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.

No abstract is available for this paper.

• Publication year

  2018

• Venue

  European journal of medicinal chemistry

• Publication date

  2018-04-25

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/j.ejmech.2018.03.003PMID 29544149
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Exploration of Type II Binding Mode: A Privileged Approach for Kinase Inhibitor Focused Drug Discovery?

  2014cited by this paper
• Platelet-derived growth factors and their receptors: structural and functional perspectives.

  2013cited by this paper
• Multifarious functions of PDGFs and PDGFRs in tumor growth and metastasis.

  2013cited by this paper
• PrimeX and the Schrödinger computational chemistry suite of programs

  2012cited by this paper
• Crenolanib Inhibits the Drug-Resistant PDGFRA D842V Mutation Associated with Imatinib-Resistant Gastrointestinal Stromal Tumors

  2012cited by this paper
• Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.

  2011cited by this paper
• Masitinib (AB1010), a Potent and Selective Tyrosine Kinase Inhibitor Targeting KIT

  2009cited by this paper
• AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.

  2009cited by this paper
• Nonclinical Antiangiogenesis and Antitumor Activities of Axitinib (AG-013736), an Oral, Potent, and Selective Inhibitor of Vascular Endothelial Growth Factor Receptor Tyrosine Kinases 1, 2, 3

  2008cited by this paper
• BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.

  2008cited by this paper
• Phaser crystallographic software

  2007cited by this paper
• A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors

  2007cited by this paper
• Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.

  2007cited by this paper
• HKL-3000: the integration of data reduction and structure solution--from diffraction images to an initial model in minutes.

  2006cited by this paper
• Biology of platelet-derived growth factor and its involvement in disease.

  2006cited by this paper
• A small molecule–kinase interaction map for clinical kinase inhibitors

  2005cited by this paper
• Platelet-derived growth factor receptor (PDGFR): a target for anticancer therapeutics.

  2005cited by this paper
• Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor

  2005cited by this paper
• Coot: model-building tools for molecular graphics.

  2004cited by this paper
• MUSCLE: multiple sequence alignment with high accuracy and high throughput.

  2004cited by this paper
• The EOL-1 cell line as an in vitro model for the study of FIP1L1-PDGFRA-positive chronic eosinophilic leukemia.

  2004cited by this paper
• The structural basis for autoinhibition of FLT3 by the juxtamembrane domain.

  2004cited by this paper
• PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease.

  2003cited by this paper
• Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.

  2003cited by this paper
• Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor.

  2000cited by this paper
• Selective inhibition of the platelet-derived growth factor signal transduction pathway by a protein-tyrosine kinase inhibitor of the 2-phenylaminopyrimidine class.

  1995cited by this paper
• Comparative protein modelling by satisfaction of spatial restraints.

  1993cited by this paper
• Induction of platelet-derived growth factor receptor expression in smooth muscle cells and fibroblasts upon tissue culturing

  1988cited by this paper
• Human proto‐oncogene c‐kit: a new cell surface receptor tyrosine kinase for an unidentified ligand.

  1987cited by this paper
• Electronic Reprint Biological Crystallography Phenix : a Comprehensive Python-based System for Macromolecular Structure Solution

  year unknowncited by this paper

• Results of a large scale study of the binding of 50 type II inhibitors to 348 kinases: The role of protein reorganization

  2026cites this paper
• Targeting JAK/STAT axis in solid tumors: resolving the therapeutic paradox through upstream suppression and downstream disruption

  2026cites this paper
• Tumor biomarkers for diagnosis, prognosis and targeted therapy

  2024cites this paper
• Synthesis and cytotoxic activity evaluation of novel imidazopyridine carbohydrazide derivatives

  2024cites this paper
• Electrochemical [4 + 1] Tandem sp3(C–H) Double Amination for the Direct Synthesis of 3-Acyl-Functionalized Imidazo[1,5-a]pyridines

  2022cites this paper
• Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma.

  2022cites this paper
• Targeting the PDGF/PDGFR signaling pathway for cancer therapy: A review.

  2022cites this paper
• Novel α-Aminophosphonates of imatinib Intermediate: Synthesis, anticancer Activity, human Abl tyrosine kinase Inhibition, ADME and toxicity prediction.

  2021cites this paper
• CBr4 Mediated [4 + 1] Dehydrocyclization for the Synthesis of Functionalized Imidazo[1,5-a]heterocycles from Pyridin-2-ylmethanamines and Aldehydes

  2021cites this paper
• S100A8 and S100A9 Promote Apoptosis of Chronic Eosinophilic Leukemia Cells

  2020cites this paper
• Identification of potential platelet-derived growth factor receptor α inhibitors by computational screening and binding simulations.

  2019cites this paper
• Renal Clearable Theranostic Nanoplatforms for Gastrointestinal Stromal Tumors

  2019cites this paper
• HMER_A_213397 109..129

  2019cites this paper
• “Let my liver rather heat with wine” - a review of hepatic fibrosis pathophysiology and emerging therapeutics

  2019cites this paper
• Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity.

  2019cites this paper
• 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.

  2019cites this paper
• Design, synthesis, cytotoxicity, and molecular modeling study of 2,4,6-trisubstituted pyrimidines with anthranilate ester moiety

  2019cites this paper