姓  名:
董晓武
工作单位:
浙江大学药学院
职  称:
教授
职  务:
办公电话:
邮  箱:
dongxw@zju.edu.cn
学科专业:
药学(专业学位)
研究方向:
蛋白降解、偶联药物的发现和应用
个人简介

董晓武, 博士,教授,博士生导师,药学系副主任,浙江大学创新药物研究中心副主任,浙江省杰出青年基金获得者。主要从事药物化学和化学生物学的研究,致力于合理药物设计和新药发现,聚焦靶向蛋白降解、人工智能药物设计、药物重定位等技术及其在新型先导分子发现中的应用,擅长创新药物临床前研究注册申报,主导研发的多个候选药物获得化药1类新药临床试验批件,并进入I、II期临床研究,部分品种已实现成果转化。迄今,在Nucleic Acids Res.、Adv. Sci.、J. Med. Chem、Brief. Bioinformatics.等国际著名刊物上发表论文100余篇,他引2000次,H指数为25。授权国家发明专利20项,其中国际授权专利4项,担任J. Am. Chem. Soc., J.Med. Chem.等期刊审稿人、浙江省药学会理事、浙江省药学会药物化学与抗生素专委会副主任委员、浙江省生物医学学会医药创新与转化专业委员会副主任委员、浙江省生物信息学学会智能药学专委会常务委员、《中国药物化学杂志》、《中国现代应用药学》等杂志编委等学术兼职。主持了国家自然科学基金面上项目3项、十三五国家新药创制重大专项、浙江省“领雁”研发攻关计划等项目,先后获浙江省科技进步奖二等奖2项。

 

教育背景

2009.7 – 2011.6  浙江大学药学院 博士后

2004.9-2009.6  浙江大学药学院  药物化学 博士

2000.9-2004.6  浙江大学药学院 药物制剂专业 学士

 

工作经历

2020.1-至今        浙江大学药学院  教授

2015.1-2019.12  浙江大学药学院 副教授 

2011.9-2013.1    香港大学化学系 博士后

2011.7-2014.12  浙江大学药学院 讲师

 

成果荣誉

详细见浙江大学药学院教师个人主页 https://person.zju.edu.cn/xiaowu

 

主持项目

  • 浙江省“领雁”研发计划攻关项目(2023C03111),针对CYP1B1表观遗传调控的新型Menin-MLL抑制剂发现、优化及抗肝癌候选药物研究

  • 新型去泛素化酶USP10抑制剂的发现、构效关系和抗肝癌机制研究,国家自然科学基金面上项目(82173660)

  • 针对肝癌去泛素酶异常调控的新型先导分子发现和机制研究,浙江省自然科学基金杰出青年项目(LR21H300003

  • 基于人工智能的新型冠状病毒导致肺纤维化的药物发现及机制研究,应急科研专项(2020XGZX010)

  • 针对多发性硬化症的新型取代哌啶类促巨噬细胞M2极化调节剂的构效关系和机制研究,国家自然基金面上项目(81973172) 

  • 靶向蛋白酶体的Best-in-class创新药物E83的系统临床前任务, “重大新药创制”科技重大专项(2018ZX09711002-011-022)

  • 新型AKT抑制剂Hu7691、Hu7151抗肿瘤新药的临床前研究任务, “重大新药创制”科技重大专项 2018ZX09711002-011-023

  • 基于靶向蛋白降解嵌合分子(PROTACs)策略的新型Akt蛋白降解功能分子的设计、合成及抗肿瘤活性评价, 中科院上海药物研究所新药研究国家重点实验室, 开放研究课题(SIMM1705KF-08)

  • 新型E3泛素连接酶WSB-1抑制剂的设计、合成和抗肿瘤转移活性研究,国家自然基金面上项目(81673294) 

  • 吡唑苯环类Akt-Braf双靶点抑制剂的设计、合成和抗肿瘤活性研究”, 浙江省科技厅公益性项目(2016C33067)

  • 新型吡唑-呋喃类Akt抑制剂设计、合成和生物活性评价”,浙江省自然科学基金(LY13H300002

  • “基于靶标结构的新型Akt抑制剂的设计、合成和抗肿瘤活性研究”,中国博士后基金一等资助(20090460103)

  • “类黄酮衍生物的心血管保护作用及类药性评价”,浙江省医药卫生科学研究基金计划(2010KYA061)

  •  苯并吡喃酮类Akt抑制剂的设计、合成以及抗肿瘤活性研究”,国家自然科学基金(青年基金,81001359

  • “苯并吡喃酮类Akt抑制剂的设计、合成以及抗肿瘤活性研究”中国博士后基金特别资助(201003734)

  • “基于靶标结构的苯并吡喃酮类Akt抑制剂的设计、合成和抗肿瘤活性研究”天然药物及仿生药物国家重点实验室(北京大学)开放基金课题编号(K20100108)

  • p53-MDM2Akt酶双靶点抑制剂的设计、合成和抗肿瘤活性研究”浙江省教育厅科研项目(Y201018915,参与

  • 新型哌嗪类CCR5拮抗剂的设计、合成和抗HIV活性研究 国家自然科学基金(81072515,参与



 

发表论文

2023:

109. Lei, T.; Wu, Y.; Zhang, W.; Lu, J.; Han, S.; Zhuang, Y.; Dong, X.*; Yang, H.*Peripheral immune cell profiling of double-hit lymphoma by mass cytometry. BMC Cancer 2023, 23(1), 184.

108. Gao, J.; Shen, Z.; Xie, Y.; Lu, Y.; Chen, S.; Bian, Q.; Guo, Y.; Shen, L.; Wu, J.; Zhou, B.; Hou, T.; He, Q.; Che, J.*; Dong, X.* TransFoxMol: predicting molecular property with focused attention. Brief Bioinform 2023, 24(5).

107. Rao, Z.; Li, K.; Hong, J.; Chen, D.; Ding, B.; Jiang, L.; Qi, X.; Hu, J.; Yang, B.; He, Q.; Dong, X.; Cao, J.*; Zhu, CL.* A practical "pre TACs-cytoblot” platform accelerates the streamlined development of PROTAC-based protein degraders. Eur J Med Chem 2023, 251, 115248.

106. Chen, S.; Gao, J.; Chen, J.; Xie, Y.; Shen, Z.; Xu, L.; Che, J.*; Wu, J.*; Dong, X.* ClusterX: a novel representation learning-based deep clustering framework for accurate visual inspection in virtual screening. Brief Bioinform 2023, 24(3), bbad126.

105. Bing, S.; Xiang, S.; Xia, Z.; Wang, Y.; Guan, Z.; Che, J.; Xu, A.; Dong, X.; Cao, J.; Yang, B.; Wang, J.*; He, Q.*; Ying, M.* Akt inhibitor Hu7691 induces differentiation of neuroblastoma cells. Acta Pharm Sin B 2023,13(4), 1522-1536.

104. Che, J.; Bing, S.; Lu, J.; Jin, Z.; Gao, J.; Sheng, H.; Li, D.; Yang, B.; He, Q.; Ying, M.*; Dong, X.* Discovery of Novel Oxazepine Derivatives as Akt/ROCK Inhibitiors for Growth Arrest and Differentiation Induction in Neuroblastoma Treatment. J Med Chem 2023, 66(19), 13530-13555.

103. Li, L.; Guo, Y.; Lu, Y.; Xu,Y.; Lu, Y.; Zhu, X.; Dong, X.; Che, J.* An updated patent review of AKT inhibitors(2020-present). Expert Opin Ther Pat 2023, 1-16.

102. Lu, J.; Guo, Y.; Hao, H.; Ma, J.; Lu, Y.; Sun, Y.; Shi, Z.; Dong, X.; Zhang, B.*; Fang, L.*; Che, J.* Targeted delivery of cathepsin-activatable near-infrared flurescenece probe for ultrahigh specific imaging of peritoneal metastasis. Eur J Med Chem 2023, 262, 115909.

2022:

101. Che J, Li D, Hong W, Wang L, Guo Y, Wu M, Lu J, Tong L, Weng Q, Wang J, Dong X. Discovery of new macrophage M2 polarization modulators as multiple sclerosis treatment agents that enable the inflammation microenvironment remodeling European journal of medicinal chemistry 2022, 243: 114732.

100. Luo M, Xu Y, Chen H, Wu Y, Pang A, Hu J, Dong X, Che J, Yang H. Advances of targeting the YAP/TAZ-TEAD complex in the hippo pathway for the treatment of cancers. European journal of medicinal chemistry 2022, 114847.

99. Zhuang Y, Che J, Wu M, Guo Y, Xu Y, Dong X, Yang H. Altered pathways and targeted therapy in double hit lymphoma. Journal of Hematology and Oncology 2022 15(1): 1-38.

98. Niu, T.; Li, K.; Jiang, L.; Zhou, Z.; Hong, J.; Chen, X.; Dong, X.; He, Q.; Cao, J.; Yang, B.*, Zhu C. L*. Noncovalent CDK12/13 dual inhibitors-based PROTACs degrade CDK12-Cyclin K complex and induce synthetic lethality with PARP inhibitor. European journal of medicinal chemistry 2022, 228, 114012.

97. Pan, C.; Luo, M.; Lu, Y.; Pan, X.; Chen, X.; Ding, L.; Che, J.*; He, Q.*; Dong, X.* Design, synthesis and biological evaluation of new dihydropyridine derivatives as PD-L1 degraders for enhancing antitumor immunity. Bioorganic chemistry 2022, 125, 105820.

96. Zhang, J.; Che, J.; Luo, X.; Wu, M.; Kan, W.; Jin, Y.; Wang, H.; Pang, A.; Li, C.; Huang, W. ;Zeng S. X.; Zhuang W. H.; Wu Y. Z.; Xu Y. J.;Zhou Y. B.*; Li J.*;Dong X.*;Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton’s Tyrosine Kinase for the Treatment of Lymphoma. Journal of medicinal chemistry 2022.

95. Zhu, C. L.; Luo, X.; Tian, T.; Rao, Z.; Wang, H.; Zhou, Z.; Mi, T.; Chen, D.; Xu, Y.; Wu Y.; Che J. X.;Zhou Y. B.; Li J.; Dong, X.*Structure-based rational design enables efficient discovery of a new selective and potent AKT PROTAC degrader. European journal of medicinal chemistry 2022, 238 (5), 114459.

94. Qu, B. #; Xu, Y. #; Lu, Y.; Zhuang, W.; Jin, X.; Shi, Q.; Yan, S.; Guo, Y.; Shen, Z.; Che, J.; Wu, Y.; Tong, L.; Dong, X.*; Yang, H.* Design, synthesis and biological evaluation of sulfonamides inhibitors of XPO1 displaying activity against multiple myeloma cells. European journal of medicinal chemistry 2022, 235, 114257.

93. Nie, W. #; Lu, Y. #; Pan, C.; Gao, J.; Luo, M.; Du, J.; Wang, J.; Luo, P.; Zhu, H.; Che, J.*; He, Q.*; Dong, X.* Design, synthesis, and biological evaluation of quinazoline derivatives with covalent reversible warheads as potential FGFR4 inhibitors. Bioorganic Chemistry 2022, 121, 105673. 

2021:   

92. Che, J. X.; Jin, Z. G.; Yan, F. J.; You, J. Q.; Xie, J. F.; Chen, B. H.; Cheng, G.; Zhu, H.; He, Q. J.; Hu, Y. Z.;Yang, B;Cao J*;Dong, X.* et al. Discovery of 5,6-Bis(4-methoxy-3-methylphenyl)pyridin-2-amine as a WSB1 Degrader to Inhibit Cancer Cell Metastasis. Journal of medicinal chemistry 2021, 64 (12), 8621-8643.

91. Pan, C.; Yang, H.; Lu, Y.; Hu, S.; Wu, Y.; He, Q.*; Dong, X.* Recent advance of peptide-based molecules and nonpeptidic small-molecules modulating PD-1/PD-L1 protein-protein interaction or targeting PD-L1 protein degradation. European journal of medicinal chemistry 2021, 213, 113170.

90. Weng, G.; Shen, C.; Cao, D.; Gao, J.; Dong, X.; He, Q.; Yang, B.; Li, D.*; Wu, J.*; Hou, T.* PROTAC-DB: an online database of PROTACs. Nucleic Acids Research 2021, 49 (D1), D1381-D1387.

89. Hu, S.; Liu, J.; Chen, S.; Gao, J.; Zhou, Y.; Liu, T.; Dong, X*. Discover Novel Covalent Inhibitors Targeting FLT3 through Hybrid Virtual Screening Strategy. Biological Pharmaceutical Bulletin 2021, 44 (12), 1872–1877.

88. Jin, Y. #; Zhuang, Y. #; Liu, M.; Che, J. *; Dong, X. * Inhibiting ferroptosis: A novel approach for stroke therapeutics. Drug Discovery Today 2021, 26, 916-930.

87. Che, J.#; Dai, X.#; Gao, J.; Sheng, H.; Zhan, W.; Lu, Y.; Li, D.; Gao, Z.; Jin, Z.; Chen, B.; Luo, P.; Yang, B.; Hu, Y.; He, Q.; Weng, Q.*; Dong, X.* Discovery of N-((3S,4S)-4-(3,4-Difluorophenyl)piperidin-3-yl)-2-fluoro-4-(1-methyl-1H-pyrazol- 5-yl)benzamide (Hu7691), a Potent and Selective Akt Inhibitor That Enables Decrease of Cutaneous Toxicity. Journal of medicinal chemistry 2021, 64, 12163-12180.  

86. Guo, Y.; Jin, Y.; Qu, B.; Zhang, Y.; Che, J.*; Dong, X.* An updated patent review of Akt inhibitors (2016-present). Expert Opin Ther Pat 2021, 31, 837-849

85. Zhang, J. #; Zhang, Y. #; Qu, B.; Yang, H.; Hu, S.*; Dong, X.* If small molecules immunotherapy comes, can the prime be far behind? European journal of medicinal chemistry 2021, 218, 113356.

84. Pan, C. #; Nie, W. #; Wang, J.; Du, J.; Pan, Z.; Gao, J.; Lu, Y.; Che, J.; Zhu, H.; Dai, H.; Chen, B.*; He, Q.*; Dong, X.* Design, synthesis and biological evaluation of quinazoline derivatives as potent and selective FGFR4 inhibitors.European journal of medicinal chemistry 2021, 225, 113794.

83. Pan, C.; Yang, H.; Lu, Y.; Hu, S.; Wu, Y.; He, Q.*; Dong, X.* Recent advance of peptide-based molecules and nonpeptidic small-molecules modulating PD-1/PD-L1 protein-protein interaction or targeting PD-L1 protein degradation. European journal of medicinal chemistry 2021, 213, 113170.

82. Che, J.; Wang, Z.; Shen, Z.; Zhuang, W.; Ying, H.; Hu, Y.; Hu, Y.*; Xie, X.*; Dong, X.* Discovery of 1,5-Dihydro-4H-imidazol-4-one Derivatives as Potent, Selective Antagonists of CXC Chemokine Receptor 2. ACS Medicinal Chemistry Letters 2021, 12, 836-845.

81. Huang, F. #; Tian, T. #; Wu, Y.; Che, J.; Yang, H.*; Dong, X.* Isocitrate Dehydrogenase 2 Inhibitors for the Treatment of Hematologic Malignancies: Advances and Future Opportunities. Mini Reviews Medicinal Chemistry 2021, 21, 1113-1122.

2020:

80. Che, J.;  Huang, F.;  Zhang, M.;  Xu, G.;  Qu, B.;  Gao, J.;  Chen, B.;  Zhang, J.;  Ying, H.;  Hu, Y.;  Hu, X.;  Zhou, Y.;  Gao, A.*;  Li, J.*; Dong, X*, Structure-based design, synthesis and bioactivity evaluation of macrocyclic inhibitors of mutant isocitrate dehydrogenase 2 (IDH2) displaying activity in acute myeloid leukemia cells. European journal of medicinal chemistry 2020, 203, 112491-112491.

79. Zhu, H.; Yan, F.; Yuan, T.; Qian, M.; Zhou, T.; Dai, X.; Cao, J.; Ying, M.; Dong, X.; He, Q.*; Yang, B.*, USP10 Promotes Proliferation of Hepatocellular Carcinoma by Deubiquitinating and Stabilizing YAP/TAZ. Cancer research 2020.

78. Yan, Y.-Y.; Shi, K.-y.; Teng, F.; Chen, J.; Che, J.-X.; Dong, X.-W.; Lin, N.-M.*; Zhang, B.*, A novel derivative of valepotriate inhibits the PI3K/AKT pathway and causes Noxa-dependent apoptosis in human pancreatic cancer cells. Acta Pharmacologica Sinica 2020.

77. Wang, B.; Yang, Y.; Lu, Y.; Wang, W.; Wang, Q.; Dong, X.; Zhao, J., Rapid and efficient removal of acetochlor from environmental water using Cr-MIL-101 sorbent modified with 3, 5-Bis(trifluoromethyl) phenyl isocyanate. Science Of the Total Environment 2020, 710.

76. Che, J.; Song, R.; Chen, B.*; Dong, X.*, Targeting CXCR1/2: The medicinal potential as cancer immunotherapy agents, antagonists research highlights and challenges ahead. European Journal Of Medicinal Chemistry 2020, 185.

2019:

75. Zhan, W.; Che, J.; Xu, L.; Wu, Y.; Hu, X.; Zhou, Y.; Cheng, G.; Hu, Y.; Dong, X.*; Li, J.*, fDiscovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors. European Journal Of Medicinal Chemistry 2019, 180, 72-85.

74. Zeng, C.; Zhu, D.; You, J.; Dong, X.; Yang, B.; Zhu, H.*; He, Q.*, Liquiritin, as a Natural Inhibitor o f AKR1C1, Could Interfere With the Progesterone Metabolism. Frontiers In Physiology 2019, 10.

73. Ye, Q.; Li, Q.; Gao, A.; Ying, H.; Cheng, G.; Chen, J.; Che, J.; Li, J.; Dong, X.*; Zhou, Y.*, Discovery of novel indoleaminopyrimidine NIK inhibitors based on molecular docking-based support vector regression (SVR) model. Chemical Physics Letters 2019, 718, 38-45.

72. Yang, Y.; Cheng, J.; Wang, B.; Guo, Y.; Dong, X.; Zhao, J.*, An amino-modified metal-organic framework (type UiO-66-NH2) loaded with cadmium(II) and lead(II) ions for simultaneous electrochemical immunosensing of triazophos and thiacloprid. Microchimica Acta 2019, 186 (2).

71.Yang, Y.; Che, J.; Wang, B.; Wu, Y.; Chen, B.; Gao, L.; Dong, X.*; Zhao, J.*, Visible-light-mediated guest trapping in a photosensitizing porous coordination network: metal-free C-C bond-forming modification of metal-organic frameworks for aqueous-phase herbicide adsorption. Chemical Communications 2019, 55 (37), 5383-5386.

70. Weng, Q.; Che, J.; Zhang, Z.; Zheng, J.; Zhan, W.; Ling, S.; Tian, T.; Wang, J.; Gai, R.; Hu, Y.; Yang, B.; He, Q.; Dong, X.*, Phenotypic Screening-Based Identification of 3,4-Disubstituted Piperidine Derivatives as Macrophage M2 Polarization Modulators: An Opportunity for Treating Multiple Sclerosis. Journal Of Medicinal Chemistry 2019, 62 (7), 3268-3285.

69.Hu, C.*; Dong, X.*, Cysteine-targeted Irreversible Inhibitors of Tyrosine Kinases and Key Interactions. Current Medicinal Chemistry 2019, 26 (31), 5811-5824.

68. Guo, R.; Huang, F.; Zhang, B.; Yan, Y.; Che, J.; Jin, Y.; Zhuang, Y.; Dong, R.; Li, Y.; Tan, B.; Song, R.; Hu, Y.; Dong, X.*; Li, X.*; Lin, N.*, GSH Activated Biotin-tagged Near-Infrared Probe for Efficient Cancer Imaging. Theranostics 2019, 9 (12), 3515-3525.

67.Dong, X.-W.; Zhang, J.-K.; Xu, L.; Che, J.-X.; Cheng, G.; Hu, X.-B.; Sheng, L.; Gao, A.-H.; Li, J.; Liu, T.; Hu*, Y.-Z.; Zhou*, Y.-B.*, Covalent docking modelling-based discovery of tripeptidyl epoxyketone proteasome inhibitors composed of aliphatic-heterocycles. European Journal Of Medicinal Chemistry 2019, 164, 602-614.

66. Dong, X.; Zhan, W.; Zhao, M.; Che, J.; Dai, X.; Wu, Y.; Xu, L.; Zhou, Y.; Zhao, Y.; Tian, T.; Chen, G.; Jin, Z.; Li, J.; Shao, Y.; He, Q.; Yang, B.; Weng, Q.*; Hu, Y.*, Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design. Journal Of Medicinal Chemistry 2019, 62 (15), 7264-7288.

65. Cheng, G.; Mei, X.-B.; Yan, Y.-Y.; Chen, J.; Zhang, B.; Li, J.; Dong, X.-W.*; Lin, N.-M.*; Zhou, Y.-B.*, Identification of new NIK inhibitors by discriminatory analysis-based molecular docking and biological evaluation. Archiv Der Pharmazie 2019, 352 (7).

2018:

64. X.-X. Bai, L. Yan, C.-Y. Ji, Q. Zhang, X.-W. Dong*, A. Chen*, M.-R. Zhao*, A combination of ternary classification models and reporter gene assays for the comprehensive thyroid hormone disruption profiles of 209 polychlorinated biphenyls. Chemosphere, 2018, 210, 312-319. 

63. D.-Q. Li, X.-T. Zhang, X.-D. Ma, L. Xu, J.-J. Yu, L.-X. Gao, X.-B. Hu, J.-K. Zhang, X.-W. Dong, J. Li, T. Liu*, Y.-B. Zhou*, Y.- Z. Hu*, Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors. J. Med. Chem., 2018, 61, 20, 9177-9204.  

62. X.-W. Dong*, Y. Yang, J.-X. Che, J. Zuo, X.-H. Li, L. Gao, Y.-Z. Hu, X.-Y. Liu*, Heterogenization of homogeneous chiralpolymers in metal-organic frameworks with enhanced catalytic performance for asymmetric catalysis. Green. Chem., 2018, 20, 17, 4085-4093.  

61. J. Wei, D.-Y. Gu, S.-D. Wang, J.-B. Hu, X.-W. Dong, R. Sheng*, Visible-light-mediated radical arylthiodifluoromethylation of isocyanides with fluorinated 2-pyridyl sulfones. Org. Chem. Front., 2018, 5, 17, 2568-2572. 

60. L. Yan, Q. Zhang, F. Huang, W.-W. Nie, C.-Q. Hu*, H.-Z. Ying, X.-W. Dong*, M.-R. Zhao*, Ternary classification models for predicting hormonal activities of chemicals via nuclear receptors. Chem. Phys. Lett., 2018, 706, 360-366.  

58. J.-H. Zhao, Y. Yang, J.-X. Che, J. Zuo, X.-H. Li, Y.-Z. Hu*, X.-W. Dong*, L. Gao*, X.-Y. Liu*, Compartmentalization of Incompatible Polymers within Metal-Organic Frameworks towards Homogenization of Heterogeneous Hybrid Catalysts for  Tandem Reactions. Chem.-Eur. J., 2018. 24, 39, 9903-9909. 

57. J.-X. Che, Z.-L. Wang, H.-C. Sheng, F. Huang, X.-W. Dong, Y.-H. Hu, X. Xie, Y.-Z. Hu*, Ligand-based pharmacophoremodel for the discovery of novel CXCR2 antagonists as anti-cancer metastatic agents. Roy. Soc. Open. Sci., 2018, 5, 7.

56. Y.-Z. Wu*, H.-Z. Ying, L. Xu, G. Cheng, J. Chen, H.-Y. Hu, T. Liu*, X.-W. Dong*, Design, synthesis, and molecular docking   study of 3H-imidazole[4,5-c]pyridine derivatives as CDK2 inhibitors. Arch. Pharm., 2018, 351, 6.

55. Z. Wang, Y. Kang, D. Li, H.-Y. Sun, X.-W. Dong, X.-J. Yao, L. Xu, S. Chang, Y.-Y. Li, T.-J. Hou, Benchmark Study Based on 2P2I(DB) to Gain Insights into the Discovery of Small-Molecule PPI Inhibitors. J. Phys. Chem. B., 2018, 122, 9, 2544-2555. 

54. L.-L. Shao, X.-L. Wang, K. Chen, X.-W. Dong, L.-M. Kong, D.-Y. Zhao, Robert C. Hider, T. Zhou, Novel hydroxypyridinone derivatives containing an oxime ether moiety: Synthesis, inhibition on mushroom tyrosinase and application in antibrowning of fresh-cut apples. Food. Chem., 2018, 242, 174-181.  

53. J.-X. Che, Z.-L. Wang, X.-W. Dong, Y.-H. Hu, X. Xie, Y.-Z. Hu*, Bicyclo[2.2.1]heptane containing N,N-diarylsquaramide CXCR2 selective antagonists as anti-cancer metastasis agents. RSC. Adv., 2018, 8, 20, 11061-11069.  

2017:

52. C.-L. Ma,  J.-H. Zhao, Y. Yang, Y; M.K. Zhang, C. Shen, R. Sheng*, X.-W. Dong*, Y.-Z. Hu*, A Copper-Catalyzed Tandem Cyclization Reaction of Aminoalkynes with Alkynes for the Construction of Tetrahydropyrrolo[1,2-a]quinolines Scaffold, 2017, 7, 16640. (IF, 4.259)

51. H.-Z. Ying, J.-F. Xie, X.-G. Liu, T.-T. Yao, X.-W. Dong*, C.-Q. Hu* Discriminatory analysis based molecular docking study for in silico identification of epigallocatechin-3-gallate (EGCG) derivatives as B-Raf V600E inhibitors. RSC Adv., 2017, 7, 44820– 44826.

50. B. Zhang, R.-Y. Guo,  Y.-Z. Hu,  X.-W. Dong,  N.-M. Lin,  X.-Y. Dai,  H.-H. Wu,  S.-L. Ma*, B. Yang* Design, synthesis and biological evaluation of valepotriate derivatives as novel antitumor agents. RSC Adv., 2017, 7, 31899–31906.

49. C.-Q. Hu, K. Li, T.-T. Yao, Y.-Z. Hu, H.-Z. Ying*, X.-W. Dong* Integrating docking scores and key interaction profiles to  improve the accuracy of molecular docking: towards novel B-Raf V600E inhibitors, Med. Chem. Commun., 2017, 8, 1835–1844.

48. Q. Zhang, L. Yan, Y. Wu, L. Ji, Y.C. Chen, M.R. Zhao*, X.-W. Dong*, A ternary classification using machine learning methods of distinct estrogen receptor activities within a large collection of  environmental chemicalsSci. Total Environ. 2017, 580, 1268-1275. 

47. T.-T. Yao, D.-X. Xiao, Z.-S. Li, J.-L. Cheng, S.-W. Fang, Y.-J. Du, J.-H. Zhao*, X.-W. Dong*, G.N. Zhu,Design, Synthesis, and Fungicidal Evaluation of Novel Pyrazole-furan and Pyrazole-pyrrole Carboxamide as Succinate Dehydrogenase Inhibitors, J. Agric. Food Chem. 2017, 65, 5397-5403. 

46. T.-T. Yao, S.-W. Fang,  Z.-S. Li, D.-X. Xiao, J.-L. Cheng, H.-Z. Ying, Y.-J. Du, J.-H. Zhao*, X.-W. Dong*, Discovery of novel succinate dehydrogenase inhibitors by the integration of in silico library design  and pharmacophore mapping. J. Agric. Food Chem. 2017, 65, 3204–3211.

45. T.-T. Yao, J.-F. Xie, X.-G. Liu, J.-L. Cheng, C.-Y. Zhu, J.-H. Zhao* and X.-W. Dong* Integration of pharmacophore mapping and molecular docking in sequential virtual screening: towards the discovery of novel JAK2 inhibitors, RSC Adv., 2017, 7,  10353–10360.

2016:

44. S.-Y. Wang, R. Jin, R.-Q. Wang, Y.-Z. Hu, X.-W. Dong*, and A.-E. Xu* The design, synthesis and biological evaluation of pro-EGCG derivatives as novel anti-vitiligo agents, RSC Adv., 2016, 6,106308–106315.

43. C.-L. Ma, X.-L. Yu, X.-L. Zhu, Y.-Z. Hu, X.-W. Dong*, B. Tan*, X.-Y. Liu* Gold-Catalyzed Tandem Synthesis of Bioactive Spiro-dipyrroloquinolines and Its Application in the One-step Synthesis of Incargranine B Aglycone and Seneciobipyrrolidine (I), Org. Chem. Front. 2016, 3, 324-329.

2015:

42. S.-J. Zhu, H.-Z. Ying, Y. Wu, N. Qiu, T. Liu, B. Yang, X.-W. Dong*, Y.-Z. Hu*, Design, Synthesis and Biological Evaluation of Novel Podophyllotoxin Derivatives Bearing 4β-Disulfide/trisulfide Bond as Cytotoxic Agents RSC advance 2015, 5, 103172-103183 (IF, 3.84).

41. X.-M. He, X.-W. Dong, D.-H. Zou, Y. Yu, Q.-Y. Fang,  Q. Zhang, M.-R. Zhao*,  Enantioselective Effects of o,p′-DDT on Cell Invasion and Adhesion of Breast Cancer Cells: Chirality in Cancer Development Environ. Sci. Technol. 2015, 49,10028-10037 (IF, 5.33).

40. W.-H. Zhan, S.-D. Lin, J. Chen, X.-W. Dong, J.-B. Chu, W.T. Du, Design, Synthesis, Biological Evaluation, and Molecular Docking of Novel Benzopyran and Phenylpyrazole Derivatives as Akt Inhibitors, Chem. Biol. Drug. Des. 2015, 85, 770–779 (IF, 2.50).

39. T.-T. Yao, J.-L. Cheng, B.-R. Xu, M.-Z. Zhang, G.-N. Zhu, Y.-z. Hu, J.-H. Zhao*, X.-W. Dong*, Support Vector Machine (SVM) Classification Model Based Rational Design of Novel Tetronic Acid Derivatives as Potent Insecticidal and Acaricidal Agents, RSC advance 2015, 5, 49195 - 49203 (IF, 3.84). 

38. C.-L. Ma, X.-L. Yu, X. Zhu, Y.-Z. Hu, Y. X.-W. Dong*, B. Tan*, X.-Y. Liu*, Platinum-Catalyzed Tandem Cyclization Reaction to Multiply Substituted Indolines under Microwave-Assisted Conditions. Adv. Synth. Catal. 2015, 357, (2), 569-575 (IF, 5.66).

 2014:

37. S. -W. Hu, Q. Gu, Z. Wang, Z. Weng, Y. Cai, X.-W. Dong, Y.-Z. Hu, T. Liu*, X. Xie*, Design, synthesis, and biological evaluation of novel piperidine-4-carboxamide derivatives as potent CCR5 inhibitors. Eur J Med Chem 2014, 71, 259-66 (IF, 3.45).

36. Q. Zhang, M. Lu, X.-W. Dong, C. Wang, C. Zhang, W.  Liu, M. Zhao*, Potential estrogenic effects of phosphorus-containing flame retardants. Environ. Sci. Technol., 2014, 48, 6995-7001 (IF, 5.33).

35. T. Liu, C.-X. Che, Y.-Z. Hu, X.-W. Dong*, X.-Y. Liu*, C.-M. Che, Alkenyl/Thiol-Derived Metal-Organic Frameworks (MOFs) by Means of Postsynthetic Modification for Effective Mercury Adsorption. Chem-Eur. J. 2014, 20, (43), 14090-5 (IF, 5.73).

34. T. Liu, D.-Q. Li, S.Y. Wang, Y.-Z. Hu, W.-W. Dong*, X.-Y. Liu*, C.M. Che, Straightforward installation of carbon-halogen, carbon-oxygen and carbon-carbon bonds within metal-organic frameworks (MOF) via palladium-catalysed direct C-H functionalization. Chem Commun (Camb) 2014, 50, (87), 13261-4 (IF, 6.83), Highlighted by synfacts.

33. W.-H. Zhan, D.-Q.Li, J.-X. Che, L. Zhang, B. Yang, Y.-Z. Hu, T. Liu, X.-W. Dong*, Integrating docking scores, interaction profiles and molecular descriptors to improve the accuracy of molecular docking: toward the discovery of novel Akt1 inhibitors. Eur J Med Chem 2014, 75, 11-20 (IF, 3.45).

32. T. Liu, T. W.-H. Zhan, Y.-M. Wang, L. Zhang, B. Yang, X.-W. Dong*, Y.-Z. Hu*, Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors. Eur J Med Chem 2014, 73, 167-76 (IF, 3.45).

2013:

31. X. -W. Dong, T. Liu, Y.-Z. Hu*, X.-Y. Liu, C. -M. Che, Urea postmodified in a metal-organic framework as a catalytically active hydrogen-bond-donating heterogeneous catalyst. Chem Commun (Camb) 2013, 49, (70), 7681-3 (IF, 6.83), inside cover picture, Highlighted by synfacts.

30. T. Liu, Z. Y. Weng, X.-W. Dong, L. Chen, L. Ma, S. Cen, N. Zhou, Y.-Z. Hu*, Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists. PLoS One 2013, 8, (1), e53636 (IF, 3.23).

29. X. –W. Dong, Y. M. Zhao, X.-Q. Huang, K. -N. Lin, J. Chen, E.-Q. Wei, T. Liu, Y.-Z. Hu, Structure-based drug design using GPCR homology modeling: Toward the discovery of novel selective CysLT2 antagonists. Eur J Med Chem 2013, 62, 754-63 (IF, 3.45).

2012:

28. X.-W. Dong, J.-Y. Yan, L.-L. Du, P. Wu, S.-F. Huang, T. Liu, Y.-Z. Hu*, Pharmacophore identification, docking and "in silico" screening for novel CDK1 inhibitors. J Mol Graph Model 2012, 37, 77-86 (1.72).

27. X.-W. Dong; J.-Y. Yan, D. Lu, P. Wu, J.-D. Gao, T. Liu, B. Yang, Y.-Z. Hu*, QSAR models for isoindolinone-based p53-MDM2 interaction inhibitors using linear and non-linear statistical methods. Chem Biol Drug Des 2012, 79, (5), 691-702 (IF, 2.50).

26.  S. -F. Huang, Y. M. Zhao, X.-L. Zhou, Y. -Z. Wu, P. Wu, T. Liu, B. Yang, Y.-Z. Hu, X. -W. Dong*, Design, synthesis and biological evaluation of 3-benzylideneflavanone derivatives as cytotoxic agents. Med Chem Res 2012, 21, (12), 4150-4157 (IF, 1.40).

25. Z. Y. Weng, W. Wei, X.-W. Dong, Y.-Z. Hu, S. -F. Huang, T. Liu*, X. Xie, Synthesis and biological evaluation of novel piperidin-4-ol derivatives. Monatsh Chem 2012, 143, (2), 303-308 (IF, 1.22).

24. P. Wu, Y. Su, X. Guan, X.-W. Liu, J. Zhang, X.-W. Dong, W.-H. Huang, Y.-Z. Hu, Identification of novel piperazinylquinoxaline derivatives as potent phosphoinositide 3-kinase (PI3K) inhibitors. PLoS One 2012, 7, (8), e43171 (IF, 3.23).

23. P. Wu, Y. Su, X.-W. Liu, J.-Y. Yan, Y. Ye, L. Zhang, J. -C. Xu, S.-Y. Weng, Y. N. Li, T. Liu, X.-W. Dong, M. T. Sun, B. Yang, Q. J. He, Y. –Z. Hu*, Discovery of novel morpholino-quinoxalines as PI3K alpha inhibitors by pharmacophore-based screening. Medchemcomm 2012, 3, (6), 659-662 (IF, 2.45). 

2011:

22. X.-W. Dong, Y. Wang, T. Liu, P. Wu, J.-D. Gao, J. Xu, B. Yang, Y.-Z. Hu*,      Flavonoids as vasorelaxant agents: synthesis, biological evaluation and      quantitative structure activities relationship (QSAR) studies. Molecules 2011, 16, 8257-72 (IF, 2.42).

21. X.-W. Dong, X.-L. Zhou, H. Jing, J. Chen, T. Liu, B. Yang, Q.-J. He, Y.-Z. Hu*,      Pharmacophore identification, virtual screening and biological evaluation      of prenylated flavonoids derivatives as PKB/Akt1 inhibitors. Eur. J.      Med. Chem. 2011, 46,      5949-58 (IF, 3.45).

20. C. -Q. Hu, X. Li, W. Wang, L. Zhang, L. Tao, X.-W. Dong, R. Sheng, B. Yang, Y.-Z Hu,*, Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. Bioorg Med Chem 2011, 19, 5454-61 (IF, 2.79).

19. C. Zhang, T.-Y. Cai, H. Zhu, L.-Q. Yang, H. Jiang, X.-W. Dong, Y.-Z. Hu, N. -M. Lin, Q.-J. He, B. Yang, Synergistic antitumor activity of gemcitabine and ABT-737 in vitro and in vivo through disrupting the interaction of USP9X and Mcl-1. Mol Cancer Ther 2011, 10, 1264-75 (IF, 5.68).

18. J. Chen, T. Liu, R. Wu, J.-S. Lou, X.-W. Dong, Q. -J. He, B. Yang, Y.-Z. Hu, Design, synthesis, and biological      evaluation of novel gamma-carboline ketones as anticancer agents. Eur. J. Med. Chem. 2011, 46, 1343-1347 (IF, 3.45).

2010:

17. X.-W. Dong, L. Wang, X.-Q. Huang, T. Liu, E.-Q. Wei, L.-L. Du, B. Yang, Y.-Z. Hu*, Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists, Bioorg. Med. Chem. 2010, 18, 5519-5527 (IF, 2.79).

16. H. Jing, X.-L. Zhou, X.-W. Dong, J. Cao, H. Zhu, J. Shu, Y.-Z. Hu, Q.-J. He, B. Yang, Abrogation of Akt signaling by Isobavachalcone contributes to its anti-proliferative effects towards human cancer cells. Cancer Lett. 2010, 294, 167-177 (IF, 5.62).

15. X.-W. Dong, L.-L. Du, Z.-C. Pan, T. Liu, B. Yang, Y.-Z. Hu* Synthesis and biological evaluation of novel hybrid chalcone derivatives as vasorelaxant agents  Eur. J. Med. Chem.  2010, 45, 3986-3992 (IF, 3.45).

2009:

14. X.-W. Dong, T. Liu, J.-Y. Yan, P. Wu, J. Chen, Y.-Z. Hu*, Synthesis, Biological Evaluation and Quantitative Structure-Activities Relationship of Flavonoids as Vasorelaxant Agents. Bioorg. Med. Chem. 2009, 17, 716-726 (IF, 2.79). 

13. X.-W. Dong, L.-L Qi, C.-Y. Jiang, J. Chen, E.-Q. Wei, Y.-Z. Hu*, Synthesis, Biological Evaluation of Prenylflavonoids as Vasorelaxant and Neuroprotective Agents. Bioorg. Med. Chem. Lett. 2009, 19, 3196-3198 (2.42).

12. X.-W. Dong, C.-Y. Jiang, H.-Y. Hu, J.-Y. Yan, J. Chen, Y.-Z. Hu*, QSAR Study of Akt/Protein Kinase B (PKB) Inhibitors Using Support Vector Machine. Eur. J. Med. Chem. 2009, 44, 4090-4097 (IF, 3.45).

11. X.-W. Dong, T. Liu, Y.-P. Gao, J. Chen, Y.-Z. Hu*, One-pot Synthesis of 3-Benzylflavones, Synth. Commun. 2009, 39, 7-742.

10. X.-W. Dong, T. Liu, J. Chen, H.-Z. Ying, Y.-Z. Hu*, Microwave-Assisted Mannich Reaction of 2-Hydroxy-Chalcones, Synth. Commun. 2009, 39, 733-742. 

9. X.-W. Dong, J. Chen, C.-Y. Jiang, T. Liu, Y.-Z. Hu*, Design, Synthesis and Biological Evaluation of Prenylated Chalcones as Vasorelaxant Agents, Arch. Pharm. 2009, 342, 428-432

8. J. Chen, X.-W. Dong, T. Liu, J.-S. Lou, C.-Y. Jiang, W.-H. Huang, Q.-J. He, B. Yang, Y.-Z. Hu*, Design, Synthesis, and Quantitative Structure-Activitiy Relationship of Cytotoxic γ-Carboline Derivatives, Bioorg. Med. Chem. 2009, 17, 3324-3331 (IF, 2.79). 

7. J. Chen, T. Liu, X.-W. Dong, Y.-Z. Hu*. Recent development of colchicine binding site inhibitors. Mini-Reviews in Medicinal Chemistry, 2009, 9 (10), 1174-1190 (IF, 2.90).

6. Y.-H. Shen, J. Zhang, R. Sheng, X.-W. Dong, Q.-J. He, B. Yang, Y.-Z. Hu*, Synthesis and biological evaluation of novel flavonoids derivatives as dual binding acetylcholinesterase inhibitors. J. Enzyme Inhib. Med. Chem., 2009, 24, 372-380.

5. J. Chen, J.-S. Lou, T. Liu, R. Wu, X.-W. Dong, Q.-J. He, B. Yang, Y.-Z. Hu*, Synthesis and in-vitro Antitumor Activities of some Mannich Bases of 9-Alkyl-1,2,3,4-Tetrahydrocarbazole-1-ones. Arch. Pharm. 2009, 342, 3165-172. 

4. T. Liu, X.-W. Dong, N. Xue, R. Wu, Q.-J. He, B. Yang, Y.-Z. Hu*, Synthesis and biological evaluation of 3,4-diaryl-5-aminoisoxazole derivatives. Bioorg. Med. Chem. 2009, 17, 6279 – 6285 (IF, 2.79).

3. T. Liu , M.-T. Sun, X.-W Dong, X. Ren, X. Yang, L.-L Du, Y.-Z. Hu*, Structure-Based Drug Design, Synthesis and Antitumor Activities of Novel CDK7 Inhibitors. Acta. Physico-chimica Sinica, 2009, 25 (10), 2107-2112.

2008:

2. X.-W Dong, Y.-J. Liu, J.-Y. Yan, C.-Y. Jiang, J. Chen, T. Liu, Y.-Z. Hu*, Identification of SVM-based classification model, synthesis and evaluation of prenylated flavonoids as vasorelaxant agents, Bioorg. Med. Chem. 2008, 16, 8151-8160 (IF, 2.79).

2007:

1. X.-W Dong, Y.-J. Fan, L.-J. Yu, Y.-Z. Hu*, Synthesis of Four Natural Prenylflavonoids and their Estrogen-like activities. Arch Pharm. 2007, 340, 372-376.

 

研究生带教情况

培养硕士,博士数十明,毕业后均进入国内外知名高校,药企等单位工作

 

最后更新时间:2025-04-25