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药物设计与合成 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。

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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. 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. 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, DOI: 10.1039/c1035cc00927h. Gao, Y.; Ding, Y.; Chen, H.; Chen, H.; Zhou, J. Targeting Krl-Like Factor 5 (KLF5) for Cancer Therapy. Curr Top Med Chem 2015, DOI: 10.2174/1568026615666150302105052. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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. 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.

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