基本信息
周兵  男  博导  中国科学院上海药物研究所
电子邮件: zhoubing@simm.ac.cn
通信地址: 上海市祖冲之路555号3508室
邮政编码:

招生信息

   
招生专业
100701-药物化学
招生方向
表观遗传创新药物研究
药物化学
C-H活化方法学

教育背景

2008-09--2011-06   中国科学院上海药物研究所   博士
2004-09--2007-03   同济大学   硕士
2000-09--2004-07   同济大学   学士

工作经历

   
工作简历
2016-03~现在, 中国科学院上海药物研究所, 研究员
2013-04~2016-03,美国密歇根大学, 博士后
2011-06~2013-03,美国普渡大学, 博士后
2008-09~2011-06,中国科学院上海药物研究所, 博士
2007-04~2008-08,和记黄埔医药(上海)有限公司, 助理研究员
2004-09~2007-03,同济大学, 硕士
2000-09~2004-07,同济大学, 学士

教授课程

药物化学

专利与奖励

   
奖励信息
(1) 上海市优秀学术带头人, 省级, 2022
(2) 上海市青年五四奖章, 省级, 2022
(3) 上海市青年科技启明星, 省级, 2017
(4) 国家海外高层次人才, 国家级, 2017
(5) 上海市药学科技奖, 二等奖, 省级, 2012
专利成果
( 1 ) 抑制SHP2活性的杂环化合物、其制备方法及用途(PCT), 2022, 第 1 作者, 专利号: WO2022237367A1

( 2 ) 三氮唑并嘧啶衍生物、其药物组合物及用途, 2022, 第 1 作者, 专利号: CN115028631A

( 3 ) 抑制SHP2活性的杂环化合物、其制备方法及用途, 2022, 第 1 作者, 专利号: CN114716448A

( 4 ) 甲状腺素受体β 选择性激动剂化合物、其药物组合物和用途(PCT), 2022, 第 1 作者, 专利号: WO2022127699A1

( 5 ) 甲状腺素受体β 选择性激动剂化合物、其药物组合物和用途, 2022, 第 1 作者, 专利号: CN114634486A

( 6 ) 一种治疗血栓性疾病的化合物, 2022, 第 3 作者, 专利号: CN113968855A

( 7 ) 抑制RIP1激酶的杂环酰胺及其用途(日本), 2021, 第 1 作者, 专利号: JP2021535190A

( 8 ) 抑制RIP1激酶的杂环酰胺及其用途(美国), 2021, 第 1 作者, 专利号: US20210371430A1

( 9 ) 组蛋白乙酰转移酶(HAT)抑制剂及其用途(日本), 2021, 第 1 作者, 专利号: JP2021522317A

( 10 ) 一种杂环化合物及其用途, 2021, 第 1 作者, 专利号: CN112940004A

( 11 ) 三氮唑并嘧啶、三氮唑并吡啶化合物及其组合物用于治疗PRC2 介导的疾病(日本), 2020, 第 1 作者, 专利号: JP2020535215A

( 12 ) 乙烯基磺酰胺或乙烯基酰胺类化合物及其制备方法和用途, 2020, 第 2 作者, 专利号: CN112010789A

( 13 ) 溴结构域抑制剂化合物及其用途(美国), 2020, 第 1 作者, 专利号: US20200354371A1

( 14 ) 三氮唑并嘧啶、三氮唑并吡啶化合物及其组合物用于治疗PRC2 介导的疾病(美国), 2020, 第 1 作者, 专利号: US20200261459A1

( 15 ) 一类杂环化合物,其制备及用途, 2020, 第 1 作者, 专利号: CN111377934A

( 16 ) 抑制RIP1激酶的杂环酰胺及其用途, 2020, 第 1 作者, 专利号: CN111138448A

( 17 ) 组蛋白乙酰转移酶(HAT)抑制剂及其用途, 2019, 第 1 作者, 专利号: CN110386927A

( 18 ) 一种三氮唑并嘧啶衍生化合物、包含其的药物组合物及其用途, 2019, 第 1 作者, 专利号: CN110156787A

( 19 ) 溴结构域抑制剂化合物及其用途, 2019, 第 1 作者, 专利号: CN110041333A

( 20 ) 三氮唑并嘧啶、三氮唑并吡啶化合物及其组合物用于治疗PRC2介导的疾病, 2019, 第 1 作者, 专利号: CN109843890A

( 21 ) 三氮唑并嘧啶、三氮唑并吡啶化合物及其组合物用于治疗PRC2介导的疾病, 2019, 第 1 作者, 专利号: CN109575013A

( 22 ) 1,4‑双取代‑1,2,3,6‑四氢吡啶类化合物、其制备方法、药物组合物及其应用, 2018, 第 4 作者, 专利号: CN107602446A

( 23 ) 咯哌丁胺衍生物及其在制备治疗混合谱系白血病的药物中的应用, 2018, 第 4 作者, 专利号: CN107602445A

( 24 ) N-取代含氟苯基-14β-氨甲基表雷公藤内酯醇衍生物及其制备方法和用途, 2012, 第 3 作者, 专利号: CN102443040A

( 25 ) N-取代-14β-氨甲基表雷公藤内酯醇衍生物及其制备方法和用途, 2012, 第 3 作者, 专利号: CN102443043A

( 26 ) N-取代含甲氧基苯基-14β-氨甲基表雷公藤内酯醇衍生物及其制备方法和用途, 2012, 第 3 作者, 专利号: CN102443042A

( 27 ) N-取代含甲基苯基-14β-氨甲基表雷公藤内酯醇衍生物及其制备方法和用途, 2012, 第 3 作者, 专利号: CN102443041A

( 28 ) N-取代含酯基苯基-14β-氨甲基表雷公藤内酯醇衍生物及其制备方法和用途, 2012, 第 3 作者, 专利号: CN102443044A

( 29 ) N-取代氨基苯基-14β-氨甲基表雷公藤内酯醇衍生物及其制备方法和用途, 2012, 第 3 作者, 专利号: CN102443039A

( 30 ) N-取代苯基-14β-氨甲基表雷公藤内酯醇衍生物及其制备方法和用途, 2012, 第 3 作者, 专利号: CN102443045A

( 31 ) 新型松香烷型二萜衍生物、其制备方法和应用, 2011, 第 3 作者, 专利号: CN102286065A

( 32 ) 3-取代-4-酮-14-甲氧基松香烷类化合物、其制备方法和用途, 2010, 第 2 作者, 专利号: CN101723865A

出版信息

   
发表论文
(1) Cyclization strategy leads to highly potent Bromodomain and extra-terminal (BET) Bromodomain inhibitors for the treatment of acute liver injury, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023, 通讯作者
(2) Discovery of Highly Potent and Selective Thyroid Hormone Receptor β Agonists for the Treatment of Nonalcoholic Steatohepatitis, Journal of Medicinal Chemistry, 2023, 通讯作者
(3) Rh(III)-catalyzed twofold unsymmetrical C-H alkenylation-annulation/amidation reaction enabled delivery of diverse furoquinazolinones, TETRAHEDRON LETTERS, 2022, 通讯作者
(4) Potent and Selective RIPK1 Inhibitors Targeting Dual-Pockets for the Treatment of Systemic Inflammatory Response Syndrome and Sepsis, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2022, 通讯作者
(5) Discovery of a Potent and Selective Degrader for USP7, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2022, 通讯作者
(6) Rhodium(III)-Catalyzed Asymmetric 1,2-Carboamidation of Alkenes Enables Access to Chiral 2,3-Dihydro-3-benzofuranmethanamides, ORGANIC LETTERS, 2022, 通讯作者
(7) Discovery of novel Thieno2,3-dimidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2022, 通讯作者
(8) Celastrol recruits UBE3A to recognize and degrade the DNA binding domain of steroid receptors, ONCOGENE, 2022, 通讯作者
(9) The p300 Inhibitor A-485 Exerts Antitumor Activity in Growth Hormone Pituitary Adenoma, JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 2022, 通讯作者
(10) A potent PGK1 antagonist reveals PGK1 regulates the production of IL-1β and IL-6, ACTA PHARMACEUTICA SINICA B, 2022, 通讯作者
(11) Rh(III)-catalyzed selective C7-H functionalization of indolines with 1,3-enynes enables access to six-membered 1,7-fused indolines, TETRAHEDRON LETTERS, 2021, 通讯作者
(12) Inhibition of Autophagy by a Small Molecule through Covalent Modification of the LC3 Protein, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2021, 通讯作者
(13) Rhodium-Catalyzed Twofold Unsymmetrical C-H Alkenylation-Annulation/Thiolation Reaction To Access Thiobenzofurans, ORGANIC LETTERS, 2021, 通讯作者
(14) Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021, 通讯作者
(15) Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021, 通讯作者
(16) Discovery of a subtype-selective, covalent inhibitor against palmitoylation pocket of TEAD3, Discovery of a subtype-selective, covalent inhibitor against palmitoylation pocket of TEAD3, ACTA PHARMACEUTICA SINICA B, 2021, 通讯作者
(17) Discovery of 8-Methyl-pyrrolo1,2-apyrazin-1(2H)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors, JOURNAL OF MEDICINAL CHEMISTRY, 2020, 通讯作者
(18) Rh(iii)-catalyzed tandem annulative redox-neutral arylation/amidation of aromatic tethered alkenes, CHEMICAL SCIENCE, 2020, 通讯作者
(19) RUTHENIUM(II)-CATALYZED REGIOSELECTIVE C-H HYDROXYMETHYLATION OF N-ARYL-AZAINDOLES WITH PARAFORMALDEHYDE, HETEROCYCLES, 2020, 通讯作者
(20) Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2020, 通讯作者
(21) Design, synthesis, and biological evaluation of tetrahydroquinolin derivatives as potent inhibitors of CBP bromodomain, BIOORGANIC CHEMISTRY, 2020, 通讯作者
(22) Ruthenium(II)-Catalyzed Regioselective Ortho C-H Allenylation of Electron-Rich Aniline and Phenol Derivatives, JOURNAL OF ORGANIC CHEMISTRY, 2020, 通讯作者
(23) Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors, JOURNAL OF MEDICINAL CHEMISTRY, 2020, 通讯作者
(24) Ru(II)-catalyzed regioselective C-7 hydroxymethylation of indolines with formaldehyde, TETRAHEDRON LETTERS, 2019, 通讯作者
(25) Discovery and biological evaluation of vinylsulfonamide derivatives as highly potent, covalent TEAD autopalmitoylation inhibitors, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2019, 通讯作者
(26) p300/CBP inhibitor A-485 alleviates acute liver injury by regulating macrophage activation and polarization, THERANOSTICS, 2019, 第 9 作者
(27) Rh(III)-catalyzed Redox-Neutral Unsymmetrical C-H Alkylation and Amidation Reactions of N-Phenoxyacetamides, J. Am. Chem. Soc, 2018, 
(28) Rh(III)-Catalyzed C-H Functionalization of Indoles with Diazo Compounds: Facile Synthesis of Structurally Diverse 2,3-Fused Indoles, Adv. Synth. Catal., 2018, 通讯作者
(29) Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor, JOURNAL OF MEDICINAL CHEMISTRY, 2018, 第 2 作者
(30) Rh(III)-Catalyzed Redox-Neutral Unsymmetrical C-H Alkylation and Amidation Reactions of &ITN&IT-Phenoxyacetamides, JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2018, 通讯作者
(31) Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression, JOURNALOFMEDICINALCHEMISTRY, 2018, 第 3 作者
(32) Rhodium-Catalyzed C-H Functionalization of Indoles with Diazo Compounds: Synthesis of Structurally Diverse 2,3-Fused Indoles, ADVANCEDSYNTHESISCATALYSIS, 2018, 通讯作者
(33) A Rh(III)-catalyzed redox-neutral C-H alkylation reaction with allylic alcohols by using a traceless oxidizing directing group, ORGANIC CHEMISTRY FRONTIERS, 2018, 通讯作者
(34) Discovery of 1,8-acridinedione derivatives as novel GCN5 inhibitors via high throughput screening, EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 通讯作者
(35) Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors, BIOORGANIC & MEDICINAL CHEMISTRY, 2018, 通讯作者
(36) High-Affinity Peptidomimetic Inhibitors of the DCN1-UBC12 Protein Protein Interaction, JOURNAL OF MEDICINAL CHEMISTRY, 2018, 第 3 作者
(37) Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression, JOURNAL OF MEDICINAL CHEMISTRY, 2018, 第 1 作者
(38) Discovery and optimization of selective inhibitors of protein arginine methyltransferase 5 by docking-based virtual screening, ORGANIC & BIOMOLECULAR CHEMISTRY, 2017, 第11作者
(39) Ruthenium-Catalyzed Direct Hydroxymethylation of Aryl C-H Bonds, ACS CATALYSIS, 2017, 通讯作者
(40) Rhodium(III)-Catalyzed Selective C-H Acetoxylation and Hydroxylation Reactions, ORGANIC LETTERS, 2017, 通讯作者
(41) Targeted degradation of BET proteins in triple-negative breast cancer, CANCER RESEARCH, 2017, 第 2 作者
(42) Rhodium(iii)-catalyzed alkylation of primary C(sp(3))-H bonds with α-diazocarbonyl compounds., 2016, 第 6 作者
(43) Rhodium(iii)-catalyzed alkyllation of primary c(sp(3))-h bonds with alpha-diazocarbonyl compounds, CHEMICAL COMMUNICATIONS, 2016, 通讯作者
(44) Identification of novel small-molecule inhibitors targeting menin-MLL interaction, repurposing the antidiarrheal loperamide, ORGANIC & BIOMOLECULAR CHEMISTRY, 2016, 其他(合作组作者)
(45) Structure-based Design of γ-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors, JOURNAL OF MEDICINAL CHEMISTRY, 2015, 第 6 作者
(46) Ir-III-Catalyzed Direct C-7 Amidation of Indolines with Sulfonyl, Acyl, and Aryl Azides at Room Temperature, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, 2015, 通讯作者
(47) Iridium(III)-Catalyzed C-7 Selective C-H Alkynylation of Indolines at Room Temperature, JOURNAL OF ORGANIC CHEMISTRY, 2015, 通讯作者
(48) Rh(III)- or Ir(III)-catalyzed ynone synthesis from aldehydes via chelation-assisted C-H bond activation, CHEMICAL COMMUNICATIONS, 2015, 第 7 作者
(49) A 4+1 Cyclative Capture Approach to 3H-Indole-N-oxides at Room Temperature by Rhodium(III)-Catalyzed C-H Activation, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2015, 通讯作者
(50) Rhodium-Catalyzed Redox-Neutral C-H Functionalization of Arylamine N-Oxides with Diazo Compounds: Primary C(sp3)-H/C(sp2)-H Activation and Oxygen Atom Transfer., Angew.Chem. Int. Ed., 2015, 通讯作者
(51) Access to Six- and Seven-Membered 1,7-Fused Indolines via Rh(III)-Catalyzed Redox-Neutral C7-Selective C-H Functionalization of Indolines with Alkynes and Alkenes, JOURNAL OF ORGANIC CHEMISTRY, 2015, 第 6 作者
(52) Rh(III)-Catalyzed C-H Amidation with N-Hydroxycarbamates: A New Entry to N-Carbamate-Protected Arylamines, ORGANIC LETTERS, 2014, 通讯作者
(53) Rhodium-Catalyzed Directed Sulfenylation of Arene C-H Bonds, CHEMISTRY-A EUROPEAN JOURNAL, 2014, 通讯作者
(54) Copper(I)-Catalyzed Aryl or Vinyl Addition to Electron-Deficient Alkenes Cascaded by Cationic Cyclization, ORGANIC LETTERS, 2014, 通讯作者
(55) Rhodium- Catalyzed Direct Amination of Arenes with Nitrosobenzenes: A New Route to Diarylamines, CHEMISTRY-A EUROPEAN JOURNAL, 2014, 第 5 作者
(56) Rh(III)-Catalyzed Intramolecular Redox-Neutral or Oxidative Cyclization of Alkynes: Short, Efficient Synthesis of 3,4-Fused Indole Skeletons, ORGANIC LETTERS, 2014, 通讯作者
(57) Rh(III)- and Ir(III)-Catalyzed C7-Alkylation of Indolines with Diazo Compounds., Chem. Eur. J., 2014, 通讯作者
(58) Rhodium(III)-Catalyzed Intramolecular Redox-Neutral Annulation of Tethered Alkynes: Formal Total Synthesis of (+/-)-Goniomitine, CHEMISTRY-A EUROPEAN JOURNAL, 2014, 通讯作者
(59) Rhodium-Catalyzed Direct Addition of Aryl C-H Bonds to Nitrosobenzenes at Room Temperature, ORGANIC LETTERS, 2013, 通讯作者
(60) Assembly of Spirooxindole Derivatives Containing Four Consecutive Stereocenters by Using Cascade Reactions Catalyzed by an N-Heterocyclic Carbene, CHEMISTRY-A EUROPEAN JOURNAL, 2013, 通讯作者
(61) Rhodium-Catalyzed Synthesis of Amides from Aldehydes and Azides by Chelation-Assisted CH Bond Activation, CHEMISTRY-A EUROPEAN JOURNAL, 2013, 通讯作者
(62) Enantioselective synthesis of spirocyclohexane-1,3′-indolin-2′-ones containing multiple stereocenters via organocatalytic Michael/aldol cascade reactions, TETRAHEDRON LETTERS, 2013, 第 2 作者
(63) S-Adenosyl-Homocysteine Is a Weakly Bound Inhibitor for a Flaviviral Methyltransferase, PLOS ONE, 2013, 第 2 作者
(64) Rhodium-Catalyzed Direct Addition of Indoles to N-Sulfonylaldimines, ADVANCED SYNTHESIS & CATALYSIS, 2013, 通讯作者
(65) Total Synthesis of (-)-(α)-Kainic Acid via a Diastereoselective Intramolecular [3+2] Cycloaddition Reaction of Aryl Cyclopropyl Ketone with an Alkyne., Org. Lett., 2013, 通讯作者
(66) Rhodium(III)-Catalyzed Amidation of Aryl Ketone O-methyl Oximes with Isocyanates via C-H Activation: Convergent Synthesis of 3-Methyleneisoindolin-1-ones., Chem. Eur. J., 2013, 通讯作者
(67) Bifunctional cinchona alkaloid-squaramide-catalyzed highly enantioselective aza-Michael addition of indolines to α,β-unsaturated ketones, TETRAHEDRON LETTERS, 2013, 第 2 作者
(68) Rh(III)-Catalyzed Addition of Alkenyl C-H Bond to Isocyanates and Intramolecular Cyclization: Direct Synthesis 5-Ylidenepyrrol-2(5H)-ones, ORGANIC LETTERS, 2013, 通讯作者
(69) Synthesis of Six-Membered Spirocyclic Oxindoles with Five Consecutive Stereocenters in an Asymmetric Organocatalytic One-Pot Michael/Michael/Aldol Addition Sequence, JOURNAL OF ORGANIC CHEMISTRY, 2013, 通讯作者
(70) Rhodium(III)-Catalyzed Intermolecular Direct Amidation of Aldehyde C H Bonds with N-Chloroamines at Room Temperature, ORGANIC LETTERS, 2013, 通讯作者
(71) Rhodium(III)-Catalyzed Synthesis of Cyclopentabpyrroles from 1,2-Diketones, 2-Aminopyridine, and Alkynes, CHEMISTRY-AN ASIAN JOURNAL, 2013, 通讯作者
(72) Rhodium-catalyzed oxidative C2-acylation of indoles with aryl and alkyl aldehydes, CHEMICAL COMMUNICATIONS, 2012, 第 1 作者
(73) Rhodium-Catalyzed Oxidative ortho-Acylation of Aryl Ketone O-Methyl Oximes with Aryl and Alkyl Aldehydes, ADVANCED SYNTHESIS & CATALYSIS, 2012, 通讯作者
(74) A Concise Synthetic Approach to (+)-Valienamine Starting from Garner's Aldehyde, SYNLETT, 2012, 第 1 作者
(75) Synthesis of Entecavir (BMS-200475), TETRAHEDRON LETTERS, 2012, 第 1 作者
(76) Rhodium-catalyzed regioselective amidation of indoles with sulfonyl azides via C-H bond activation, ORGANIC & BIOMOLECULAR CHEMISTRY, 2012, 通讯作者
(77) Total synthesis of novel D-ring-modified triptolide analogues: structure-cytotoxic activity relationship studies on the D-ring of triptolide, ORGANIC & BIOMOLECULAR CHEMISTRY, 2011, 第 1 作者
(78) Synthesis and biological evaluation of novel triptolide analogues for anticancer activity, BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 第 1 作者
(79) Efficient synthesis of the key intermediate triptophenolide methyl ether for the synthesis of (−)-triptolide, TETRAHEDRON, 2010, 第 1 作者
(80) ChemInform Abstract: Rhodium(III)‐Catalyzed Alkylation of Primary C(sp3)—H Bonds with α‐Diazocarbonyl Compounds., CHEMINFORM, 第 6 作者

科研活动

   
科研项目
( 1 ) 老药新用—Menin-MLL相互作用小分子抑制剂的发现和结构优化, 负责人, 中国科学院计划, 2016-01--2017-12
( 2 ) 组蛋白乙酰化酶抑制剂的发现与优化, 负责人, 中国科学院计划, 2018-01--2019-12
( 3 ) VIII族元素(钴、铑、铱)催化的C(sp3)-H键官能化反应研究, 负责人, 国家任务, 2018-01--2020-12
( 4 ) p300/CBP小分子抑制剂的发现与结构优化, 负责人, 国家任务, 2020-01--2023-12
( 5 ) 化合物高效合成技术, 负责人, 国家任务, 2018-01--2020-12
( 6 ) 国家“海外高层次人才引进计划”青年项目, 负责人, 国家任务, 2018-01--2020-12
( 7 ) Menin-MLL相互作用小分子抑制剂的构效关系与成药性研究, 负责人, 地方任务, 2017-04--2020-03
( 8 ) 靶向TEADs高选择性小分子创新药物研究, 负责人, 地方任务, 2022-09--2025-08