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Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.
Li X, Wang A, Yu K, Qi Z, Chen C, Wang W, Hu C, Wu H, Wu J, Zhao Z, Liu J, Zou F, Wang L, Wang B, Wang W, Zhang S, Liu J, Liu Q. Li X, et al. Among authors: yu k. J Med Chem. 2015 Dec 24;58(24):9625-38. doi: 10.1021/acs.jmedchem.5b01611. Epub 2015 Dec 14. J Med Chem. 2015. PMID: 26630553
Ibrutinib selectively targets FLT3-ITD in mutant FLT3-positive AML.
Wu H, Hu C, Wang A, Weisberg EL, Wang W, Chen C, Zhao Z, Yu K, Liu J, Wu J, Nonami A, Wang L, Wang B, Stone RM, Liu S, Griffin JD, Liu J, Liu Q. Wu H, et al. Among authors: yu k. Leukemia. 2016 Mar;30(3):754-7. doi: 10.1038/leu.2015.175. Epub 2015 Jul 3. Leukemia. 2016. PMID: 26139428 Free PMC article. No abstract available.
Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells.
Wu H, Wang A, Zhang W, Wang B, Chen C, Wang W, Hu C, Ye Z, Zhao Z, Wang L, Li X, Yu K, Liu J, Wu J, Yan XE, Zhao P, Wang J, Wang C, Weisberg EL, Gray NS, Yun CH, Liu J, Chen L, Liu Q. Wu H, et al. Among authors: yu k. Oncotarget. 2015 Oct 13;6(31):31313-22. doi: 10.18632/oncotarget.5182. Oncotarget. 2015. PMID: 26375053 Free PMC article.
Discovery of a Highly Selective STK16 Kinase Inhibitor.
Liu F, Wang J, Yang X, Li B, Wu H, Qi S, Chen C, Liu X, Yu K, Wang W, Zhao Z, Wang A, Chen Y, Wang L, Gray NS, Liu J, Zhang X, Liu Q. Liu F, et al. Among authors: yu k. ACS Chem Biol. 2016 Jun 17;11(6):1537-43. doi: 10.1021/acschembio.6b00250. Epub 2016 Apr 22. ACS Chem Biol. 2016. PMID: 27082499
Discovery of a highly potent FLT3 kinase inhibitor for FLT3-ITD-positive AML.
Wu H, Wang A, Qi Z, Li X, Chen C, Yu K, Zou F, Hu C, Wang W, Zhao Z, Wu J, Liu J, Liu X, Wang L, Wang W, Zhang S, Stone RM, Galinsky IA, Griffin JD, Weinstock D, Christodoulou A, Wang H, Shen Y, Zhai Z, Weisberg EL, Liu J, Liu Q. Wu H, et al. Among authors: yu k. Leukemia. 2016 Oct;30(10):2112-2116. doi: 10.1038/leu.2016.151. Epub 2016 May 25. Leukemia. 2016. PMID: 27220667 Free PMC article. No abstract available.
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kinase.
Li B, Wang A, Liu J, Qi Z, Liu X, Yu K, Wu H, Chen C, Hu C, Wang W, Wu J, Hu Z, Ye L, Zou F, Liu F, Wang B, Wang L, Ren T, Zhang S, Bai M, Zhang S, Liu J, Liu Q. Li B, et al. Among authors: yu k. J Med Chem. 2016 Sep 22;59(18):8456-72. doi: 10.1021/acs.jmedchem.6b00902. Epub 2016 Aug 30. J Med Chem. 2016. PMID: 27545040
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.
Wang Q, Liu F, Wang B, Zou F, Qi Z, Chen C, Yu K, Hu C, Qi S, Wang W, Hu Z, Liu J, Wang W, Wang L, Liang Q, Zhang S, Ren T, Liu Q, Liu J. Wang Q, et al. Among authors: yu k. J Med Chem. 2017 Jan 12;60(1):273-289. doi: 10.1021/acs.jmedchem.6b01290. Epub 2016 Dec 14. J Med Chem. 2017. PMID: 27966954
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.
Liang X, Lv F, Wang B, Yu K, Wu H, Qi Z, Jiang Z, Chen C, Wang A, Miao W, Wang W, Hu Z, Liu J, Liu X, Zhao Z, Wang L, Zhang S, Ye Z, Wang C, Ren T, Wang Y, Liu Q, Liu J. Liang X, et al. Among authors: yu k. J Med Chem. 2017 Mar 9;60(5):1793-1816. doi: 10.1021/acs.jmedchem.6b01413. Epub 2017 Feb 14. J Med Chem. 2017. PMID: 28140585
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 Mutant Kinase Inhibitor with a Distinct Binding Mode.
Wang A, Li X, Wu H, Zou F, Yan XE, Chen C, Hu C, Yu K, Wang W, Zhao P, Wu J, Qi Z, Wang W, Wang B, Wang L, Ren T, Zhang S, Yun CH, Liu J, Liu Q. Wang A, et al. Among authors: yu k. J Med Chem. 2017 Apr 13;60(7):2944-2962. doi: 10.1021/acs.jmedchem.6b01907. Epub 2017 Mar 22. J Med Chem. 2017. PMID: 28282122
8,764 results