姓    名: 陈海军
性    别:

 

职    称: 副教授
学    历: 博士
职    务:
电    话: 15859189043
专    业: 药物化学
电子邮件: chenhaij@gmail.com
研究方向: 药物设计与合成

教育工作经历
教育经历
☆ 2003.09–2008.07 中国科学院上海药物研究所 博士
专业:药物化学
☆ 1999.09–2003.07 福州大学 理学和工学 双学士学位
专业:理科化学,生物工程

工作经历
☆ 2013.03-至今 福州大学化学化工学院 副教授
☆ 2011.03–2013.02 美国德州大学加尔维斯顿医学分部 博士后
☆ 2008.06–2011.02 ShangPharma 课题组长
 

教学简介
 

科研简介
主要从事创新药物设计及构效关系研究,通过基于活性天然产物类药性骨架进行多样性合成和衍生化,结合现代药物结构优化策略,探索药物的结构与活性、结构与靶向性、结构与成药性等规律,进而开发具有抗病毒、抗神经退行性疾病和抗肿瘤活性的新型药物。在新型小分子药物的设计与合成方面取得了一定的成绩,攻读博士期间,主要开展抗乙肝病毒药物的设计与合成研究工作,成功设计并合成出具有自主知识产权、拥有全新作用机制的非核苷类抗乙肝病毒创新药物(1.1类新药)——异噻氟定,该候选药物于2012年顺利获批进入临床试验。迄今,在J. Med. Chem., ACS Med. Chem. Lett., Drug Discov. Today, Cancer Lett., ChemMedChem, Eur. J. Med. Chem., Bioorg. Med. Chem., Bioorg. Med. Chem. Lett.等药物化学杂志上发表40余篇SCI论文,申请发明专利20余项,获授权专利12项。 

社会兼职
 

科研项目
引进人才项目,科研启动项目,科技发展基金,国家自然基金 

代表性论文
2016年
1. He, G.; Gao, Y.; Li, C.; Wu, G.; Li, Y.; Dong, L.; Huang, C.; Chen, H. A convenient and efficient approach to synthesize negletein from baicalin. Tetrahedron Lett 2016, 57, 2001-2005.
2. Wu, J.; Yu, X.; Liu, J.; Lin, Y.; Yu, G.; Jia, L.; Chen, H. Synthesis of metapristone through an efficient Ndemethylation of mifepristone. RSC Adv 2016, 6, 7195-7197.
3. Chen, H.; Zhou, X.; Gao, Y.; Chen, H.; Zhou, J. Fragment-Based Drug Design: Strategic Advances and Lessons Learned. Comprehensive Medicinal Chemistry, 3rd Edition 2016.
4. Zheng, Y.; Zhang, Y.; Chen, D.; Chen, H.; Lin, L.; Zheng, C.; Guo, Y. Monascus Pigment Rubropunctatin: A Potential Dual Agent for Cancer Chemotherapy and Phototherapy. J Agric Food Chem 2016, 64, 2541-2548.
5. Chen, H.; Wu, J.; Gao, Y.; Chen, H.; Zhou, J. Scaffold Repurposing of Old Drugs Towards New Cancer Drug Discovery. Curr Top Med Chem 2016, DOI: 10.2174/1568026616666160216155556.
6. Liu, R.; Shi, P.; Nie, Z.; Liang, H.; Zhou, Z.; Chen, W.; Chen, H.; Dong, C.; Yang, R.; Liu, S.; Chen, C. Mifepristone Suppresses Basal Triple-Negative Breast Cancer Stem Cells by Down-regulating KLF5 Expression. Theranostics 2016, 6, 533-544.
7. Yang, L.; Wang, Y. J.; Chen, H. J.; Shi, L. P.; Tong, X. K.; Zhang, Y. M.; Wang, G. F.; Wang, W. L.; Feng, C. L.; He, P. L.; Xu, Y. B.; Lu, M. J.; Tang, W.; Nan, F. J.; Zuo, J. P. Effect of a hepatitis B virus inhibitor, NZ-4, on capsid formation. Antiviral Res 2016, 125, 25-33.

2015年
8. Chen, H.; Zhou, X.; Wang, A.; Zheng, Y.; Gao, Y.; Zhou, J. Evolutions in Fragment-Based Drug Design: Deconstruction-Reconstruction Approach. Drug Discov Today 2015, 20, 105-113.
9. Chen, H. J.; Huang, X. R.; Zhou, X. B.; Zheng, B. Y.; Huang, J. D. Potential sonodynamic anticancer activities of artemether and liposome-encapsulated artemether. Chem Commun (Camb) 2015, 51, 4681-4684.
10. Chen, H.; Gao, Y.; Wang, A.; Zhou, X.; Zheng, Y.; Zhou, J. Evolution in medicinal chemistry of ursolic acid derivatives as anticancer agents. Eur J Med Chem 2015, 92, 648-655.
11. Gao, Y.; Ding, Y.; Chen, H.; Chen, H.; Zhou, J. Targeting Krl-Like Factor 5 (KLF5) for Cancer Therapy. Curr Top Med Chem 2015, 15, 699-713.
12. Gao, Y.; Li, Z.; Wang, C.; You, J.; Jin, B.; Mo, F.; Chen, J.; Zheng, Y.; Chen, H. Self-assembled chitosan/rose bengal derivative nanoparticles for targeted sonodynamic therapy: preparation and tumor accumulation. RSC Adv 2015, 5, 17915–17923.
13. Xu, H. N.; Chen, H. J.; Zheng, B. Y.; Zheng, Y. Q.; Ke, M. R.; Huang, J. D. Preparation and sonodynamic activities of water-soluble tetra-alpha-(3-carboxyphenoxyl) zinc(II) phthalocyanine and its bovine serum albumin conjugate. Ultrason Sonochem 2015, 22, 125-131.
14. Gao, Y.; Li, Z.; Xie, X.; Wang, C.; You, J.; Mo, F.; Jin, B.; Chen, J.; Shao, J.; Chen, H.; Jia, L. Dendrimeric anticancer prodrugs for targeted delivery of ursolic acid to folate receptor-expressing cancer cells: Synthesis and biological evaluation. Eur J Pharm Sci 2015, 70C, 55-63.
15. Ye, N.; Zhu, Y.; Chen, H.; Liu, Z.; Mei, F. C.; Wild, C.; Chen, H.; Cheng, X.; Zhou, J. Structure-Activity Relationship Studies of Substituted 2-(Isoxazol-3-yl)-2-oxo-N'-phenyl-acetohydrazonoyl Cyanide Analogues: Identification of Potent Exchange Proteins Directly Activated by cAMP (EPAC) Antagonists. J Med Chem 2015, 58, 6033-6047.
16. Zhu, Y.; Chen, H.; Boulton, S.; Mei, F.; Ye, N.; Melacini, G.; Zhou, J.; Cheng, X. Biochemical and pharmacological characterizations of ESI-09 based EPAC inhibitors: defining the ESI-09 "therapeutic window". Sci Rep 2015, 5, 9344.

2014年
17. Chen, H.; Zhou, X.; Gao, Y.; Zheng, B.; Tang, F.; Huang, J. Recent progress in development of new sonosensitizers for sonodynamic cancer therapy. Drug Discov Today 2014, 19, 502-509.
18. Chen, H.; Gao, Y.; Wu, J.; Chen, Y.; Chen, B.; Hu, J.; Zhou, J. Exploring therapeutic potentials of baicalin and its aglycone baicalein for hematological malignancies. Cancer Lett 2014, 354, 5-11.
19. Chen, H.; Wild, C.; Zhou, X.; Ye, N.; Cheng, X.; Zhou, J. Recent Advances in the Discovery of Small Molecules Targeting Exchange Proteins Directly Activated by cAMP (EPAC). J Med Chem 2014, 57, 3651-3665.
20. Chen, H.; He, G.; Li, C.; Dong, L.; Xie, X.; Wu, J.; Gao, Y.; Zhou, J. Development of a Concise Synthetic Approach to Access Oroxin A. RSC Adv 2014, 4, 45151-45154.
21. Chen, H.; Mrazek, A. A.; Wang, X.; Ding, C.; Ding, Y.; Porro, L. J.; Liu, H.; Chao, C.; Hellmich, M. R.; Zhou, J. Design, synthesis, and characterization of novel apigenin analogues that suppress pancreatic stellate cell proliferation in vitro and associated pancreatic fibrosis in vivo. Bioorg Med Chem 2014, 22, 3393-3404.
22. Chen, H.; Yang, Z.; Ding, C.; Xiong, A.; Wild, C.; Wang, L.; Ye, N.; Cai, G.; Flores, R. M.; Ding, Y.; Shen, Q.; Zhou, J. Discovery of potent anticancer agent HJC0416, an orally bioavailable small molecule inhibitor of signal transducer and activator of transcription 3 (STAT3). Eur J Med Chem 2014, 82C, 195-203.
23. Yang, L.; Shi, L. P.; Chen, H. J.; Tong, X. K.; Wang, G. F.; Zhang, Y. M.; Wang, W. L.; Feng, C. L.; He, P. L.; Zhu, F. H.; Hao, Y. H.; Wang, B. J.; Yang, D. L.; Tang, W.; Nan, F. J.; Zuo, J. P. Isothiafludine, a novel non-nucleoside compound, inhibits hepatitis B virus replication through blocking pregenomic RNA encapsidation. Acta Pharmacol Sin 2014, 35, 410-418.
24. Natarajan, R.; Singal, V.; Benes, R.; Gao, J.; Chan, H.; Chen, H.; Yu, Y.; Zhou, J.; Wu, P. STAT3 Modulation to Enhance Motor Neuron Differentiation in Human Neural Stem Cells. PLoS One 2014, 9, e100405.
25. Wang, W. L.; Huang, C.; Gao, L. X.; Tang, C. L.; Wang, J. Q.; Wu, M. C.; Sheng, L.; Chen, H. J.; Nan, F. J.; Li, J. Y.; Li, J.; Feng, B. Synthesis and biological evaluation of novel bis-aromatic amides as novel PTP1B inhibitors. Bioorg Med Chem Lett 2014, 24, 1889-1894.
26. Wang, J.; Chen, J.; Wan, L.; Shao, J.; Lu, Y.; Zhu, Y.; Ou, M.; Yu, S.; Chen, H.; Jia, L. Synthesis, spectral characterization, and in vitro cellular activities of metapristone, a potential cancer metastatic chemopreventive agent derived from mifepristone (RU486). AAPS J 2014, 16, 289-298.
27. Gao, Y.; Xie, J.; Chen, H.; Gu, S.; Zhao, R.; Shao, J.; Jia, L. Nanotechnology-based intelligent drug design for cancer metastasis treatment. Biotechnol Adv 2014, 32, 761-777.
28. Ding, C.; Wang, L.; Chen, H.; Wild, C.; Ye, N.; Ding, Y.; Wang, T.; White, M. A.; Shen, Q.; Zhou, J. ent-Kaurane-based regio- and stereoselective inverse electron demand hetero-Diels-Alder reactions: synthesis of dihydropyran-fused diterpenoids. Org Biomol Chem 2014, 12, 8442-8452.

2013年
29. Chen, H.; Yang, Z.; Ding, C.; Chu, L.; Zhang, Y.; Terry, K.; Liu, H.; Shen, Q.; Zhou, J. Fragment-based drug design and identification of HJC0123, a novel orally bioavailable STAT3 inhibitor for cancer therapy. Eur J Med Chem 2013, 62, 498-507.
30. Chen, H.; Yang, Z.; Ding, C.; Chu, L.; Zhang, Y.; Terry, K.; Liu, H.; Shen, Q.; Zhou, J. Discovery of O-Alkylamino Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents. ACS Med Chem Lett 2013, 4, 180-185.
31. Chen, H.; Wang, C. Z.; Ding, C.; Wild, C.; Copits, B.; Swanson, G. T.; Johnson, K. M.; Zhou, J. A combined bioinformatics and chemoinformatics approach for developing asymmetric bivalent AMPA receptor positive allosteric modulators as neuroprotective agents. ChemMedChem 2013, 8, 226-230.
32. Chen, H.; Tsalkova, T.; Chepurny, O. G.; Mei, F. C.; Holz, G. G.; Cheng, X.; Zhou, J. Identification and characterization of small molecules as potent and specific EPAC2 antagonists. J Med Chem 2013, 56, 952-962.
33. Chen, H.; Ding, C.; Wild, C.; Liu, H.; Wang, T.; White, M. A.; Cheng, X.; Zhou, J. Efficient Synthesis of ESI-09, A Novel Non-cyclic Nucleotide EPAC Antagonist. Tetrahedron Lett 2013, 54, 1546-1549.
34. Wang, W. L.; Yang, D. L.; Gao, L. X.; Tang, C. L.; Ma, W. P.; Ye, H. H.; Zhang, S. Q.; Zhao, Y. N.; Xu, H. J.; Hu, Z.; Chen, X.; Fan, W. H.; Chen, H. J.; Li, J. Y.; Nan, F. J.; Li, J.; Feng, B. 1H-2,3-dihydroperimidine derivatives: a new class of potent protein tyrosine phosphatase 1B inhibitors. Molecules 2013, 19, 102-121.
35. Ding, C.; Zhang, Y.; Chen, H.; Yang, Z.; Wild, C.; Ye, N.; Ester, C. D.; Xiong, A.; White, M. A.; Shen, Q.; Zhou, J. Oridonin ring A-based diverse constructions of enone functionality: identification of novel dienone analogues effective for highly aggressive breast cancer by inducing apoptosis. J Med Chem 2013, 56, 8814-8825.
36. Ding, C.; Zhang, Y.; Chen, H.; Yang, Z.; Wild, C.; Chu, L.; Liu, H.; Shen, Q.; Zhou, J. Novel nitrogen-enriched oridonin analogues with thiazole-fused A-ring: protecting group-free synthesis, enhanced anticancer profile, and improved aqueous solubility. J Med Chem 2013, 56, 5048-5058.
37. Ding, C.; Zhang, Y.; Chen, H.; Wild, C.; Wang, T.; White, M. A.; Shen, Q.; Zhou, J. Overcoming synthetic challenges of oridonin A-ring structural diversification: regio- and stereoselective installation of azides and 1,2,3-triazoles at the C-1, C-2, or C-3 position. Org Lett 2013, 15, 3718-3721.
38. Almahariq, M.; Tsalkova, T.; Mei, F. C.; Chen, H.; Zhou, J.; Sastry, S. K.; Schwede, F.; Cheng, X. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol Pharmacol 2013, 83, 122-128.

2012年之前
39. Chen, H.; Tsalkova, T.; Mei, F. C.; Hu, Y.; Cheng, X.; Zhou, J. 5-Cyano-6-oxo-1,6-dihydro-pyrimidines as potent antagonists targeting exchange proteins directly activated by cAMP. Bioorg Med Chem Lett 2012, 22, 4038-4043.
40. Wang, W. L.; Chen, H. J.; Ma, W. P.; Gu, M.; Fan, M. Z.; Li, J. Y.; Feng, B.; Nan, F. J. Synthesis and antiviral activity of conformational analogues of leucamide A. Molecules 2012, 17, 14522-14530.
41. Chen, H. J.; Liu, Y.; Wang, L. N.; Shen, Q.; Li, J.; Nan, F. J. Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B. Bioorg Med Chem Lett 2010, 20, 2876-2879.
42. Chen, H. J.; Wang, W. L.; Wang, G. F.; Shi, L. P.; Gu, M.; Ren, Y. D.; Hou, L. F.; He, P. L.; Zhu, F. H.; Zhong, X. G.; Tang, W.; Zuo, J. P.; Nan, F. J. Rational design and synthesis of 2,2-bisheterocycle tandem derivatives as non-nucleoside hepatitis B virus inhibitors. ChemMedChem 2008, 3, 1316-1321.
43. Wan, J.; Zhu, Y. N.; Feng, J. Q.; Chen, H. J.; Zhang, R. J.; Ni, J.; Chen, Z. H.; Hou, L. F.; Liu, Q. F.; Zhang, J.; Yang, L.; Tang, W.; Yang, Y. F.; Nan, F. J.; Zhao, W. M.; Zuo, J. P. Periplocoside A, a pregnane glycoside from Periploca sepium Bge, prevents concanavalin A-induced mice hepatitis through inhibiting NKT-derived inflammatory cytokine productions. Int Immunopharmacol 2008, 8, 1248-1256.


 

获奖情况
☆ 2012年Behavior, Biology and Chemistry (BBC) meeting travel award
☆ 2008年中国科学院“优秀毕业生”
☆ 中科院2007-2008学年“三好学生”
☆ 2003年福州大学“优秀毕业生”
 

其他
 
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