基本信息
谢华  女  博导  中国科学院上海药物研究所
电子邮件: hxie@simm.ac.cn
通信地址: 上海张江祖冲之路555号
邮政编码:

招生信息

   
招生专业
100706-药理学
招生方向
肿瘤药理学

教育背景

2001-09--2004-07   郑州大学   博士

工作经历

   
工作简历
2011-01~2012-06,美国Hormel研究所, 博士后
2004-08~现在, 上海药物研究所, 研究员
2001-09~2004-07,郑州大学, 博士
1994-08~2004-08,郑州大学, 助教,讲师

教授课程

肿瘤药理学概论
肿瘤药理学
肿瘤药理

专利与奖励

   
奖励信息
(1) 上海市五一劳动奖章, 市地级, 2021
(2) 抗肿瘤1类新药EGFR三代抑制剂ASK120067项目, 一等奖, 市地级, 2021
专利成果
( 1 ) 联苯甲酰胺类化合物及其应用, 2023, 第 2 作者, 专利号: 2023104812661

( 2 ) 一种萘酰胺化合物治疗KRAS突变相关疾病的用途, 2022, 第 3 作者, 专利号: 202211313469.1

( 3 ) 一类四氢苯并呋喃[2,3-c]吡啶类激酶抑制剂及其制备方法及用途, 2022, 第 4 作者, 专利号: 202211167412.5

( 4 ) CSF1R激酶抑制剂及其用途, 2022, 第 3 作者, 专利号: CN114246864A

( 5 ) 嘧啶并[5,4-b]吲嗪或嘧啶并[5,4-b]吡呤化合物、其制备方法及用途, 2022, 第 3 作者, 专利号: CN109983016B

( 6 ) 一种布鲁顿酪氨酸激酶抑制剂的用途, 2021, 第 4 作者, 专利号: CN202111235137.1

( 7 ) 2-氨基嘧啶类化合物及其药物组合物和应用, 2021, 第 6 作者, 专利号: CN105601573B

( 8 ) 一类作为TBK1抑制剂的化合物、包含其的药物组合物及其用途, 2021, 第 4 作者, 专利号: 202110280860.5

( 9 ) 一类IRAK4激酶抑制剂及其制备和应用, 2021, 第 4 作者, 专利号: CN112480101A

( 10 ) 吲哚-1-碳酸酯类化合物、其制备方法和应用, 2021, 第 7 作者, 专利号: CN108250187B

( 11 ) 一种2-氨基嘧啶类化合物的多晶型形式, 2020, 第 4 作者, 专利号: CN107417626B

( 12 ) 一种2-氨基嘧啶类化合物的药用组合物及其制备方法, 2019, 第 6 作者, 专利号: CN110446701A

出版信息

   
发表论文
(1) Discovery of HCD3514 as a potent EGFR inhibitor against C797S mutation in vitro and in vivo, JOURNAL OF CANCER, 2023, 通讯作者
(2) Design, synthesis and evaluation of (R)-8-((tetrahydrofuran-2-yl)methyl)pyrido[2,3-d]pyrimidin-7-ones as novel selective ACK1 inhibitors to combat acquired resistance to the 3rd-generation EGFR inhibitor, JOURNAL OF MEDICINAL CHEMISTRY, 2023, 通讯作者
(3) Development of a series of quinazoline-2,5-diamine derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023, 通讯作者
(4) Application of deep generative model for design of Pyrrolo2,3-d pyrimidine derivatives as new selective TANK binding kinase 1 (TBK1) inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023, 通讯作者
(5) Design, synthesis and biological evaluation of KRASG12C-PROTACs as protein degraders, Bioorganic & Medicinal Chemistry, 2023, 通讯作者
(6) 18F-Labeled o‑aminopyridyl alkynyl radioligands targeting colony-stimulating factor 1 receptor for neuroinflammation imaging, BIOORGANIC & MEDICINAL CHEMISTRY, 2023, 通讯作者
(7) LS-106, a novel EGFR inhibitor targeting C797S, exhibits antitumor activities both in vitro and in vivo, CANCER SCIENCE, 2022, 通讯作者
(8) Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-GenerationEpidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations, JOURNAL OF MEDICINAL CHEMISTRY, 2022, 通讯作者
(9) Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR(T790M/C797S) Mutants, ACS MEDICINAL CHEMISTRY LETTERS, 2022, 通讯作者
(10) Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2022, 通讯作者
(11) Identification of 1H-pyrazolo3,4-bpyridine derivatives as novel and potent TBK1 inhibitors: design, synthesis, biological evaluation, and molecular docking study, JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2022, 通讯作者
(12) TANK-binding kinase 1 (TBK1): An emerging therapeutic target for drug discovery, DRUG DISCOVERY TODAY, 2021, 通讯作者
(13) 2-Oxo-3,4-dihydropyrimido4,5-d pyrimidines as new reversible inhibitors of EGFR C797S(Cys797 to Ser797)mutant, 2-Oxo-3,4-dihydropyrimido4,5-d pyrimidines as new reversible inhibitors of EGFR C797S (Cys797 to Ser797) mutant, CHINESE CHEMICAL LETTERS, 2020, 通讯作者
(14) Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance, MOLECULAR CANCER, 2020, 通讯作者
(15) C11 , a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor, suppresses breast cancer metastasis and angiogenesis, c11anovelfibroblastgrowthfactorreceptor1fgfr1inhibitorsuppressesbreastcancermetastasisandangiogenesis, ACTA PHARMACOLOGICA SINICA, 2019, 通讯作者
(16) DW10075, a novel highly selective inhibitor of vascular endothelial growth factor receptor, exhibits antitumor activities both in vitro and in vivo., Acta Pharmacol Sin, 2016, 通讯作者
(17) Discovery of 1,3-Diaryl-pyridones as Potent VEGFR-2 Inhibitors: Design, Synthesis, and Biological Evaluation, CHEMICAL BIOLOGY & DRUG DESIGN, 2016, 通讯作者
(18) Discovery and Structural Optimization of N5-Substituted 6,7-Dioxo-6,7-dihydropteridines as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation, JOURNAL OF MEDICINAL CHEMISTRY, 2016, 通讯作者
(19) Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY, 2016, 通讯作者
(20) Design, synthesis and biological evaluation of biphenylurea derivatives as VEGFR-2 kinase inhibitors (II), CHINESE CHEMICAL LETTERS, 2016, 第 8 作者
(21) A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFRL858R/T790M mutant with improved pharmacokinetic properties., Eur J Med Chem, 2016, 通讯作者
(22) C-5 Substituted Pyrido[2,3-d] pyrimidin-7-ones as highly specific kinase inhibitors targeting the clinica resistance-related EGFRT790M mutant, MedChemComm, 2015, 通讯作者
(23) Design, synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors (I), CHINESE CHEMICAL LETTERS, 2015, 第 6 作者
(24) Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors, MEDCHEMCOMM, 2015, 通讯作者
(25) 2,4-Diarylamino-pyrimidines as kinase inhibitors co-targeting IGF1R and EGFR(L858R/T790M), BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2015, 通讯作者
(26) Topoisomerase II inhibitors from the roots of Stellera chamaejasme L., BIOORGANIC & MEDICINAL CHEMISTRY, 2014, 通讯作者
(27) Identification of DW532 as a novel anti-tumor agent targeting both kinase and tubulin, Acta Pharmacologica Sinica, 2014, 通讯作者
(28) Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors, ACS MEDICINAL CHEMISTRY LETTERS, 2014, 通讯作者
(29) Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno2,3-dpyrimidines as irreversible epidermal growth factor receptor inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY, 2014, 通讯作者
(30) Novel metal complexes of naphthalimide–cyclam conjugates as potential multi-target receptor tyrosine kinase (RTK) inhibitors: Synthesis and biological evaluation, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2014, 第 7 作者
(31) Naphthalimides exhibit invitro antiproliferative and antiangiogenic activities by inhibiting both topoisomerase II (topo II) and receptor tyrosine kinases (RTKs), EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 第 9 作者
(32) Identification of an Aurora Kinase Inhibitor Specific for the Aurora B Isoform, CANCER RESEARCH, 2013, 第 1 作者
(33) Design, Synthesis and Biological Evaluation of novel 4-Anilinoquinazolines with C-6 Urea-linked side chains as the Epidermal Growth Factor Receptor (EGFR) Inhibitors, Bioorg Med Chem, 2013, 通讯作者
(34) Discovery of the novel mTOR inhibitor and its antitumor activities in vitro and in vivo, MOLECULAR CANCER THERAPEUTICS, 2013, 第 1 作者
(35) Discovery of novel selective inhibitors for EGFR-T790M/L858R, BIOORGANICMEDICINALCHEMISTRYLETTERS, 2012, 第 10 作者
(36) Identification of mammalian target of rapamycin (mTOR) as a direct target of fenretinib both in vitro and in vivo., Carcinogenesis, 2012, 第 1 作者
(37) Novel Acenaphtho[1,2-b]pyrrole Derivatives as Potent and Selective Fibroblast Growth Factor Receptors 1 Inhibitors: Design, Synthesis and Biological Evaluation., Journal of Medicinal Chemistry, 2011, 通讯作者
(38) AST1306, an irreversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, exhibits its anticancer activities both in vitro and in vivo., 2011, 第 1 作者
(39) Establishment of platform for screening insulin-like growth factor-1 receptor inhibitors and evaluation of novel inhibitors, Establishment of platform for screening insulin-like growth factor-1 receptor inhibitors and evaluation of novel inhibitors, 中国药理学报:英文版, 2011, 第 2 作者
(40) Discovery and SAR of Thiazolidine-2,4-dione Analogues as Insulin-like Growth Factor-1 Receptor (IGF-1R) Inhibitors via Hierarchical Virtual Screening, JOURNAL OF MEDICINAL CHEMISTRY, 2010, 通讯作者
发表著作
( 1 ) 《高等药理学》(第二版), 科学出版社, 2019-07, 第 其他 作者
( 2 ) 个性化药物:新药研发的未来, 上海科学技术文献出版社, 2020-03, 第 其他 作者
( 3 ) 大肠癌:基础与临床的转化, 上海交通大学出版社, 2020-06, 第 其他 作者

科研活动

   
科研项目
( 1 ) 新型VEGFR抑制剂抗肿瘤作用及生物标志物研究, 负责人, 中国科学院计划, 2015-09--2016-09
( 2 ) EGFR T790M耐药突变选择性抑制剂120067生物标志物研究, 负责人, 中国科学院计划, 2016-05--2018-12
( 3 ) 肺癌耐药新靶标的发现与确证及抑制剂研究, 负责人, 中国科学院计划, 2022-05--2023-05
( 4 ) 克服肺癌耐药新型抑制剂研发, 负责人, 中国科学院计划, 2022-06--2025-06
( 5 ) 三阴性乳腺癌转移的分子机制研究, 参与, 中国科学院计划, 2022-06--2025-06
( 6 ) 支链氨基酸转氨酶1(BCAT1)介导EGFR三代抑制剂耐药机制研究, 负责人, 国家任务, 2023-01--2026-12
( 7 ) BCAT1作为肿瘤耐药关键靶标的确证及克服BCAT1介导耐药的候选药物发现, 参与, 中国科学院计划, 2023-01--2024-12
参与会议
(1)新型EGFR三代抑制剂ASK120067抗肿瘤作用及标志物研究   四届东方药理论坛上海市药理学会第二十二届学术年会   2021-12-16
(2)Identification of novel inhibitors against EGFR T790M resistance mutation   2016-12-07