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 您现在的位置:首页 > 机构设置 > 研究机构 > 研究室 > 药物化学研究室 > 张 翱研究组
张 翱研究组
张 翱研究组

 

   目前研究组共有成员18名,包括:研究员1名,助理研究员2名,博士后1名,研究助理4名,硕博研究生6名,联合培养研究生5名。

 

 

   张翱研究组主要从事创新药物研发及相关基础研究,尤其是靶向G-蛋白偶联受体(GPCR)和酪氨酸激酶(RTK)新型小分子药物的设计与合成研究。主要是通过发展新颖简捷合成方法实现类药性优势骨架的高效合成,以及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,进而开发具有抗神经退行性疾病和抗肿瘤活性的新型药物。

 

  【1】具有抗肿瘤活性的类药性天然产物的合成及基于成药性的结构优化;

  【2】靶向酪氨酸激酶或DNG修复等特异性或多靶性抑制剂抗肿瘤药物的设计与合成;

  【3】靶向G-蛋白偶联受体小分子药物的设计及抗神经退行性疾病活性研究。

 

 

  一、药物设计与合成代表性文章(2007-):

  1. Hai Zhang, Na Ye, Shanglin Zhou, Lin Guo, Longtai Zheng, Zhili Liu, Bo Gao, Xuechu Zhen, and Ao Zhang: Identification of N-Propylnoraporphin-11-yl 5-(1,2-Dithiolan-3-yl)pentanoate as a New Anti-Parkinson's Agent Possessing a Dopamine D2 and Serotonin 5-HT1A Dual-Agonist Profile. J. Med. Chem. 2011, 54, 4324-4338.
  2. Yuanxiang Wang,Jing Ai,Ying Wang, Yi Chen, Lu Wang,Gang Liu, Meiyu Geng, Ao Zhang: Synthesis and c-Met kinase inhibition of 3,5-di- and 3,5,7-tri- substituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)- 5-(3-nitrobenzylamino)- 7- (trifluoromethyl)quinoline as a novel anticancer agent. J. Med. Chem. 2011, 54, 2127–2142.
  3. Zhili Liu,Hai Zhang,Na Ye, Jing Zhang, QianQian Wu, Peihua Sun, Linyong Li, Xuechu Zhen,andAo Zhang: Synthesis of Dihydrofuroaporphine Derivatives: Identification of a Potent and Selective Serotonin 5-HT1A Receptor Agonist. J. Med. Chem. 2010, 53, 1319-1328.
  4. Ao Zhang, Fuying Li, Chunyong Ding, Qizheng Yao, Jean M Bidlack, Jannifer E Hilbert, Brian I Knapp, John L Neumeyer: Further Investigation on the Ring C of Levorphanol: Synthesis and Pharmacological Evaluation of 6,7-Thiazolo/ Indolo-Morphinans. J. Med. Chem. 2007, 50, 2747-2751.
  5. Ao Zhang, Yi Zhang, Ross J Baldessarini, John L Neumeyer: Development of aporphinoids as dopaminergic agents. J. Med. Chem. 2007, 50, 181-191.
  6. Ao Zhang (Guest Editor): ReceptorDimerization and Bivalent Ligands, an Emerging Topic for Drug Design. Curr. Top. Med. Chem.2007, 7,341.
  7. Ao Zhang,* John L Neumeyer, Ross J Baldessarini: Recent Progress in the Development of Dopamine Receptor Subtype Compounds: Potential Therapeutic Agents for Neurological and Neuropsychiatric Disorders. Chem. Rev. 2007, 107, 274-303.
  8. Fuying Li, Chenlei Yin, Jie Chen, Jinggen Liu, Xin Xie, Ao Zhang:[6,7]-Heterocycle-Fused 14-Hydroxymorphinan Derivatives: Design, Synthesis, and Opioid Receptor Activity. ChemMedChem 2009, 4, 2103-2110.
  9. Zhili Li, Jing Zhang, Ao Zhang: Design of multivalent ligand targeting g-protein-coupled receptors. Curr Pharm Des. 2009, 15, 682-718.
  10. Jing Zhang, Bing Xiong, Xuechu Zhen, Ao Zhang: Dopamine D1 receptor ligands: Where are we now and where are we going, Med. Res. Rev. 2009, 29, 272-294.

  二、 药物合成方法学代表性文章:

  1. Chengtang Du, Fulong Li, Xuefeng Zhang, Wenxiang Hu, Qizheng Yao, Ao Zhang. Lewis Acid-Catalyzed Cyclization of Glycals/2-deoxy-D-ribose with Aryl Amines: Additional Findings on Product Structure and Reaction Diastereoselectivity. J. Org. Chem. 2011, 76,8833-8839.
  2. Fulong Li, Chunyong Ding, Meining Wang, Qizheng Yao, Ao Zhang: InBr3-Catalyzed Glycosidation of Glycals with Arylamines: An Alternative Approach To Access 4-Aminocyclopent-2-enones. J. Org. Chem. 2011, 76, 2820–2827.
  3. Yuanxiang Wang, Jing Ai, Gang Liu, Meiyu Geng, Ao Zhang. Expeditious one-pot synthesis of C3-piperazinyl-substituted quinolines: key precursors to potent c-Met inhibitors. Org. Biomol. Chem. 2011, 9, 5930-5933.
  4. Jing Zhang, Kui Wu, Meining Wang, Jianqin Jiang, Ao Zhang: FeCl3.6H2O-promoted skeleton-rearrangement of 1-substituted-3-benzazepines: substrate extension and product utilization. Tetrahedron2011, 67, 842-848.
  5. Chunyong Ding, Shanghui Tu, Qizheng Yao, Fulong Li, Yuanxiang Wang, Wenxiang Hu, Ao Zhang: One-Pot Three-step Synthesis of Naphtho [2,3-a]carbazole-5,13-diones Using Tandem Radical Alkylation-Cyclization -Aromatization Reaction Sequence. Adv Syn Catal 2010, 352, 847-853.
  6. Yi Zhang, Zhaobin Han, Fuying Li, Kuiling Ding and Ao Zhang: Highly enantioselective hydrogenation of a-aryl-b-substituted acrylic acids catalyzed by Ir-SpinPHOX.Chem. Commun.2010, 46, 156–158.
  7. Jing Zhang, Ao Zhang: Unprecedented FeCl3·6H2O-Promoted Skeleton-Rearrangement of 1-Aryl-2,3,4,5-tetrahydro-1H-3-benzazepines: a New Strategy for the Synthesis of C-1 Quaternary Tetrahydroisoquinolines. Chem. Eur. J.2009, 15, 11119-11122.
  8. Chunyong Ding, Shanghui Tu,Fuying Li, Yuanxiang Wang, Qizheng Yao,Wenxiang Hu,Hua Xie, Linghua Meng, Ao Zhang: Synthesis Study on Marmycin A: Preparation of the C3’-Desmethyl Analogues. J. Org. Chem. 2009, 74, 6111-6119.
  9. Yuanxiang Wang, Ao Zhang: Expeditious synthesis of 2,3-dihydro-2-alkoxy-3-methylenebenzofurans from N-benzofuran-3-ylmethyl N,N,N-trialkylammonium bromides. Tetrahedron2009, 65, 6986-6990.
  10. Ao Zhang, Chunyong Ding, Chen Cheng, Qizhen Yao: Convenient synthesis of natural products-based 2,7-naphthyridines. J. Comb. Chem. 2007, 9, 916-919.

 

 

 
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研究室组织结构

  徐明华课题组 /  沈敬山课题组李援朝课题组柳 红课题组沈竞康课题组

 

 

   研究组目前正在进行的研究课题主要有:

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