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药物化学系

发布者:金雪明发布时间:2020-04-21浏览次数:1584

本系概况

我系现有教师14名,其中教授7名,副教授5名,讲师2名。包括国家杰出青年基金获得者1名,特聘教授3名,博士生导师4名,硕士生导师8名。本系承担药学院本科生及研究生药物化学等相关课程的教学,开设药物化学、药物合成反应等课程,本系在本科生及研究生培养方面取得丰硕成果,近两年先后获得省级优秀硕士论文及优秀本科生论文奖励,指导国家级、省级、校级大学生创新计划10余项。

 

科学研究

药物化学系主要从事具有自主知识产权的小分子化学药物的研究与开发,同时针对与新药研发过程密切相关的基础理论和关键技术开展系统研究,其研究领域涉及先导化合物的发现和结构优化、计算机辅助药物设计、化学生物学、药物合成新技术新方法等。重点研究抗肿瘤药物、抗病毒药物、抗寄生虫药物、抗炎免疫药物、神经系统疾病及心血管疾病治疗药物。
       
近年来,承担了国家级科研项目10余项、省部及市厅级项目20余项,在J Med ChemEuro J Med Chem ACS Chem Neurosci Bioorg Med ChemAdv. Synth. CatalOrg  LettOrg Biomol ChemJ Org Chem等专业杂志上发表SCI 收录论文100余篇,申请专利50余项。

 


主要研究方向及近期论文

 

一、先导药物的发现和结构优化

1. Development of Adenosine A2A Receptor Antagonists for the Treatment of Parkinson's Disease: A Recent Update and Challenge. ACS Chem. Neurosci.2019, 10, 783-791.

2. Orphan Receptor GPR88 as an Emerging Neurotherapeutic Target. ACS Chem. Neurosci., 201910, 190−200.

3.N-Arylsulfonylsubstituted-1H indole derivatives as small molecule dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and tubulin. Bioorg. Med.Chem201826, 96–106.

4. Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3). J. Med. Chem. 201861, 1204-1217.

5. Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT). J. Med. Chem. 201861, 1541-1551.

6. Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for Combinational Treatment of Leukemia and Invasive Fungal Infections. J Med Chem, 2018, 61, 6056-6074.

7. Discovery of potent and novel smoothened antagonists via structure-based virtual screening and biological assays. Eur. J. Med. Chem. 2018,155, 34-48.

8. Discovery and characterization of a potent Wnt and hedgehog signaling pathways dual inhibitor. Eur. J. Med. Chem. 2018,149, 110-121.

9. Rational Design of Conjugated Photosensitizers with Controllable Photoconversion for Dually Cooperative Phototherapy. Advanced Materials, 2018, 30, 1801216.

10. Design, Synthesis, and Structure-Activity-Relationship of a Novel Series of CXCR4 Antagonists. Eur. J. Med. Chem. 2018,149, 30-44.

11. Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout. Bioorg Med Chem2018, 26, 1653-1664.

12. Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents, Bioorg. Med. Chem. Lett. 2017, 27, 1341-1345.

 

药物合成新方法

1. “The Employment of Sodium Hydride as a Michael Donor in Palladium-catalyzed Reductions of α, β-Unsaturated Carbonyl CompoundsAdv. Synth. Catal.,2019, 361, DOI: 10.1002/adsc.201801676.

2. HFIP-Promoted Michael Reactions: Direct para-Selective C-H Activation of Anilines with Maleimides. Org. Biomol. Chem.201917 2242-2246.

3. “Thermo-promoted Reactions of Anthranils with Carboxylic Acids, Amines, Phenols and Malononitrile under Catalyst-free ConditionsJ. Org. Chem. 2019, 84 (4), 2022-2031.

4. Cu-Mediated Stereoselective [4+2]Annulation between N-Hydroxybenzimidoyl Cyanide and Norbornene  The Journal of Organic Chemistry2018, 83,8457-8463.

5. Oxycyanation of Vinyl Ethers with 2,2,6,6-Tetramethyl-N-oxopiperidinium Enabled by Electron Donor-Acceptor Complex. Org. Lett. 2018, 20, 720-723.

6. “Pd-Catalyzed Debenzylation and Deallylation of Ethers and Esters with Sodium HydrideACS catal., 2018, 8 (4), 3016-3020.

7. Palladium-Catalyzed Oxidative Three-Component Coupling of Anthranilamides with Isocyanides and Arylboronic Acids:Access to 2,3-Disubstituted Quinazolinones  The Journal of Organic Chemistry  2018, 83,9201-9209

8.  “Visible light-promoted umpolung coupling of aryl tri-/difluoroethanones with 2-alkenylpyridines” Chem. Commun. 201854, 11017-11020.

9. Palladium-catalyzed carbonylative synthesis of isocoumarins and phthalides by using phenyl formate as a carbon monoxide source Org. Biomol. Chem2017, 1628-1635.

 


药物化学系教师

 

姓名

职称职务

办公室

电子邮箱

龙亚秋

医学部副主任,教授

云轩楼2311

longyaqiu@suda.edu.cn

张小虎

系主任,教授

云轩楼1427

xiaohuzhang@suda.edu.cn

季兴跃

系副主任,教授

云轩楼1237

jixy@suda.edu.cn

刘峰

系副主任,教授

云轩楼1125

fliu2@suda.edu.cn

乔春华

教授

云轩楼1432

qiaochunhua@suda.edu.cn

朱永明

教授

云轩楼1438

zhuyongming@suda.edu.cn

张士磊

教授

云轩楼1439

zhangshilei@suda.edu.cn

敖桂珍

副教授

云轩楼1430

aoguizhen@suda.edu.cn

胡延维

副教授

云轩楼1434

huyanwei@suda.edu.cn

李环球

副教授

云轩楼1324

huanqiuli@suda.edu.cn

叶娜

副教授

云轩楼1225

yena@suda.edu.cn

何慧

副教授

云轩楼1329

hhe@suda.edu.cn

郑计岳

讲师

云轩楼1523

jyzheng@suda.edu.cn

田盛

讲师

云轩楼2307

stian@suda.edu.cn