RECENT NEWS

  • Sep 2017
    We just published a new paper on J. Med. Chem. reporting a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML. doi: 10.1021/acs.jmedchem.7b00840.
  • Aug 2017
    We just published a new paper on Eur. J. Med. Chem. reporting a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR associated drug resistant mutants in NSCLC. doi: 10.1016/j.ejmech.2017.08.035.
  • Jun 2017
    We just published a new paper on Eur. J. Med. Chem. reporting structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors. doi: 10.1016/j.ejmech.2017.06.016.
  • Mar 2017
    We just published a new paper on Scientific Reports reporting a Novel Irreversible BTK Kinase Inhibitor. doi: 10.1038/s41598-017-00482-4
  • Mar 2017
    We just published a new paper on J. Med. Chem. reporting a Novel Irreversible EGFR Mutants Kinase Inhibitor with a Distinct Binding Mode.
    doi: 10.1021/acs.jmedchem.6b01907
  • Mar 2017
    We just published a new paper on Eur. J. Med. Chem. reporting a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor. doi: 10.1016/j.ejmech.2017.03.001
  • Feb 2017
    We just published a new paper on Oncotarget reporting a highly selective irreversible EGFR inhibitor. doi: 10.18632/oncotarget.15443
  • Jan 2017
    We just published a new paper on J. Med. Chem. reporting a a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor. doi: 10.1021/acs.jmedchem.6b01413

RECENT PUBLICATIONS

89. Hua Jiang#, Hongbin He, Yun Chen, Wei Huang, Jinbo Cheng, Jin Ye, Aoli Wang, Jinhui Tao, Chao Wang, Qingsong Liu, Tengchuan Jin, Wei Jiang, Xianming Deng, Rongbin Zhou*. Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders. J Exp Med. 2017 Oct 11. doi: 10.1084/jem.20171419. [Epub ahead of print]

88. Aoli Wang#, Xixiang Li#, Cheng Chen#, Hong Wu#, Ziping Qi#, Chen Hu#, Kailin Yu, Jiaxin Wu, Juan Liu, Xiaochuan Liu, Zhenquan Hu, Wei Wang, Wenliang Wang, Wenchao Wang, Li Wang, Beilei Wang, Qingwang Liu, Lili Li, Jian Ge, Tao Ren, Shanchun Zhang, Ruixiang Xia*, Jing Liu*, and Qingsong Liu*. Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d] pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML. J. Med. Chem. 2017 Sep 28. doi: 10.1021/acs.jmedchem.7b00840. [Epub ahead of print]

87. Yongfei Chen#, Jiaxin Wu#, Aoli Wang#, Ziping Qi#, Taoshan Jiang#, Cheng Chen, Fengming Zou, Chen Hu, Wei Wang, Hong Wu, Zhenquan Hu, Wenchao Wang, Beilei Wang, Li Wang, Tao Ren, Shanchun Zhang, Qingsong Liu*, Jing Liu*. Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR associated drug resistant mutants in NSCLC. Eur J Med Chem. 2017 Aug 18;139:674-697. doi: 10.1016/j.ejmech.2017.08.035. [Epub ahead of print]

86. Kwok-Kin Wong, Yan Liu, Yuyang Li, Xiaoen Wang, Feiyang Liu, Peng Gao, Max M. Quinn, Fei Li, Ashley A. Merlino, Cyril H. Benes, Qingsong Liu and Nathanael S. Gray. Gemcitabine and Chk1 inhibitor AZD7762 synergistically suppress the growth of Lkb1-deficient lung adenocarcinoma. Cancer Res. 2017,Jul 28. pii: canres.0567.2017. doi: 10.1158/0008-5472.CAN-17-0567. [Epub ahead of print]

85. Beilei Wang#, Yuanxin Deng#, Yongfei Chen#, Kailin Yu, Aoli Wang, Qianmao Liang, Wei Wang, Cheng Chen, Hong Wu, Chen Hu, Weili Miao, Wooyoung Hur, Wenchao Wang, Zhenquan Hu, Ellen L. Weisberg, Jinhua Wang, Tao Ren, Yinsheng Wang, Nathanael S. Gray, Qingsong Liu*, Jing Liu*. Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors. Eur. J. Med. Chem. 2017,Available online 9 June 2017. doi: 10.1016/j.ejmech.2017.06.016. [Epub ahead of print]

84. Tao Hu#, Xiaoxue Yuan#, Rongcai Ye#, Huiqiao Zhoua, Jun Lina, Chuanhai Zhang, Hanlin Zhang, Gang Wei, Meng Dong, Yuanyuan Huang, Wonchung Lime, Qingsong Liu, Hyuek Jong Lee*, Wanzhu Jin*. Brown adipose tissue activation by rutin ameliorates polycystic ovary syndrome in rat. J Nutr Biochem. 2017, Apr 22; 47: 21-28. doi: 10.1016/j.jnutbio.2017.04.012. [Epub ahead of print]

83. Chen Hu#, Aoli Wang#, Hong Wu#, Ziping Qi#, Xixiang Li#, Xiao-E Yan#, Cheng Chen, Kailin Yu, Fengming Zou, Wenchao Wang, Wei Wang, Jiaxin Wu, Juan Liu, Beilei Wang, Li Wang, Tao Ren, Shanchun Zhang, Cai-Hong Yun*, Jing Liu*, Qingsong Liu.* Discovery and characterization of a novel irreversible EGFR mutants selective and potent kinase inhibitor CHMFL-EGFR-26 with a distinct binding mode. Oncotarget 2017, 8(11): 18359-18372. doi: 10.18632/oncotarget.15443

82. Zheng Zhao, Qingsong Liu, Spencer Bliven, Lei Xie*, Philip E. Bourne*. Determining cysteines available for covalent inhibition across the human kinome. J. Med. Chem. 2017. doi: 10.1021/acs.jmedchem.6b01815

81. Hong Wu#, Qiong Huang#, Ziping Qi#, Yongfei Chen#, Aoli Wang, Cheng Chen, Qianmao Liang, Jinghua Wang, Wensheng Chen, Jin Dong, Kailin Yu, Chen Hu, Wenchao Wang, Xiaochuan Liu, Xiaoxiang Li, Nathanael S. Gray, Jing Liu*, Wei Wei*, Qingsong Liu*. Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model. Scientific Reports 2017, doi: 10.1038/s41598-017-00482-4

80. Aoli Wang#, Xixiang Li#, Hong Wu#, Fengming Zou#, Xiao-E Yan#, Cheng Chen, Chen Hu, Kailin Yu, Wenchao Wang, Peng Zhao, Jiaxin Wu, Ziping Qi, Wei Wang, Beilei Wang, Li Wang, Tao Ren, Shanchun Zhang, Cai-Hong Yun*, Jing Liu*, Qingsong Liu*. Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy) phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutants Kinase Inhibitor with a Distinct Binding Mode. J. Med. Chem. 2017. 10.1021/acs.jmedchem.6b01907

79. Juanjuan Liu, Xingxing Yang, Binhua Li, Junjun Wang, Wenchao Wang, Jing Liu, Qingsong Liu, Xin Zhang*. STK16 regulates actin dynamics to control Golgi organization and cell cycle. Scientific Reports 2017, 7: 44607. doi: 10.1038/srep44607.

78. Qianmao Liang#, Yongfei Chen#, Kailin Yu#, Cheng Chen#, Shouxiang Zhang, Aoli Wang, Wei Wang, Hong Wu, Xiaochuan Liu, Beilei Wang, Li Wang, Zhenquan Hu, Wenchao Wang, Tao Ren, Shanchun Zhang, Qingsong Liu*, Cai-Hong Yun*, Jing Liu*. Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor. Eur. J. Med. Chem. 2017, 131: 107-125. doi: 10.1016/j.ejmech.2017.03.001.

77. Yanke Liang, Melissanne De Wispelaere, Margot Carocci, Qingsong Liu, Jinhua Wang, Priscilla L. Yang*, Nathanael S Gray*. Structure-Activity Relationship study of QL47 - a Broad-spectrum Antiviral agent. ACS Med. Chem. Lett. 2017, 8: 344-349. doi: 10.1021/acsmedchemlett.7b00008.

76. Xiaofei Liang#, Fengchao Lv#, Beilei Wang#, Kailin Yu#, Hong Wu, Ziping Qi, Zongru Jiang, Cheng Chen, Aoli Wang, Weili Miao, Wenchao Wang, Zhenquan Hu, Juan Liu, Xiaochuan Liu, Zheng Zhao, Li Wang, Shanchun Zhang, Zi Ye, Chu Wang, Tao Ren, Yinsheng Wang, Qingsong Liu*, and Jing Liu*. Discovery of 2-((3-acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor. J. Med. Chem. 2017, 60(5):1793-1816. doi: 10.1021/acs.jmedchem.6b01413.

75. Wu R, Sun JG, Wang JQ, Li B, Qingsong Liu, Ning G, Jin W, Yuan Z*. c-Abl inhibition mitigates diet-induced obesity through improving insulin sensitivity of subcutaneous fat in mice. Diabetologia 2017, Jan 10. doi: 10.1007/s00125-016-4202-2.

74. Yifei Yang, Yuan Zhang, LingYun Yang, Leilei Zhao, Lianghui Si, Huibin Zhang, Qingsong Liu, Jinpei Zhou*. Discovery of imidazopyridine derivatives as novel c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. Bioorg. Chem. 2017, 70:126-132. doi: 10.1016/j.bioorg.2016.12.002.

73. de Wispelaere M, Carocci M, Liang Y, Qingsong Liu, Sun E, Vetter ML, Wang J, Gray NS, Yang PL.Discovery of host-targeted covalent inhibitors of dengue virus. Antiviral Res. 2017, 139: 171-179. doi: 10.1016/j.antiviral.2016.12.017.

72. Qiang Wang#, Feiyang Liu#, Beilei Wang#, Fengming Zou#, Ziping Qi, Cheng Chen, Kailin Yu, Chen Hu, Shuang Qi, Wenchao Wang, Zhenquan Hu, Juan Liu, Wei Wang, Li Wang, Qianmao Liang, Shanchun Zhang, Tao Ren, Qingsong Liu*,Jing Liu*. Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl) phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. J. Med. Chem. 2017, 60(1): 273-289. doi: 10.1021/acs.jmedchem.6b01290.

71. Xiaoxue Yuan#, Gang Wei#, Yilin You#,Yuanyuan Huang, Hyuek Jong Lee,Meng Dong, Jun Lin, Tao Hu, Hanlin Zhang,Chuanhai Zhang, Huiqiao Zhou,Rongcai Ye, Xiaolong Qi, Baiqiang Zhai,Weidong Huang,Shunai Liu,Wen Xie, Qingsong Liu, Xiaomeng Liu,Chengbi Cui,Donghao Li,Jicheng Zhan,Jun Cheng,Zengqiang Yuan, Wanzhu Jin. Rutin ameliorates obesity through brown fat activation. FASEB J. 2017, 31(1): 333-345. doi: 10.1096/fj.201600459RR.