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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.
Chen Y, Wu J, Wang A, Qi Z, Jiang T, Chen C, Zou F, Hu C, Wang W, Wu H, Hu Z, Wang W, Wang B, Wang L, Ren T, Zhang S, Liu Q, Liu J. Chen Y, et al. Among authors: chen c. Eur J Med Chem. 2017 Oct 20;139:674-697. doi: 10.1016/j.ejmech.2017.08.035. Epub 2017 Aug 18. Eur J Med Chem. 2017. PMID: 28850922
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.
Wang A, Li X, Chen C, Wu H, Qi Z, Hu C, Yu K, Wu J, Liu J, Liu X, Hu Z, Wang W, Wang W, Wang W, Wang L, Wang B, Liu Q, Li L, Ge J, Ren T, Zhang S, Xia R, Liu J, Liu Q. Wang A, et al. Among authors: chen c. J Med Chem. 2017 Oct 26;60(20):8407-8424. doi: 10.1021/acs.jmedchem.7b00840. Epub 2017 Oct 17. J Med Chem. 2017. PMID: 28956923
Discovery of a highly selective KIT kinase primary V559D mutant inhibitor for gastrointestinal stromal tumors (GISTs).
Yu K, Liu X, Jiang Z, Hu C, Zou F, Chen C, Ge J, Wu J, Liu X, Wang A, Wang W, Wang W, Qi Z, Wang B, Wang L, Yan H, Wang J, Ren T, Tang J, Liu Q, Liu J. Yu K, et al. Among authors: chen c. Oncotarget. 2017 Nov 15;8(67):111110-111118. doi: 10.18632/oncotarget.22624. eCollection 2017 Dec 19. Oncotarget. 2017. PMID: 29340041 Free PMC article.
Discovery of N-(4-(6-Acetamidopyrimidin-4-yloxy)phenyl)-2-(2-(trifluoromethyl)phenyl)acetamide (CHMFL-FLT3-335) as a Potent FMS-like Tyrosine Kinase 3 Internal Tandem Duplication (FLT3-ITD) Mutant Selective Inhibitor for Acute Myeloid Leukemia.
Liang X, Wang B, Chen C, Wang A, Hu C, Zou F, Yu K, Liu Q, Li F, Hu Z, Lu T, Wang J, Wang L, Weisberg EL, Li L, Xia R, Wang W, Ren T, Ge J, Liu J, Liu Q. Liang X, et al. Among authors: chen c. J Med Chem. 2019 Jan 24;62(2):875-892. doi: 10.1021/acs.jmedchem.8b01594. Epub 2019 Jan 8. J Med Chem. 2019. PMID: 30565931
Discovery of a novel and highly selective CDK9 kinase inhibitor (JSH-009) with potent antitumor efficacy in preclinical acute myeloid leukemia models.
Wang L, Hu C, Wang A, Chen C, Wu J, Jiang Z, Zou F, Yu K, Wu H, Liu J, Wang W, Wang Z, Wang B, Qi Z, Liu Q, Wang W, Li L, Ge J, Liu J, Liu Q. Wang L, et al. Among authors: chen c. Invest New Drugs. 2020 Oct;38(5):1272-1281. doi: 10.1007/s10637-019-00868-3. Epub 2019 Dec 23. Invest New Drugs. 2020. PMID: 31872348
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: chen l, chen c. Oncotarget. 2015 Oct 13;6(31):31313-22. doi: 10.18632/oncotarget.5182. Oncotarget. 2015. PMID: 26375053 Free PMC article.
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: chen c. 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
91,804 results
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