基本信息
艾菁  女  博导  中国科学院上海药物研究所
email: jai@simm.ac.cn
address: 上海浦东新区祖冲之路555号2413室
postalCode: 201203

招生信息

   
招生专业
100706-药理学
招生方向
肿瘤药理学,肿瘤生物学

教育背景

2006-09--2009-06   中国海洋大学   博士
2003-09--2006-06   中国海洋大学   硕士
1999-09--2003-06   中国海洋大学   学士

工作经历

   
工作简历
2015-10~现在, 中国科学院上海药物研究所, 研究员
2011-10~2015-09,中科院上海药物研究所, 副研究员
2009-07~2011-09,中科院上海药物研究所, 助理研究员
2006-09~2009-06,中国海洋大学, 博士
2003-09~2006-06,中国海洋大学, 硕士
1999-09~2003-06,中国海洋大学, 学士
社会兼职
2022-10-01-今,JCO 中文版肿瘤标志物专刊 编委,
2021-11-01-今,中国老年学和老年医学学会肿瘤基础及转化研究专家委员会委员,
2021-09-01-今,中国临床肿瘤学会(CSCO)肿瘤标志物专家委员会委员,
2020-11-01-今,中国药理学会肿瘤药理专业委员会委员、中国抗癌协会抗癌药物专业委员会委员,

专利与奖励

   
奖励信息
(1) 第二十四届中国专利银奖(一类五元杂环并吡啶类化合物及其制备方法和用途), 二等奖, 国家级, 2023
(2) 上海职工优秀创新成果奖, 二等奖, 其他, 2019
(3) 上海市药学科技奖, 一等奖, 市地级, 2017
(4) 赛诺菲-上海生科院优秀青年人才奖, , 院级, 2014
(5) 上海药物研究所“优秀青年科技工作者”, 研究所(学校), 2014
(6) 中国药理学会Servier青年药理工作者奖, , 其他, 2012
专利成果
( 1 ) 一种CSF-1R激酶抑制剂的用途, 2021, 第 3 作者, 专利号: CN113318110A

( 2 ) 具有Axl与c-Met激酶抑制活性的化合物及其制备和应用, 2021, 第 5 作者, 专利号: CN112457295A

( 3 ) 喹啉或喹唑啉类化合物及其应用, 2021, 第 6 作者, 专利号: CN112351971A

( 4 ) 3-氨基吡唑类化合物及其应用, 2021, 第 6 作者, 专利号: CN112313213A

( 5 ) 稠环嘧啶氨基化合物、其制备方法、药物组合物及应用, 2021, 第 6 作者, 专利号: CN112239459A

( 6 ) 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 6 作者, 专利号: CN112236430A

( 7 ) 具有BET抑制活性的化合物及其制备方法和用途, 2020, 第 10 作者, 专利号: CN111683932A

( 8 ) 癌症患者根据脾酪氨酸激酶进行分层, 2020, 第 3 作者, 专利号: CN111521810A

( 9 ) 2,4-二胺基嘧啶化合物、其制备方法、药物组合物及用途, 2020, 第 4 作者, 专利号: CN107586278B

( 10 ) 含邻氨基杂芳环炔基的化合物及其制备方法和用途, 2019, 第 6 作者, 专利号: CN110582483A

( 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 6 作者, 专利号: CN110511218A

( 12 ) 一类芳基二氟苄基醚类化合物、制备方法及用途, 2019, 第 4 作者, 专利号: CN110240587A

( 13 ) 一种具有AXL抑制活性的化合物及其制备和应用, 2019, 第 5 作者, 专利号: CN110036014A

( 14 ) 五元杂环并3,4-d哒嗪酮类化合物、其制备方法、药物组合物及其应用, 2019, 第 5 作者, 专利号: CN109641908A

( 15 ) 一类多取代的吡嗪/三嗪酰胺类化合物及其制备方法和应用, 2019, 第 4 作者, 专利号: CN109384774A

( 16 ) 一种具有FGFR抑制活性的新型化合物及其制备和应用, 2019, 第 4 作者, 专利号: CN109328187A

( 17 ) 一种具有FGFR抑制活性的新型化合物及其制备和应用, 2019, 第 4 作者, 专利号: CN109328187A

( 18 ) 氘代SGX523及其用途, 2018, 第 4 作者, 专利号: CN108864101A

( 19 ) 多肽类化合物及其在制备组织蛋白酶D抑制剂中的用途, 2018, 第 4 作者, 专利号: CN108727234A

( 20 ) 一类取代的氨基六元氮杂环类化合物及其制备和用途, 2018, 第 4 作者, 专利号: CN108699030A

( 21 ) 五元杂环并吡嗪化合物、制备方法、中间体、组合和应用, 2018, 第 5 作者, 专利号: CN108570052A

( 22 ) 五元并六元杂环化合物、制备方法、中间体、组合和应用, 2018, 第 5 作者, 专利号: CN108570053A

( 23 ) 取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用, 2018, 第 6 作者, 专利号: CN108473434A

( 24 ) 含邻氨基杂芳环炔基的化合物及其制备方法和用途, 2018, 第 6 作者, 专利号: CN108456163A

( 25 ) 一种具有Axl抑制活性的化合物及其制备和应用, 2018, 第 5 作者, 专利号: CN108250200A

( 26 ) 一种吡啶并氮杂环化合物及其制备方法和用途, 2018, 第 4 作者, 专利号: CN107709320A

( 27 ) 一类含苯酚片段的2,4‑二胺基嘧啶化合物、其制备方法、药物组合物及用途, 2018, 第 4 作者, 专利号: CN107586278A

( 28 ) 五元杂环并3,4‑d哒嗪酮类化合物、其制备方法、药物组合物及其应用, 2017, 第 5 作者, 专利号: CN107417687A

( 29 ) 一类多取代喹诺酮类化合物及其制备方法和用途, 2017, 第 4 作者, 专利号: CN107151240A

( 30 ) 一类取代的氨基吡啶类化合物及其制备和用途, 2017, 第 4 作者, 专利号: CN107098884A

( 31 ) 取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用, 2017, 第 6 作者, 专利号: CN106467541A

( 32 ) 吲唑类化合物的制备方法和用途, 2017, 第 5 作者, 专利号: CN106317023A

( 33 ) 氘代的3-(6-喹啉基)二氟甲基-6-(1-甲基)-4-吡唑基1,2,4三唑并4,3-b哒嗪及其应用, 2017, 第 4 作者, 专利号: CN106279176A

( 34 ) 一种新型激酶抑制剂的制备及其应用, 2017, 第 6 作者, 专利号: CN106279119A

( 35 ) 一种吡啶并氮杂环化合物及其制备方法和用途, 2017, 第 4 作者, 专利号: CN106279147A

( 36 ) 吡唑并3,4-b吡啶类和吲唑类化合物的制备方法和用途, 2016, 第 5 作者, 专利号: CN106146493A

( 37 ) 喹啉酮类化合物及其制备方法和用途, 2016, 第 4 作者, 专利号: CN106146464A

( 38 ) 吲唑类化合物及其制备方法和用途, 2016, 第 6 作者, 专利号: CN106032359A

( 39 ) 一类杂环取代的吲哚并萘酮衍生物、其制备方法、药物组合物及其用途, 2016, 第 4 作者, 专利号: CN105566307A

( 40 ) 作为FGFR激酶抑制剂的吲唑类化合物及其制备和应用, 2016, 第 6 作者, 专利号: CN105524048A

( 41 ) 一种硫酸酯化聚古洛糖酸多糖或其可药用盐及其制备方法和用途, 2016, 第 2 作者, 专利号: CN105358582A

( 42 ) 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途, 2016, 第 7 作者, 专利号: CN105218548A

( 43 ) 一类3-氨基-苯并五元杂环化合物及其制备方法和用途, 2015, 第 4 作者, 专利号: CN105175351A

( 44 ) 一类双香豆素类化合物及其制备方法和用途, 2015, 第 4 作者, 专利号: CN104910118A

( 45 ) ALK激酶抑制剂, 2015, 第 5 作者, 专利号: CN104854101A

( 46 ) 一种硫酸酯化聚古洛糖酸多糖或其可药用盐及其制备方法和用途, 2015, 第 2 作者, 专利号: CN104277130A

( 47 ) 一类五元杂环并吡啶类化合物及其制备方法和用途, 2014, 第 5 作者, 专利号: CN104230922A

( 48 ) 2,4-二氨基嘧啶类化合物及其医药用途, 2014, 第 4 作者, 专利号: CN104230954A

( 49 ) 一类炔基杂环类化合物及其应用, 2014, 第 5 作者, 专利号: CN104211639A

( 50 ) 杂环取代的吲哚并萘酮衍生物、其制备方法、药物组合物及其用途, 2014, 第 4 作者, 专利号: CN104211687A

( 51 ) 杂环基取代的吲哚并萘酮衍生物及其医药用途, 2014, 第 5 作者, 专利号: CN104177342A

( 52 ) 酰胺基取代的吲哚并萘酮衍生物及其医药用途, 2014, 第 5 作者, 专利号: CN104177332A

( 53 ) 三取代咪唑并二氮杂萘酮化合物及其制备方法和用途, 2014, 第 5 作者, 专利号: CN103709162A

( 54 ) 哒嗪酮类化合物、其制备方法、药物组合物及其用途, 2014, 第 5 作者, 专利号: CN103664895A

( 55 ) 苯氮卓类化合物及其制备方法和用途, 2014, 第 5 作者, 专利号: CN103664903A

( 56 ) 新型咪唑并1,2-a吡啶类化合物、其制备方法、包含此类化合物的药物组合物及其用途, 2013, 第 4 作者, 专利号: CN103214481A

( 57 ) 吡啶类化合物、其制备方法、包含该化合物的药物组合物及其用途, 2013, 第 4 作者, 专利号: CN102850328A

( 58 ) pIgR作为肿瘤早期复发和/或转移的分子标志物和抗肿瘤转移的药物干预靶点的用途, 2012, 第 3 作者, 专利号: CN102841200A

( 59 ) 一类吡啶并五元杂环衍生物及其制备方法和用途, 2012, 第 5 作者, 专利号: CN102827186A

( 60 ) 一类哒嗪酮类化合物,其药物组合物、制备方法及用途, 2012, 第 4 作者, 专利号: CN102731409A

( 61 ) 新型胺基吡啶类化合物、其制备方法、包含此类化合物的药物组合物及其用途, 2012, 第 5 作者, 专利号: CN102718745A

( 62 ) 三氟甲基取代的喹啉或喹喔啉类化合物、其制备方法、包含该化合物的药物组合物及其用途, 2012, 第 3 作者, 专利号: CN102690269A

( 63 ) 一类双香豆素类化合物及其制备方法和用途, 2012, 第 4 作者, 专利号: CN102558049A

( 64 ) 1,2,4三唑并4,3-b1,2,4三嗪类化合物、其制备方法和用途, 2012, 第 4 作者, 专利号: CN102532141A

( 65 ) 一类五元杂环并嘧啶类化合物及其制备方法和用途, 2012, 第 4 作者, 专利号: CN102464667A

( 66 ) 喹啉类化合物、其制备方法、包含该化合物的药物组合物及该化合物的用途, 2011, 第 4 作者, 专利号: CN101993416A

出版信息

   
发表论文
(1) Structural Optimization of Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors, JOURNAL OF MEDICINAL CHEMISTRY, 2023, 通讯作者
(2) SYK-mediated epithelial cell state is associated with response to c-Met inhibitors in c-Met-overexpressing lung cancer, Signal Transduction and Targeted Therapy, 2023, 通讯作者
(3) Discovery of 10H-Benzobpyrido2,3-e1,4oxazine AXL Inhibitors via Structure-Based Drug Design Targeting c-Met Kinase, JOURNAL OF MEDICINAL CHEMISTRY, 2022, 通讯作者
(4) Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors, JOURNAL OF MEDICINAL CHEMISTRY, 2022, 通讯作者
(5) F-18-FDG PET as an imaging biomarker for the response to FGFR-targeted therapy of cancer cells via FGFR-initiated mTOR/HK2 axis, THERANOSTICS, 2022, 通讯作者
(6) Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor, JOURNAL OF MEDICINAL CHEMISTRY, 2021, 通讯作者
(7) Design, Synthesis, and Pharmacological Evaluation of Biaryl-Containing PD-1/PD-L1 Interaction Inhibitors Bearing a Unique Difluoromethyleneoxy Linkage, JOURNAL OF MEDICINAL CHEMISTRY, 2021, 通讯作者
(8) Design, synthesis and biological evaluation of pyrazolo3,4-dpyridazinone derivatives as covalent FGFR inhibitors, Design, synthesis and biological evaluation of pyrazolo3,4-dpyridazinone derivatives as covalent FGFR inhibitors, ACTA PHARMACEUTICA SINICA B, 2021, 通讯作者
(9) The Novel RET Inhibitor SYHA1815 Inhibits RET-Driven Cancers and Overcomes Gatekeeper Mutations by Inducing G1 Cell-Cycle Arrest through c-Myc Downregulation, MOLECULAR CANCER THERAPEUTICS, 2021, 通讯作者
(10) Discovery of pyrrolo2,3-dpyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021, 通讯作者
(11) Preclinical evaluation of 3D185, a novel potent inhibitor of FGFR1/2/3 and CSF-1R, in FGFR-dependent and macrophage-dominant cancer models., CANCER IMMUNOLOGY RESEARCH, 2020, 第 13 作者
(12) Discovery and Development of a Series of Pyrazolo3,4-dpyridazinone Compounds as the Novel Covalent Fibroblast Growth Factor Receptor Inhibitors by the Rational Drug Design, JOURNAL OF MEDICINAL CHEMISTRY, 2019, 通讯作者
(13) The Secretome Engages STAT3 to Favor a Cytokine-rich Microenvironment in Mediating Acquired Resistance to FGFR Inhibitors, MOLECULAR CANCER THERAPEUTICS, 2019, 通讯作者
(14) Discovery of a series of dimethoxybenzene FGFR inhibitors with 5H-pyrrolo2,3-bpyrazine scaffold: structure-activity relationship, crystal structural characterization and and in vivo study, ACTA PHARMACEUTICA SINICA B, 2019, 通讯作者
(15) Preclinical evaluation of 3D185, a novel potent inhibitor of FGFR1, JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH, 2019, 第 16 作者
(16) Discovery of a potent tyrosine kinase AXL inhibitor bearing the 3-((2,3,4,5-tetrahydro-1H-benzo d azepin-7-yl)amino)pyrazine core, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2019, 通讯作者
(17) Farnesoid X Receptor Constructs an Immunosuppressive Microenvironment and Sensitizes (FXRPD)-P-high-L1(low) NSCLC to Anti-PD-1 Immunotherapy, CANCER IMMUNOLOGY RESEARCH, 2019, 通讯作者
(18) Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2019, 通讯作者
(19) Preclinical evaluation of 3D185, a novel potent inhibitor of FGFR1/2/3 and CSF-1R, in FGFR-dependent and macrophage-dominant cancer models, JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH, 2019, 通讯作者
(20) Evaluation of Deuterium-Labeled JNJ38877605: Pharmacokinetic, Metabolic, and in Vivo Antitumor Profiles, CHEMICAL RESEARCH IN TOXICOLOGY, 2018, 通讯作者
(21) Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors (vol 61, pg 9085, 2018), JOURNAL OF MEDICINAL CHEMISTRY, 2018, 第 7 作者
(22) somcl085anovelmultitargetedfgfrinhibitordisplayspotentanticanceractivityinfgfraddictedhumancancermodels, ACTA PHARMACOLOGICA SINICA, 2018, 通讯作者
(23) Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 通讯作者
(24) Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 第 8 作者
(25) Structure-Based Discovery of a Series of 5H-Pyrrolo2,3-bpyrazine FGFR Kinase Inhibitors, MOLECULES, 2018, 通讯作者
(26) Structure-Based Discovery of a Series of 5H-Pyrrolo2,3-bpyrazine FGFR Kinase Inhibitors, MOLECULES, 2018, 通讯作者
(27) Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models, MOLECULAR CANCER THERAPEUTICS, 2018, 通讯作者
(28) Discovery and Biological Evaluation of a Series of Pyrrolo2,3- b pyrazines as Novel FGFR Inhibitors, MOLECULES : A JOURNAL OF SYNTHETIC CHEMISTRY AND NATURAL PRODUCT CHEMISTRY, 2017, 第 8 作者
(29) Evaluation of in vitro and in vivo activity of a multityrosine kinase inhibitor, AL3810, against human thyroid cancer., ACTA PHARMACOLOGICA SINICA, 2017, 第 3 作者
(30) Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer, JOURNAL OF MEDICINAL CHEMISTRY, 2017, 通讯作者
(31) Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2017, 通讯作者
(32) Evaluation of in vitro and in vivo activity of a multityrosine kinase inhibitor, AL3810, against human thyroid cancer, Evaluation of in vitro and in vivo activity of a multityrosine kinase inhibitor, AL3810, against human thyroid cancer, 中国药理学报:英文版, 2017, 第 3 作者
(33) Polymeric immunoglobulin receptor promotes tumor growth in hepatocellular carcinoma, HEPATOLOGY, 2017, 第 2 作者
(34) Palladium-Catalyzed, Silver-Assisted Direct C-5-H Arylation of 3-Substituted 1,2,4-Oxadiazoles under Microwave Irradiation, ADVANCED SYNTHESIS & CATALYSIS, 2017, 第 3 作者
(35) Synthesis and structure–activity relationship study of pyrazolo3,4-dpyrimidines as tyrosine kinase RET inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 通讯作者
(36) c-Myc Alteration Determines the Therapeutic Response to FGFR Inhibitors, CLINICAL CANCER RESEARCH, 2017, 第 2 作者
(37) Optimization of 1H-indazol-3-amine derivatives as potent fibroblast growth factor receptor inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 通讯作者
(38) Cyanobacterial peptides as a prototype for the design of cathepsin D inhibitors, JOURNAL OF PEPTIDE SCIENCE, 2017, 通讯作者
(39) Discovery and Biological Evaluation of a Series of Pyrrolo2,3-bpyrazines as Novel FGFR Inhibitors, MOLECULES, 2017, 通讯作者
(40) c-Myc alteration determines the therapeutic response to FGFR inhibitors., Clin Cancer Res., 2017, 
(41) Discovery of 6-(difluoro(6-(4-fluorophenyl)-1,2,4triazolo4,3-b1,2,4triazin-3-yl)methyl)quinoline as a highly potent and selective c-Met inhibitor, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2016, 通讯作者
(42) An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzobcarbazolone core, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2016, 通讯作者
(43) Design and synthesis of novel benzodoxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2016, 第 6 作者
(44) Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzobcarbazolone core, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 通讯作者
(45) The Marine-Derived Oligosaccharide Sulfate MS80, a Novel Transforming Growth Factor beta 1 Inhibitor, Reverses Epithelial Mesenchymal Transition Induced by Transforming Growth Factor-beta 1 and Suppresses Tumor Metastasis, JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2016, 通讯作者
(46) Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2016, 通讯作者
(47) Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 第 3 作者
(48) Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 通讯作者
(49) The Marine-Derived Oligosaccharide Sulfate MS80, a Novel TGF-β1 Inhibitor, Reverses TGF-β1-Induced Epithelial-Mesenchymal Transition and Suppresses Tumor Metastasis., J Pharmacol Exp Ther., 2016, 通讯作者
(50) Discovery of Substituted 1 H -Pyrazolo3,4- b pyridine Derivatives as Potent and Selective FGFR KinaseInhibitors, ACS MEDICINAL CHEMISTRY LETTERS, 2016, 通讯作者
(51) Discovery of 3-(5 '-substituted)-benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1h-indazoles as potent fibroblast growth factor receptor inhibitors: design, synthesis, and biological evaluation, JOURNAL OF MEDICINAL CHEMISTRY, 2016, 通讯作者
(52) Simm530, a novel and highly selective c-Met inhibitor, blocks c-Met-stimulated signaling and neoplastic activities, ONCOTARGET, 2016, 通讯作者
(53) Discovery of a new series of imidazo1,2-apyridine compounds as selective c-Met inhibitors, Discovery of a new series of imidazo1,2-apyridine compounds as selective c-Met inhibitors, ACTA PHARMACOLOGICA SINICA, 2016, 通讯作者
(54) Discovery of a new series of imidazo1,2-apyridine compounds as selective c-Met inhibitors, Discovery of a new series of imidazo1,2-apyridine compounds as selective c-Met inhibitors, 中国药理学报:英文版, 2016, 第11作者
(55) Design, Synthesis and Biological Evaluation of 6-(2,6-Dichloro-3,5-dimethoxyphenyl)-4-substituted-1 H -indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors, MOLECULES, 2016, 通讯作者
(56) Novel tetracyclic benzobcarbazolones as highly potent and orally bioavailable ALK inhibitors: Design, synthesis, and structure—activity relationship study, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2015, 第 3 作者
(57) Design, Synthesis and Biological Evaluation of Novel FGFR Inhibitors Bearing Indazole Scaffold., 2015, 通讯作者
(58) Discovery of Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent Inhibitory Activities against both Wild-type and Mutant ALK Kinases., J Med Chem., 2015, 
(59) Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold, ORGANIC & BIOMOLECULAR CHEMISTRY, 2015, 通讯作者
(60) Discovery of Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent Inhibitory Activities against Both Wild-type and Mutant ALK Kinases, JOURNAL OF MEDICINAL CHEMISTRY, 2015, 通讯作者
(61) 5-氨基吡唑及5-氨基三唑类成纤维细胞生长因子受体激酶抑制剂的设计合成, Design and Synthesis of 5-Aminopyrazole and 5-Aminotriazole Derivatives as Fibroblast Growth Factor Receptor Inhibitors, CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2015, 第 6 作者
(62) 5-氨基吡唑及5-氨基三唑类成纤维细胞生长因子受体激酶抑制剂的设计合成, Design and Synthesis of 5-Aminopyrazole and 5-Aminotriazole Derivatives as Fibroblast Growth Factor Receptor Inhibitors, CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2015, 第 6 作者
(63) Design and Optimization of a Series of 1-Sulfonylpyrazolo4,3-bpyridines as Selective c-Met Inhibitors, JOURNAL OF MEDICINAL CHEMISTRY, 2015, 第 13 作者
(64) Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzodisoxazole or 3-aminoindazole scaffold, BIOORGANIC & MEDICINAL CHEMISTRY, 2015, 第 8 作者
(65) Design, Synthesis, and Biological Evaluation of NovelImidazo1,2- a pyridine Derivatives as Potentc-Met Inhibitors, ACS MEDICINAL CHEMISTRY LETTERS, 2015, 第 2 作者
(66) Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2015, 第 2 作者
(67) Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities, ACS Med. Chem. Lett, 2014, 
(68) Discovery of potent, selective and non-ATP competitive c-Met inhibitors: Daphnetin C-3 dimer derivatives, ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2014, 第 2 作者
(69) Design and synthesis of 3,3 '-biscoumarin-based c-Met inhibitors, ORGANIC & BIOMOLECULAR CHEMISTRY, 2014, 第 2 作者
(70) Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold, MOLECULES, 2014, 第 2 作者
(71) SOMG-833, a Novel Selective c-MET Inhibitor, Blocks c-MET-Dependent Neoplastic Effects and Exerts Antitumor Activity, JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2014, 第 3 作者
(72) SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo, CANCER LETTERS, 2014, 第 2 作者
(73) Design, synthesis and pharmacological evaluation of 2-(thiazol-2-amino)-4-arylaminopyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2014, 第 9 作者
(74) Yhhu3813 is a novel selective inhibitor of c-Met kinase that inhibits c-Met-dependent neoplastic phenotypes of human cancer cells, Yhhu3813 is a novel selective inhibitor of c-Met kinase that inhibits c-Met-dependent neoplastic phenotypes of human cancer cells, ACTA PHARMACOLOGICA SINICA, 2014, 第 2 作者
(75) Discovery of Anilinopyrimidines as Dual Inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and Cellular Activity., ACS MEDICINAL CHEMISTRY LETTERS, 2014, 第 2 作者
(76) Yhhu3813 is a novel selective inhibitor of c-Met kinase that inhibits c-Met-dependent neoplastic phenotypes of human cancer cells, Yhhu3813 is a novel selective inhibitor of c-Met kinase that inhibits c-Met-dependent neoplastic phenotypes of human cancer cells, 中国药理学报:英文版, 2014, 第 2 作者
(77) Prenylated Indole Diketopiperazines from the Marine-Derived Fungus Aspergillus versicolor, JOURNAL OF ORGANIC CHEMISTRY, 2014, 第 4 作者
(78) Discovery of novel type II c-Met inhibitors based on BMS-777607, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2014, 第 2 作者
(79) A novel, potent, highly selective inhibitor of c-Met kinase, Simm559, inhibits c-Met-dependent neoplastic phenotypes in vitro and in vivo., MOLECULAR CANCER THERAPEUTICS, 2013, 第 1 作者
(80) Investigation on the 1,6-naphthyridine motif: discovery and SAR study of 1H-imidazo4,5-h1,6naphthyridin-2(3H)-one-based c-Met kinase inhibitors, ORGANIC & BIOMOLECULAR CHEMISTRY, 2013, 第 3 作者
(81) Discovery of 2,4-diarylaminopyrimidine SOMCL-12-81 as a potent inhibitor targeting both wild and mutant ALK kinases., MOLECULAR CANCER THERAPEUTICS, 2013, 第 2 作者
(82) Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY, 2013, 第 3 作者
(83) Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 第 2 作者
(84) Anthraquinone Derivatives as Potent Inhibitors ofc-Met Kinase and the Extracellular Signaling Pathway, ACS MEDICINAL CHEMISTRY LETTERS, 2013, 第 2 作者
(85) Energetic factors determining the binding of type I inhibitors to c-Met kinase: experimental studies and quantum mechanical calculations, ACTA PHARMACOLOGICA SINICA, 2013, 第 3 作者
(86) Further SAR studies on 3,5-diamino-7-trifluoromethylquinolines as highly potent tyrosine kinase c-Met inhibitors: efforts to correct hERG inhibition, MEDCHEMCOMM, 2012, 第 2 作者
(87) Potent HGF/c-Met Axis Inhibitors from Eucalyptus globules: the Coupling of Phloroglucinol and Sesquiterpenoid Is Essential for the Activity, Journal of Medicinal Chemistry, 2012, 
(88) Discovery of 3H-Imidazo4,5-bpyridines as Potent c-Met Kinase Inhibitors: Design, Synthesis, and Biological Evaluation, CHEMMEDCHEM, 2012, 第 5 作者
(89) Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY, 2012, 第 2 作者
(90) Multisubstituted quinoxalines and pyrido2,3-dpyrimidines: Synthesis and SAR study as tyrosine kinase c-Met inhibitors, BIOORGANICMEDICINALCHEMISTRYLETTERS, 2012, 第 2 作者
(91) Diketopiperazine alkaloids from a mangrove rhizosphere soil derived fungus Aspergillus effuses H1-1, ORGANIC & BIOMOLECULAR CHEMISTRY, 2012, 第 8 作者
(92) Potent HGF/c-Met Axis Inhibitors from Eucalyptus globulus: the Coupling of Phloroglucinol and Sesquiterpenoid Is Essential for the Activity, JOURNAL OF MEDICINAL CHEMISTRY, 2012, 第 3 作者
(93) O-Linked Triazolotriazines: Potent and Selective c-Met Inhibitors, CHEMMEDCHEM, 2012, 第 3 作者
(94) Discovering potent inhibitors against c-Met kinase: molecular design, organic synthesis and bioassay, ORGANIC & BIOMOLECULAR CHEMISTRY, 2012, 第 3 作者
(95) The Role of Polymeric Immunoglobulin Receptor in Inflammation-Induced Tumor Metastasis of Human Hepatocellular Carcinoma, JNCI-JOURNAL OF THE NATIONAL CANCER INSTITUTE, 2011, 第 1 作者
(96) The role of histone deacetylase 7 (HDAC7) in cancer cell proliferation: regulation on c-Myc, JOURNAL OF MOLECULAR MEDICINE-JMM, 2011, 第 4 作者
(97) Sulfated polymannuroguluronate inhibits Tat-induced SLK cell adhesion via a novel binding site, a KKR spatial triad, ACTA PHARMACOLOGICA SINICA, 2011, 第 2 作者
(98) Aspergiolides C and D: Spirocyclic Aromatic Polyketides with Potent Protein Kinase c-Met Inhibitory Effects, CHEMISTRY-A EUROPEAN JOURNAL, 2011, 第 2 作者
(99) Identification and synthesis of N′-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 第 3 作者
(100) Synthesis and c-Met Kinase Inhibition of 3,5-Disubstituted and 3,5,7-Trisubstituted Quinolines: Identification of 3-(4-Acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a Novel Anticancer Agent, J Med Chem, 2011, 
(101) Trigochinins A-C: Three New Daphnane-Type Diterpenes from Trigonostemon chinensis, ORGANIC LETTERS, 2010, 第 4 作者
(102) Novel carbon-bridged citrinin dimers from a volcano ash-derived fungus Penicillium citrinum and their cytotoxic and cell cycle arrest activities, TETRAHEDRON, 2010, 第 5 作者
(103) 酪氨酸激酶抑制剂类抗肿瘤药物研究方法进展, Advances in Research of Protein-tyrosine Kinases Inhibitors as Anticancer Drug, 现代生物医学进展, 2010, 第 2 作者
(104) Trigochilides A and B, Two Highly Modified Daphnane-Type Diterpenoids from Trigonostemon chinensis, ORGANIC LETTERS, 2009, 第 3 作者
(105) The Role of Polymeric Immunoglobulin Receptor in Inflammation-Induced Tumor Metastasis of Human Hepatocellular Carcinoma, JNCI JOURNAL OF THE NATIONAL CANCER INSTITUTE, 第 1 作者
(106) SIGNAL TRANSDUCTION AND TARGETED THERAPY, 第 19 作者

科研活动

   
科研项目
( 1 ) ALK二代抑制剂ZG006抗肿瘤药效学评价及克服Crizotinib耐药研究, 负责人, 国家任务, 2015-01--2018-12
( 2 ) 靶向c-Met抑制剂药效监控标志物的发现研究, 参与, 国家任务, 2012-01--2014-12
( 3 ) 中国科学院青年创新促进会人才项目, 负责人, 中国科学院计划, 2013-01--2016-12
( 4 ) 靶向酪氨酸激酶c-Met小分子抑制剂的设计、合成及抗肿瘤活性研究, 参与, 国家任务, 2012-01--2015-12
( 5 ) 新型ALK二代抑制剂丁二酸复瑞替尼(SAF-189s)个性化特征研究, 负责人, 中国科学院计划, 2015-09--2018-12
( 6 ) SCC244抗肿瘤药效学以及肿瘤适应症拓展研究, 负责人, 其他国际合作项目, 2015-07--2018-09
( 7 ) 研究免疫因子和小分子化合物在肿瘤发生发展中的调控与干预的分子机制, 参与, 国家任务, 2012-01--2016-12
( 8 ) 免疫稳态失衡在炎癌转化的开关机制-免疫负性调控因子SIRPα在免疫球蛋白受体pIgR 免疫背叛中的调控, 参与, 国家任务, 2013-01--2016-12
( 9 ) 新型成纤维生长因子受体FGFR抑制剂SO MCL-15-290的临床前研究, 负责人, 地方任务, 2017-06--2020-09
( 10 ) 新型FGFR候选新药GF008个性化特征研究——GF008获得性耐药机制探讨, 负责人, 国家任务, 2018-01--2021-12
( 11 ) 新型选择性FGFR抑制剂HH185临床前以及临床研究, 负责人, 国家任务, 2017-01--2020-12
( 12 ) 成纤维生长因子受体FGFR抑制剂SOMCL-15-290的临床前研究, 负责人, 中国科学院计划, 2016-09--2018-08
( 13 ) c-Met候选新药SCC244重塑肿瘤微环境、调节肠道菌群个性化特征与调控机制研究, 负责人, 国家任务, 2022-01--2025-12
( 14 ) HPK1抑制剂的遴选与作用特性评价, 负责人, 中国科学院计划, 2022-06--2024-06
( 15 ) AXL/FLT-3/TRK 靶向抑制剂JND30134临床前药效学特性研究, 负责人, 中国科学院计划, 2019-05--2020-12
( 16 ) 基于免疫表型的新型免疫制剂研发和肺癌精准化治疗策略研究, 参与, 地方任务, 2020-06--2025-05
( 17 ) 肝细胞癌靶向药物耐药新机制和治疗新策略的研究,课题来源, 参与, 国家任务, 2019-01--2023-12