个人简介
向皞月,硕士生导师,毕业于中科院上海药物研究所,在杂环化合物库的构建、苗子/先导化合物的发现取得了一定进展。构建了基于色酮的含氮杂环小分子化合物库,并从中发现了一些结构新颖的抗肿瘤先导化合物;设计合成了系列PI3K抑制剂,在体外表现出了良好的抗肿瘤活性。2015年加入中南大学以来,致力于光氧化还原催化体系研究以及含氮/氟杂环小分子化合物库构建新方法的开发。2021年受KC Wong奖学金资助,赴英国King's College London和University College London进行酶催化领域博士后研究工作。主持国家自然科学基金、湖南省优青、中国博士后科学基金面上项目等课题5项,以第一或通讯作者在Angew. Chem. Int. Ed.,ACS Catal., Org. Lett., J. Org. Chem., Eur J Med Chem., Bioorg. Med. Chem. Lett.,等国际权威期刊发表SCI论文60余篇,参与撰写学术专著2部,申请PCT专利1项(已在美国、欧盟、日本等国授权),授权中国专利2项。
科研项目:
1. 2022-2024 基于可见光-有机催化绿色合成方法学研究 湖南省自然科学基金委 优青项目
2. 2020-2023 可见光促进的含氟杂环化合物库集群式构建研究 湖南省自然科学基金委 面上项目
3. 2018~2020 基于优势骨架的片螺素类似物的设计/优化及抗肿瘤活性研究 国家自然科学基金委 青年基金
4. 2017~2018 选择性靶向PI3K的共价键抑制剂/酶降解剂的 新药研究国家重点实验室
5. 2017~2018 芳基取代吡咯并三嗪类化合物的抗肿瘤活性研究 中国博士后基金会
6. 2017~2019 新型呫吨酮衍生物的设计合成及抗肿瘤活性研究 湖南省自然科学基金委 青年基金
代表性学术论文:(ORCID, 0000-0002-7404-4247)
2020
Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo [2,1-f] [1,2,4] triazine derivatives. Bioorganic & Medicinal Chemistry Letters 2020, 30, 127194.
Photoinduced Single-Electron-Transfer Process as an Enabling Principle in Radical Borylation of Alkenes with NHC-borane Angewandte Chemie International Edition 2020, 59, 6706-6710.
Photocatalytic C-F Bond Borylation of Polyfluoroarenes with NHC-boranes.Organic Letters 2020, 22, 1742-1747.
Phosphine-Mediated MBH-Type/Umpolung Addition Domino Sequence: Divergent Construction of Coumarins. Organic Letters 2020, 22, 488-492.
Visible-Light-Induced, Catalyst-Free Radical Cross-Coupling Cyclization of N-Allylbromodifluoroacetamides with Disulfides or Diselenides. Journal of Organic Chemistry 2020, 85, 5670-5682.
O-Perfluoropyridin-4-yl Oximes: Iminyl Radical Precursors for Photo- or Thermal-Induced N-O Cleavage in C(sp(2)) C(sp(3)) Bond Formation. Journal of Organic Chemistry 2020, 85, 3538-3547.
2019
Visible-Light-Driven, Photoredox-Catalyzed Cascade of ortho-Hydroxycinnamic Esters To Access 3-Fluoroalkylated Coumarins. Journal of Organic Chemistry 2019, 84, 7480-7487.
Photocatalytic, Phosphoranyl Radical-Mediated N-O Cleavage of Strained Cycloketone Oximes. Organic Letters 2019, 21, 2658-2662. (ESI高被引)
Organocatalytic, Enantioselective, Polarity-Matched Ring-Reorganization Domino Sequence Based on the 3-Oxindole Scaffold. Organic Letters 2019, 21, 2166-2170.
A One-Pot Ring-Opening/Ring-Closure Sequence for the Synthesis of Polycyclic Spirooxindoles. Chemistry-A European Journal 2019, 25, 4673-4677.
Photocatalytic reductive radical-radical coupling of N,N '-cyclicazomethine imines with difluorobromo derivatives. Chemical Communications 2019, 55, 2712-2715.
2018
Visible-Light-Induced External Radical-Triggered Annulation To Access CF2-Containing Benzoxepine Derivatives. Organic Letters 2018, 20, 1363-1366.
Solvent-Minimized, Chromatography-Free, Diastereoselective Synthesis of Oxazolidine-Dispirooxindoles via oxa-1,3-Dipolar Cycloaddition of 3-Oxindole. Journal of Organic Chemistry 2018, 83, 2948-2953.
Photoredox-catalyzed direct aminoalkylation of isatins: diastereoselective access to 3-hydroxy-3-aminoalkylindolin-2-ones analogues. Organic Chemistry Frontiers 2018, 5, 1608-1612.
Visible-Light-Promoted Synthesis of 1,4-Dicarbonyl Compounds via Conjugate Addition of Aroyl Chlorides. Chemistry-an Asian Journal 2018, 13, 271-274.
Organocatalytic Domino Entry to an Octahydroacridine Scaffold Bearing Three Contiguous Stereocenters. Journal of Organic Chemistry 2018, 83, 12284-12290.
Unraveling and Manipulating the Stereospecific Retro-Aldol Reaction in the Organocatalytic Asymmetric Aldol Reaction of Isatin and Cyclohexanone. Organic Letters 2018, 20, 7535-7538.
7-Site Substituted Pyrrole Triazine Compounds or Pharmaceutically Acceptable Salts Thereof, and Preparation Method Therefor and Uses Thereof. 2018, WO20182333684 (A1).
2017-
Selectfluor-Triggered Tandem Cyclization of o-Hydroxyarylenaminones To Access Difluorinated 2-Amino-Substituted Chromanones. Journal of Organic Chemistry 2017, 82, 9837-9843.
Visible-Light-Driven, Radical-Triggered Tandem Cyclization of o-Hydroxyaryl Enaminones: Facile Access to 3-CF2 /CF3-Containing Chromones. Organic Letters 2017, 19, 146-149.(Nature Index)
Photoredox-Catalyzed Reductive Dimerization of Isatins and Isatin-Derived Ketimines: Diastereoselective Construction of 3,3′-Disubstituted Bisoxindoles. Journal of Organic Chemistry 2017, 82, 3895-3900.
Diastereoselective Intramolecular [3 + 2]-Annulation of Donor–Acceptor Cyclopropane with Imine-Assembling Hexahydropyrrolo[3,2-c]quinolinone Scaffolds. Journal of Organic Chemistry 2016, 81, 11185-11194.
A Facile and General Approach to 3-((Trifluoromethyl)thio)-4H-chromen-4-one. Organic Letters 2014, 16, 5686-5689.(Nature Index)
教育经历
[1] 2006.9-2010.7
湖南师范大学 | 制药工程 | 学士学位 | 大学本科毕业
[2] 2010.9-2015.7
中科院上海药物研究所 | 药物化学 | 博士学位 | 博士研究生毕业
工作经历
[1] 2021.6-2022.11
King's College London/University College London/Nanomerics
|
药学院
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KC Wong Fellow/技术顾问(Nanomerics)
[2] 2017.9-至今
中南大学
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化学化工学院
|
副教授 硕士生导师
[3] 2015.9-2017.9
中南大学
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化学化工学院
|
讲师
团队成员
团队名称:阳华课题组
团队介绍:阳华,博士,中南大学“升华学者”特聘教授,博士生导师。阳华教授长期以来致力于有机合成,不对称催化,可见光催化及手性药物分子的全合成研究工作,主持国家自然科学基金,湖南省科技厅重点项目,参与多项美国NSF以及NIH的基金研究工作。研发出具有优异性能的有机催化剂-“Hua Cat”, 广泛应用在手性分子的不对称合成中,并申请国际专利,并已通过精细化学品公司-- Sigma-Aldrich公司商品化,在全球销售。近年来在J. Am. Chem. Soc., Org. Lett., Chem. Comm., J. Org. Chem. 等世界一流期刊上发表学术论文近50篇。