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Axitinib overcomes multiple imatinib resistant cKIT mutations including the gatekeeper mutation T670I in gastrointestinal stromal tumors.
Liu F, Zou F, Chen C, Yu K, Liu X, Qi S, Wu J, Hu C, Hu Z, Liu J, Liu X, Wang L, Ge J, Wang W, Ren T, Bai M, Cai Y, Xiao X, Qian F, Tang J, Liu Q, Liu J. Liu F, et al. Among authors: chen c. Ther Adv Med Oncol. 2019 May 17;11:1758835919849757. doi: 10.1177/1758835919849757. eCollection 2019. Ther Adv Med Oncol. 2019. PMID: 31205508 Free PMC article.
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: chen c. 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 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 (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 and characterization of a novel highly potent and selective type II native and drug-resistant V299L mutant BCR-ABL inhibitor (CHMFL-ABL-039) for Chronic Myeloid Leukemia (CML).
Wu J, Wang A, Li X, Chen C, Qi Z, Hu C, Wang W, Wu H, Huang T, Zhao M, Wang W, Hu Z, Liu Q, Wang B, Wang L, Li L, Ge J, Ren T, Xia R, Liu J, Liu Q. Wu J, et al. Among authors: chen c. Cancer Biol Ther. 2019;20(6):877-885. doi: 10.1080/15384047.2019.1579958. Epub 2019 Mar 20. Cancer Biol Ther. 2019. PMID: 30894066 Free PMC article.
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 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: chen c. 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 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
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