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 irrevers:(发现n -(3 -(5 -((3-acrylamido-4 -(morphol).pdfVIP
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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 irrevers:(发现n -(3 -(5 -((3-acrylamido-4 -(morphol)
European Journal of Medicinal Chemistry 131 (2017) 107e125
Contents lists available at ScienceDirect
European Journal of Medicinal Chemistry
journal homepage: /locate/ejmech
Research paper
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 Brutons tyrosine kinase (BTK) inhibitor
a, b, 1 b, c, 1 b, d, 1 b, c, 1
Qianmao Liang , Yongfei Chen , Kailin Yu , Cheng Chen ,
e, 1 b, d b, c b, d a, b
Shouxiang Zhang , Aoli Wang , Wei Wang , Hong Wu , Xiaochuan Liu ,
Beilei Wang b, c, Li Wang b, c, Zhenquan Hu b, c, Wenchao Wang b, c, Tao Ren f,
Shanchun Zhang c, g, Qingsong Liu b, c, d, f, Cai-Hong Yun e, *, Jing Liu b, c, **
a Department of Chemistry, University of Science and Technology of China, Hefei, Anhui 230036, PR China
b High Magnetic Field Laboratory, Chinese Academy of Sciences, Mailbox 1110, 350 Shushanhu Road, Hefei, Anhui 230031, PR China
c CHMFL-HCMTC Target Therapy Joint Laboratory, 350 Shushanhu Road, Hefei, Anhui 230031, PR China
d University of Science and Technology of China, Hefei, Anhui 230036, PR China
e Institute of Systems Biomedicine, Department of Biophysics, Beijing Key Laboratory of Tumor Systems Biology and Center for Molecular and Translational
Medicine, School of Basic Medical Sciences, Peking University Health
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