemical characterization of DC07090 as a novel potent small molecule inhibitor against human enterovirus 71 3C protease by structure-based virtual screening, EUROPEANJOURNALOFMEDICINALCHEMISTRY, 2016, 第 12 作者  通讯作者
(70) Preclinical Efficacy and Safety Assessment of Artemisinin-Chemotherapeutic Agent Conjugates for Ovarian Cancer, EBIOMEDICINE, 2016, 第 2 作者
(71) Structural optimization and biological evaluation of l,5-disubstituted pyrazole-3-carboxamines as potent inhibitors of human 5-lipoxygenase, ACTA PHARMACEUTICA SINICA B, 2016, 第 1 作者
(72) Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II-III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas, CHEMICAL REVIEWS, 2016, 第 1 作者
(73) Synthesis and Anti-HIV-1 Activity Evaluation for Novel 3a,6a-Dihydro-1 H -pyrrolo3,4- c pyrazole-4,6-dione Derivatives, MOLECULES, 2016, 第 3 作者
(74) Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selective alpha(1A)-Adrenoceptor Antagonists, JOURNAL OF MEDICINAL CHEMISTRY, 2016, 第 4 作者
(75) Design, Synthesis, and Biological Evaluation of Indoline and Indole Derivatives as Potent and Selective alpha(1A)-Adrenoceptor Antagonists, JOURNAL OF MEDICINAL CHEMISTRY, 2016, 第 7 作者
(76) N-Heterocyclic Carbene Catalytic 4+2 Cyclization of 3-Alkylenyloxindoles with Enals: gamma-Carbon Activation for Enantioselective Assembly of Spirocarbocyclic Oxindoles, JOURNAL OF ORGANIC CHEMISTRY, 2016, 第 2 作者
(77) Palladium-catalyzed picolinamide-directed coupling of C(sp(2))-H and C(sp(2))-H: a straightforward approach to quinolinone and pyridone scaffolds, CHEMICAL COMMUNICATIONS, 2015, 第 4 作者
(78) Fluorescent Coumarin-Artemisinin Conjugates as Mitochondria-Targeting Theranostic Probes for Enhanced Anticancer Activities, CHEMISTRY-A EUROPEAN JOURNAL, 2015, 第 5 作者
(79) ��-Carbon Activation Through N-Heterocyclic Carbene/Br��nsted Acids Cooperative Catalysis: A Highly Enantioselective Route to ��-Lactams., Organic Letters., 2015, 
(80) Total synthesis of periploside A, a unique pregnane hexasaccharide with potent immunosuppressive effects, NATURE COMMUNICATIONS, 2015, 第 2 作者
(81) Direct access to pyrido/pyrrolo2,1-bquinazolin-9(1H)-ones through silver-mediated intramolecular alkyne hydroamination reactions, BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY, 2015, 第 7 作者  通讯作者
(82) gamma-Carbon Activation through N-Heterocyclic Carbene/Bronsted Acids Cooperative Catalysis: A Highly Enantioselective Route to delta-Lactams, ORGANIC LETTERS, 2015, 第 6 作者  通讯作者
(83) 通过串联反应不对称合成氧化吲哚螺环化合物的研究进展, Asymmetric Synthesis of Spirooxindoles via Organocascade Strategies, CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2015, 第 2 作者
(84) JNJ-40411813合成工艺研究, Improved synthetic process of JNJ-40411813, 中国药物化学杂志, 2015, 第 5 作者
(85) Inhibition of human copper trafficking by a small molecule significantly attenuates cancer cell proliferation., NATURE CHEMISTRY, 2015, 
(86) Discovery and Optimization of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Pharmacophore- and Docking-Based Virtual Screening., JOURNAL OF MEDICINAL CHEMISTRY, 2015, 第 13 作者
(87) A Mannich/Cyclization Cascade Process for the Asymmetric Synthesis of Spirocyclic Thioimida-zolidinexoindoles., Chemical Communications, 2014, 第 1 作者
(88) 先导化合物结构优化策略三通过化学修饰改善水溶性, 药学学报, 2014, 第 3 作者
(89) One-pot metal-free synthesis of highly substituted pyrroles from 2-acetyl-3-methylene-1,4-dicarbonyl compounds and primary amines via TBHP and activated carbon oxidative aromatization of dihydropyrrole, RSC ADVANCES, 2014, 第 2 作者
(90) 先导化合物结构优化策略四改善化合物的血脑屏障通透性, 药学学报, 2014, 第 2 作者
(91) A Mannich/cyclization cascade process for the asymmetric synthesis of spirocyclic thioimidazolidineoxindoles, CHEMICAL COMMUNICATIONS, 2014, 第 2 作者
(92) Asymmetric Michael Addition of N-tert-ButanesulfinylImidates: an Efficient Strategy for the Synthesis of (R)-3-Substituted Indanone Derivatives, Organic Letters, 2013, 第 1 作者  通讯作者
(93) Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D1, D2 and serotonin 5-HT1A multi-action profile, BIOORGANIC & MEDICINAL CHEMISTRY, 2013, 第 9 作者
(94) 高效合成技术在药物研发中的应用, 药学学报, 2013, 第 1 作者
(95) Asymmetric Michael Addition of N-tert-Butanesulfinyl lmidate with alpha,beta-Unsaturated Diesters: Scope and Application to the Synthesis of Indanone Derivatives, ORGANIC LETTERS, 2013, 第 2 作者  通讯作者
(96) Au(I)/Ag(I)-Catalyzed Cascade Approach for the Synthesis of Benzo4,5imidazo1,2-cpyrrolo1,2-aquinazolinones, JOURNAL OF ORGANIC CHEMISTRY, 2013, 第 2 作者  通讯作者
(97) Gold-catalyzed Michael addition/intramolecular annulation cascade: an effective pathway for the chemoselective- and regioselective synthesis of tetracyclic indole derivatives in water, GREEN CHEMISTRY, 2013, 第 2 作者
(98) Gold(I)-Catalyzed Cascade Approach for the Synthesis of Tryptamine-Based Polycyclic Privileged Scaffolds as alpha(1)-Adrenergic Receptor Antagonists, JOURNAL OF ORGANIC CHEMISTRY, 2013, 第 5 作者
(99) ���One-pot��� Synthesis of Dihydrobenzo4,51,3oxazino2,3- a isoquinolines via a Silver(I)-Catalyzed Cascade Approach, MOLECULES, 2013, 第 2 作者  通讯作者
(100) Mycophenolic acid derivative 118 improves outcome of skin grafts by suppressing IL-17 production, ACTA PHARMACOLOGICA SINICA, 2013, 第 10 作者
(101) Synthesis of polysubstituted beta-amino cyclohexane carboxylic acids via Diels-Alder reaction using Ni(II)-complex stabilized beta-alanine derived dienes, AMINO ACIDS, 2013, 第 7 作者
(102) Corrigendum to "Structural revision of periplocosides and periperoxides, natural immunosuppressive agents from the genus Periploca" Phytochemistry 72/17 (2011) 2230���2236, PHYTOCHEMISTRY, 2013, 第 3 作者
(103) Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2012, 第 4 作者
(104) An expedient Pd/DBU mediated cyanation of aryl/heteroaryl bromides with K-4Fe(CN)(6), CHEMICAL COMMUNICATIONS, 2012, 第 4 作者
(105) Gold-catalyzed tandem reaction in water: an efficient and convenient synthesis of fused polycyclic indoles, GREEN CHEMISTRY, 2012, 第 2 作者
(106) Highly Enantioselective Michael Addition of 2-Oxindole-3-carboxylate Esters to Nitroolefins Promoted by Cinchona Alkaloid-Thiourea-Bronsted Acid Cocatalysts, ADVANCED SYNTHESIS & CATALYSIS, 2012, 第 5 作者
(107) SM934 Treated Lupus-Prone NZBxNZW F-1 Mice by Enhancing Macrophage Interleukin-10 Production and Suppressing Pathogenic T Cell Development, PLOS ONE, 2012, 第 8 作者
(108) Design, synthesis, and pharmacological evaluation of novel tetrahydroprotoberberine derivatives: Selective inhibitors of dopamine D1 receptor, BIOORGANIC & MEDICINAL CHEMISTRY, 2012, 第 9 作者
(109) Recent advances in the gold-catalyzed additions to C���C multiple bonds, BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY, 2011, 第 2 作者
(110) Recent Advances in Silver-Mediated Organic Synthesis Reactions, PROGRESS IN CHEMISTRY, 2011, 第 2 作者
(111) Synthesis of Pyrrolo[1,2-a]quinoxalines via Gold (?)-Mediated Cascade Reactions., ACS Combinatorial Science, 2011, 第 1 作者
(112) Silver- and Gold-Mediated Domino Transformation: A Strategy for Synthesizing Benzo[e]indolo[1,2-a]pyrrolo/pyrido[2,1-c][1,4] diazepine-3,9-dione., Journal of Organic Chemistry, 2011, 第 1 作者
(113) Structural revision of periplocosides and periperoxides, natural immunosuppressive agents from the genus Periploca, PHYTOCHEMISTRY, 2011, 第 3 作者
(114) An Effective Synthetic Entry to Fused Benzimidazoles via Iodocyclization, ADVANCED SYNTHESIS & CATALYSIS, 2011, 第 2 作者
(115) Synthesis of Pyrrolo1,2-aquinoxalines via Gold(I)-Mediated Cascade Reactions, ACS COMBINATORIAL SCIENCE, 2011, 第 2 作者
(116) 银催化有机合成反应的研究进展, Recent Advances in Silver-Mediated Organic Synthesis Reactions, 化学进展, 2011, 第 2 作者
(117) Silver-catalyzed intramolecular hydroamination of alkynes in aqueous media: efficient and regioselective synthesis for fused benzimidazoles, GREEN CHEMISTRY, 2011, 第 2 作者
(118) Synthesis of 2-Phenylnaphthalenes through Gold-Catalyzed Dimerization via a Highly Selective Carbon Nucleophile Pathway, JOURNAL OF ORGANIC CHEMISTRY, 2011, 第 4 作者
(119) Silver- and Gold-Mediated Domino Transformation: A Strategy for Synthesizing Benzoeindolo1,2-apyrrolo/pyrido2,1-c1,4-diazepine-3,9-diones, JOURNAL OF ORGANIC CHEMISTRY, 2011, 第 1 作者
(120) Gold(I)-Catalyzed One-Pot Tandem Coupling/Cyclization: An Efficient Synthesis of Pyrrolo-/Pyrido2,1-bbenzod1,3oxazin-1-ones, ADVANCED SYNTHESIS & CATALYSIS, 2010, 第 1 作者
(121) Gold(I)-Catalyzed One-Pot Tandem Coupling/Cyclization: An Efficient Synthesis of Pyrrolo-/Pyrido[2,1-b]benzo [d][1,3]oxazin-1-one., Advanced Synthesis Catalysis, 2010, 第 1 作者
(122) Gold(I)-Catalyzed Cascade for Synthesis of Pyrrolo1,2-a:2 ',1 '-c-/Pyrido2,1-cpyrrolo1,2-aquinoxalinones, ADVANCED SYNTHESIS & CATALYSIS, 2010, 第 1 作者
(123) Structural Optimization and Biological Evaluation of Substituted Bisphenol A Derivatives as β-Amyloid Peptide Aggregation Inhibitors, JOURNAL OF MEDICINAL CHEMISTRY, 2010, 第 1 作者
(124) Silver- and Gold-Mediated Intramolecular Cyclization to Substituted Tetracyclic Isoquinolizinium Hexafluorostilbates, JOURNAL OF ORGANIC CHEMISTRY, 2010, 第 4 作者
(125) HIV整合酶抑制剂的研究进展, Research Progress in HIV Integrase Inhibitors, CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2010, 第 3 作者
(126) HIV整合酶抑制剂的研究进展, Research Progress in HIV Integrase Inhibitors, CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2010, 第 3 作者
(127) Metal-Free Synthesis of 2-Substituted (N, O, C) Benzothiazoles via an Intramolecular C-S Bond Formation, JOURNAL OF COMBINATORIAL CHEMISTRY, 2010, 第 3 作者
(128) Regioselective Synthesis of 3-Benzazepinones and Unexpected 5-Bromo-3-benzazepinones, JOURNAL OF ORGANIC CHEMISTRY, 2010, 第 3 作者
(129) Gold(I)-Catalyzed Tandem Transformation: A Simple Approach for the Synthesis of Pyrrolo/Pyrido2,1-a1,3benzoxazinones and Pyrrolo/Pyrido2,1-aquinazolinones, JOURNAL OF ORGANIC CHEMISTRY, 2010, 第 2 作者
(130) Ligand-free iron/copper cocatalyzed N-arylations of aryl halides with amines under microwave irradiation, GREEN CHEMISTRY, 2010, 第 3 作者
(131) An Effective Synthetic Entry to Fused Benzimidazoles via Iodocyclization., Advanced Synthesis Catalysis, 2010, 第 1 作者
(132) Metal-free tandem reaction in water: An efficient and regioselective synthesis of 3-hydroxyisoindolin-1-ones, GREEN CHEMISTRY, 2010, 第 1 作者  通讯作者
(133) Structural Optimization and Biological Evaluation of Substituted Bisphenol A Derivatives as ��-Amyloid Peptide Aggregation Inhibitors., Journal of Medicinal Chemistry, 2010, 第 1 作者
(134) First Reaction of a Chiral Gly-Ni(���) Complex in Water, CHINESE JOURNAL OF CHEMISTRY, 2010, 第 2 作者
(135) First Reaction of a Chiral Gly-Ni(II) Complex in Water, CHINESE JOURNAL OF CHEMISTRY, 2010, 第 2 作者
(136) Gold-Catalyzed One-Pot Cascade Construction of Highly Functionalized Pyrrolo1,2-aquinolin-1(2H)-ones, JOURNAL OF ORGANIC CHEMISTRY, 2009, 第 1 作者
(137) raltegravir的合成工艺研究, 中国药科大学学报, 2009, 第 4 作者
(138) Current Strategies for the Discovery of K+ Channel Modulators, CURRENT TOPICS IN MEDICINAL CHEMISTRY, 2009, 第 4 作者
(139) Silver-Catalyzed Intramolecular Cyclization of o-(1-Alkynyl)benzamides: Efficient Synthesis of (1H)-Isochromen-1-imines, ADVANCED SYNTHESIS & CATALYSIS, 2009, 第 2 作者
(140) Gold- and Silver-Catalyzed Intramolecular Hydroamination of Terminal Alkynes: Water-Triggered Chemo- and Regioselective Synthesis of Fused Tricyclic Xanthines, ADVANCED SYNTHESIS & CATALYSIS, 2009, 第 3 作者
(141) SM934, a water-soluble derivative of arteminisin, exerts immunosuppressive functions in vitro and in vivo, INTERNATIONAL IMMUNOPHARMACOLOGY, 2009, 第 6 作者
(142) Gold-catalyzed intramolecular hydroamination of terminal alkynes in aqueous media: efficient and regioselective synthesis of indole-1-carboxamides, GREEN CHEMISTRY, 2009, 第 4 作者
(143) Copper(I)-Catalyzed One-Pot Synthesis of 2H-1,4-Benzoxazin-3-(4H)-ones from o-Halophenols and 2-Chloroacetamides, JOURNAL OF ORGANIC CHEMISTRY, 2009, 第 3 作者
(144) Anti-inflammatory effects of Z23 on LPS-induced inflammatory responses in RAW264.7 macrophages, JOURNAL OF ETHNOPHARMACOLOGY, 2008, 第 7 作者
(145) 扎那米韦的合成工艺研究, Improved synthesis of zanamivir, 中国药物化学杂志, 2008, 第 1 作者
(146) Simultaneous 2-O-deacetylation and 4-amination of peracetylated Neu5Ac: application to the synthesis of (4���4)-piperazine derivatives linked sialic acid dimers, TETRAHEDRON, 2008, 第 4 作者
(147) Synthesis of (S)-, (R)-, and (rac)-2-amino-3,3-bis(4-fluorophenyl)propanoic acids and an evaluation of the DPP IV inhibitory activity of Denagliptin diastereomers, TETRAHEDRON, 2008, 第 5 作者
(148) An unusual de-nitro reduction of 2-substituted-4-nitroquinolines, TETRAHEDRON LETTERS, 2006, 第 1 作者
(149) Discovery and Optimization of Novel Nonbile Acid FXR Agonists as Preclinical Candidates for the Treatment of Inflammatory Bowel Disease, JOURNAL OF MEDICINAL CHEMISTRY, 第 19 作者
发表著作
( 1 ) 高等药物化学, 化学工业出版社, 2011-01, 第 1 作者
( 2 ) 新药研发的案例研究, 化学工业出版, 2013-03, 第 1 作者
( 3 ) 个性化药物——新药研发的未来, 上海科学技术文献出版社, 2020-05, 第 2 作者
( 4 ) 创新药物研发经纬, 化学工业出版社, 2020-10, 第 2 作者

科研活动

   
科研项目
( 1 ) 靶向溶酶体氢离子通道TMEM175的化合物设计、合成及抗帕金森先导化合物发现研究, 负责人, 国家任务, 2024-01--2027-12
( 2 ) 靶向脑血流的全新机制抗AD候选药物发现研究, 负责人, 研究所自主部署, 2023-10--2025-09
( 3 ) 靶向 DAT-CDK9- TFEB 全新机制的抗 AD 候选化合物发现研究, 参与, 研究所自主部署, 2023-01--2025-06
( 4 ) 靶向TFEB介导溶酶体生成的化合物设计、合成及抗AD先导化合物发现研究, 负责人, 国家任务, 2022-01--2025-12
( 5 ) 靶向AXL/c-Met双重抑制剂的设计、合成及药理活性研究, 负责人, 国家任务, 2020-01--2023-12
参与会议
(1)新型抗 AD 药物发现及分子调控机制研究   中国药物化学学术会议暨中欧药物化学研讨会   2023-10-07
(2)The Discovery of Next Generation AChE Inhibitors:FromHighlyEfficient Synthesis Strategy to Clinical Candidate(OP-64)   中国药物化学学术会议暨中欧药物化学研讨会   2021-09-27