【近5年来主要科研成果概述】 1.主持国家级、省级科研项目2项,主持国内、国外医药企业委托的创新药及仿制药研究项目多项。 2.在EJMC、BMCL、CBDD等药物设计、药物化学领域重要期刊发表论文20余篇。 3.申请发明专利20余项,现授权8项,部分专利获得美国、欧盟、俄罗斯等国际授权。 【近5年来主持项目】 1.基于囊泡内药物代谢途径发现的肿瘤多药耐药机制研究(国家自然科学基金,主持,结题) 2.以心肌肌球蛋白为靶的新型抗心力衰竭药物研发(江苏省前瞻性联合研究项目,主持,结题) 3.原料药及新化合物的工艺研究与开发(北京万生药业有限责任公司,主持,结题) 4. APAP合成工艺优化研究(诺化仕(无锡)制药有限公司,主持,结题) 5. PROTAC分子设计及抗肿瘤活性评价(常州润诺生物科技有限公司,主持,在研) 6. FY001创新药物项目化合物设计、合成及抗肿瘤活性测试技术服务(北京福元医药股份有限公司,主持,在研) 7.对乙酰氨基酚合成工艺研究(诺化仕(无锡)制药有限公司,主持,在研) 8.医药应用为导向的多硫醇合成工艺条件优化及其与M-XDI聚合工艺研究(江苏快达农化股份有限公司,主持,在研) 【近5年来代表性论文】 1. Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors[J]. Bioorganic & Medicinal Chemistry Letters, 2020, 30(23). 2. Pyrazolo[1,5- a ]pyrimidine based Trk inhibitors: Design, synthesis, biological activity evaluation[J]. Bioorganic & Medicinal Chemistry Letters, 2021, 31, 127712. 3. Discovery and biological evaluation of novel G protein‐coupled receptor 119 agonists for type 2 diabetes[J]. Archiv der Pharmazie, 2019, 352(4): 1800267. 4. Design, synthesis, and evaluation of a series of novel phenylpropanoic acid derivatives agonists for the FFA1[J]. Chemical biology & drug design, 2019, 93(5): 900-909. 5. Design, synthesis and biological evaluation of 2-(4-(methylsulfonyl)phenyl)pyridine derivatives as GPR119 agonists. Chemical biology & drug design[J]. 2019, 93(1): 67-74. 6. Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors. European Journal of Medicinal Chemistry. 2018, 157: 935-945. 7. Synthesis and biological evaluation of novel 5, 6-dihydropyrimido [4, 5-f] quinazoline derivatives as potent CDK2 inhibitors. Bioorganic & medicinal chemistry letters. 2018, 28(20): 3385-3390. 8. TrpC5 regulates differentiation through the Ca2+/Wnt5a signalling pathway in colorectal cancer[J]. Clinical Science, 2017, 131(3): 227-237. 9. Gene expression profiling of H9c2 cells subjected to H2O2-induced apoptosis with/without AF-HF001.[J]. Biological & Pharmaceutical Bulletin, 2016, 39(2):207-214. 10. Zebrafish as a New Model for Phenotype-based Screening of Positive Inotropic Agents[J]. Chemical biology & drug design, 2015, 85(3): 253-258. 11. Synthesis and In Vivo Hepatoprotective Activity of Some Novel Andrographolide Derivatives[J]. Letters in Drug Design & Discovery, 2014, 11(5): 677-685. 12. Synthesis and Biological Evaluation of Andrographolide Derivatives as Potent Hepatoprotective Agents[J]. Chemical biology & drug design, 2014, 83(3): 324-333. 【近5年主要授权专利】 1.一种增强TRPV4-KCa2.3复合体耦联度的化合物及其在抗高血压中的应用. CN107056715B; 2. Compound for enhancing TRPV4-KCa2.3 complex coupling degree and its application in anti-hypertension drug. US10336712(美国授权)、EP 3556747(欧盟授权)、RU 2718913(俄罗斯授权) 3.吡唑并[4,3-h]喹唑啉类化合物及其用途. CN107383019A 4.一种嘧啶并[4,5-f]喹唑啉类化合物及其用途. CN108484606A 5.一种含氮氢类化合物的烷基化方法及其应用. CN108503583A 6.一种吡唑并[1,5-a]嘧啶类化合物及其应用. CN108484613B |