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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: jiang z. 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 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: jiang z. 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 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: jiang z. 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 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: jiang z. 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: jiang z. 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: jiang z. 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
Repurposing cabozantinib to GISTs: Overcoming multiple imatinib-resistant cKIT mutations including gatekeeper and activation loop mutants in GISTs preclinical models.
Lu T, Chen C, Wang A, Jiang Z, Qi Z, Hu Z, Hu C, Liu F, Wang W, Wu H, Wang B, Wang L, Qi S, Wu J, Wang W, Tang J, Yan H, Bai M, Liu Q, Liu J. Lu T, et al. Among authors: jiang z. Cancer Lett. 2019 Apr 10;447:105-114. doi: 10.1016/j.canlet.2019.01.024. Epub 2019 Jan 24. Cancer Lett. 2019. PMID: 30684595
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: jiang z. 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: jiang z. 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
17,908 results
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