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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: liu j, liu x, liu q. 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 (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: liu j, liu x, liu q. 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: liu j, liu q, liu f. 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: liu j, liu q. 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: liu j, liu q. 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: liu j, liu q. 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 2-(4-Chloro-3-(trifluoromethyl)phenyl)-N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors.
Wu Y, Wang B, Wang J, Qi S, Zou F, Qi Z, Liu F, Liu Q, Chen C, Hu C, Hu Z, Wang A, Wang L, Wang W, Ren T, Cai Y, Bai M, Liu Q, Liu J. Wu Y, et al. Among authors: liu j, liu q, liu f. J Med Chem. 2019 Jul 11;62(13):6083-6101. doi: 10.1021/acs.jmedchem.9b00280. Epub 2019 Jun 28. J Med Chem. 2019. PMID: 31250638
Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants.
Wang B, Zhang W, Liu X, Zou F, Wang J, Liu Q, Wang A, Hu Z, Chen Y, Qi S, Jiang Z, Chen C, Hu C, Wang L, Wang W, Liu Q, Liu J. Wang B, et al. Among authors: liu j, liu x, liu q. Eur J Med Chem. 2020 Dec 1;207:112744. doi: 10.1016/j.ejmech.2020.112744. Epub 2020 Aug 30. Eur J Med Chem. 2020. PMID: 32949955
Discovery of (S)-2-(1-(4-Amino-3-(3-fluoro-4-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)propyl)-3-cyclopropyl-5-fluoroquinazolin-4(3H)-one (IHMT-PI3Kδ-372) as a Potent and Selective PI3Kδ Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease.
Li F, Liang X, Jiang Z, Wang A, Wang J, Chen C, Wang W, Zou F, Qi Z, Liu Q, Hu Z, Cao J, Wu H, Wang B, Wang L, Liu J, Liu Q. Li F, et al. Among authors: liu j, liu q. J Med Chem. 2020 Nov 25;63(22):13973-13993. doi: 10.1021/acs.jmedchem.0c01544. Epub 2020 Nov 12. J Med Chem. 2020. PMID: 33180507
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