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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: chen c, chen y. 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 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 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia.
Wang Q, Liu F, Qi S, Qi Z, Yan XE, Wang B, Wang A, Wang W, Chen C, Liu X, Jiang Z, Hu Z, Wang L, Wang W, Ren T, Zhang S, Yun CH, Liu Q, Liu J. Wang Q, et al. Among authors: chen c. Eur J Med Chem. 2018 Apr 25;150:366-384. doi: 10.1016/j.ejmech.2018.03.003. Epub 2018 Mar 20. Eur J Med Chem. 2018. PMID: 29544149
Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor.
Liang X, Li F, Chen C, Jiang Z, Wang A, Liu X, Ge J, Hu Z, Yu K, Wang W, Zou F, Liu Q, Wang B, Wang L, Zhang S, Wang Y, Liu Q, Liu J. Liang X, et al. Among authors: chen c. Eur J Med Chem. 2018 Aug 5;156:831-846. doi: 10.1016/j.ejmech.2018.07.036. Epub 2018 Jul 17. Eur J Med Chem. 2018. PMID: 30053721
Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.
Wang B, Wu J, Wu Y, Chen C, Zou F, Wang A, Wu H, Hu Z, Jiang Z, Liu Q, Wang W, Zhang Y, Liu F, Zhao M, Hu J, Huang T, Ge J, Wang L, Ren T, Wang Y, Liu J, Liu Q. Wang B, et al. Among authors: chen c. Eur J Med Chem. 2018 Oct 5;158:896-916. doi: 10.1016/j.ejmech.2018.09.025. Epub 2018 Sep 13. Eur J Med Chem. 2018. PMID: 30253346
Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia.
Liu X, Wang B, Chen C, Jiang Z, Hu C, Wu H, Zhang Y, Liu X, Wang W, Wang J, Hu Z, Wang A, Huang T, Liu Q, Wang W, Wang L, Wang W, Ren T, Li L, Xia R, Ge J, Liu Q, Liu J. Liu X, et al. Among authors: chen c. Eur J Med Chem. 2018 Dec 5;160:61-81. doi: 10.1016/j.ejmech.2018.10.007. Epub 2018 Oct 5. Eur J Med Chem. 2018. PMID: 30317026
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 ( E)- N1-(3-Fluorophenyl)- N3-(3-(2-(pyridin-2-yl)vinyl)-1 H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs).
Liu X, Wang B, Chen C, Qi Z, Zou F, Wang J, Hu C, Wang A, Ge J, Liu Q, Yu K, Hu Z, Jiang Z, Wang W, Wang L, Wang W, Ren T, Bai M, Liu Q, Liu J. Liu X, et al. Among authors: chen c. J Med Chem. 2019 May 23;62(10):5006-5024. doi: 10.1021/acs.jmedchem.9b00176. Epub 2019 May 14. J Med Chem. 2019. PMID: 31046271
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
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
86,231 results
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