【近年来获得的学术科研成果】 主持和参加了国家自然科学基金计划、国家重大新药创制专项、中国科学院新药研究科技专项、部省级科研计划和企业合作项目近10项,主持完成项目5项。获行业科技进步奖1次,公开和获得授权国家发明专利共计20项。在包括Journal of Medicinal Chemistry、European Journal of Medicinal Chemistry、Journal of Biological Chemistry、Journal of Organic Chemistry、ChemMedChem和Bioorganic & Medicinal Chemistry Letters等国内外重要学术期刊发表论著30余篇。 【近年来主要研究课题】 [1]共价结合药物研发技术,重大新药创制科技重大专项(2018ZX09711002-007-001),主持在研 [2] E76K突变型蛋白酪氨酸磷酸酶SHP2变构抑制剂的设计、连续化合成及抗髓系白血病活性研究,国家自然科学基金面上项目(21772068),主持在研 [3] E76K突变型蛋白酪氨酸磷酸酶SHP2变构抑制剂的设计、合成及构效关系研究,新药研究国家重点实验室开放课题(SIMM1705KF-01)主持在研 [4]基于连续流化学技术的新型吖啶酯化学发光诊断试剂的研发,江苏省政策引导类计划(产学研合作)前瞻性联合研究项目(BY2016022-37)主持在研 [5]新型SHP2选择性抑制剂设计、合成及构效关系研究,主持国家自然科学基金面上项目(21472069)主持结题 [6]新型抗血吸虫药物的发现及结构优化,卫生部寄生虫病预防与控制技术重点项目(WK014-002)主持结题 【近年来主要代表作】 [1]Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitor.Bioorganic & Medicinal Chemistry Letters.2018,24, 1889–1894. [2]Decoquinate derivatives: A new class of potent antischistosomal agents againstSchistosoma japonicum.Chinese Chemical Letters.2017,28(7), 1547-1552. [3]Synthesis of Aromatic Amide Derivatives and Their Biological Evaluation against Protein Tyrosine Phosphatase 1B and Scr Homology-2 Domain Containing Protein Tyrosine Phosphatase-2. Chinese. Journal of Organic Chemistry. 2016, 36(9), 2142-2149. [5]Synthesis of Novel 3-aryl-1-oxa-2,8-diazaspiro[4.5]dec-2-ene Derivatives and Their Biological Evaluation Against Protein Tyrosine Phosphatase 1B.Chemical Biology & Drug Design2015, 86(5), 1161–1167. [6]Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors.Bioorganic & Medicinal Chemistry Letters2014,24, 1889-1894. [7]1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors.Molecules.2014,19, 102-121. [8]Synthesis and evaluation of the antischistosomal activity against S. japonicum of 1-methyl-1,2,3,4-tetrahydroisoquinoline derivatives.Chinese. Journal of Organic Chemistry.2013,33,2588-2599. [9]Synthesis and SAR studies of praziquantel derivatives with activity againstSchistosoma japonicum.Molecules.2013,18(8), 9163-9178. [10]Synthesis and antiviral activity of conformational analogues of leucamide A.Molecules.2012,17(12), 14522-14530. [11]Synthesis and biological evaluation of salicylate-based compounds as a novel class of methionine aminopeptidase inhibitors.Bioorganic & Medicinal Chemistry Letters.2011,21(23), 7151-7154. [12]Inhibition of Mycobacterium tuberculosis Methionine Aminopeptidases by Bengamide Derivatives.ChemMedChem.2011,6, 1041-1048. [13]Growth inhibition ofEscherichia coliand methicillin-resistantStaphylococcus aureusby targeting cellular methionine aminopeptidase.European Journal Medicinal Chemistry2011,46, 3537-3540. [14]Searching for Disease Modifiers - PKC Activation and HDAC Inhibition - A Dual Drug Approach to Alzheimer’s Disease that Reduces Aβ Production while Blocking Oxidative Stress.ChemMedChem.2009,4, 1095-1105. [15]Synthesis and structure-function analysis of Fe(II)-form-selective antibacterial inhibitors of Escherichia coli methionine aminopeptidase,Bioorganic & Medicinal Chemistry Letters.2009,19, 1080-1083. [16]Fe(II) is the native cofactor forEscherichia colimethionine aminopeptidase.Journal of Biological Chemistry.2008, 283,26879-26885. [17]Discovery of inhibitors ofEscherichia colimethionine aminopeptidase with the Fe(II)-form selectivity and antibacterial activity.Journal of Medicinal Chemistry.2008, 51,6110-6120. [18]Discovery and Structural Modification of Inhibitors Of Human Hepatitis B Virus inspired from marine natural product Leucamide A.ChemMedChem.2008,3, 1316-1321. [19]Synthesis and biological evaluation of novel bisheterocycle-containing compounds as potential anti-influenza virus agents.Bioorganic & Medicinal Chemistry Letters. 2005,15(23), 5284-5287. [20]First total synthesis of leucamide A.Journal of Organic Chemistry.2003,68(4), 1636-1639. 【主要授权国家发明专利】 [1]一类2,3-二氢萘嵌间二氮杂苯类似物、其合成方法、药物组合物及用途(ZL201310365517.6) [2]一类苯环-芳香环串联化合物、其制备方法和医药用途(ZL201410030074.X) [3]一类螺异噁唑啉衍生物、其制备方法及医药用途(ZL201410112206.3) [4]一类1,2,5-噁二唑-2氧化物类似物、其制备方法和用途(ZL201310298298.4) [5]一类吡喹酮类似物、其制备方法和用途(ZL201310007886.8) |