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Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.

Hu E, Tasker A, White RD, Kunz RK, Human J, Chen N, Bürli R, Hungate R, Novak P, Itano A, Zhang X, Yu V, Nguyen Y, Tudor Y, Plant M, Flynn S, Xu Y, Meagher KL, Whittington DA, Ng GY
J Med Chem 51 3065-8 (2008)
Related entries: 3cpb, 3cpc

Cited: 15 times
EuropePMC logo PMID: 18447379

Abstract

Inhibition of c-Kit has the potential to treat mast cell associated fibrotic diseases. We report the discovery of several aminoquinazoline pyridones that are potent inhibitors of c-Kit with greater than 200-fold selectivity against KDR, p38, Lck, and Src. In vivo efficacy of pyridone 16 by dose-dependent inhibition of histamine release was demonstrated in a rodent pharmacodynamic model of mast cell activation.

Articles - 3cp9 mentioned but not cited (5)

  1. Biological activity, quantitative structure-activity relationship analysis, and molecular docking of xanthone derivatives as anticancer drugs. Miladiyah I, Jumina J, Haryana SM, Mustofa M. Drug Des Devel Ther 12 149-158 (2018)
  2. Elucidation of molecular targets of bioactive principles of black cumin relevant to its anti-tumour functionality - An Insilico target fishing approach. Sridhar A, Saremy S, Bhattacharjee B. Bioinformation 10 684-688 (2014)
  3. Antitumor Activity and Mechanism of Robustic Acid from Dalbergia benthami Prain via Computational Target Fishing. Huang J, Liang Y, Tian W, Ma J, Huang L, Li B, Chen R, Li D. Molecules 25 E3919 (2020)
  4. Pioglitazone Induces Cardiomyocyte Apoptosis and Inhibits Cardiomyocyte Hypertrophy Via VEGFR-2 Signaling Pathway. Zhong W, Jin W, Xu S, Wu Y, Luo S, Liang M, Chen L. Arq Bras Cardiol 111 162-169 (2018)
  5. Antiproliferative activity and interaction with proteins of N-cyclohexylacrylamide. Çankaya N, Yalçin S. Saudi J Biol Sci 29 101670 (2022)


Articles citing this publication (10)

  1. Diamine Ligands in Copper-Catalyzed Reactions. Surry DS, Buchwald SL. Chem Sci 1 13-31 (2010)
  2. Type-II kinase inhibitor docking, screening, and profiling using modified structures of active kinase states. Kufareva I, Abagyan R. J Med Chem 51 7921-7932 (2008)
  3. Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2. Hilton S, Naud S, Caldwell JJ, Boxall K, Burns S, Anderson VE, Antoni L, Allen CE, Pearl LH, Oliver AW, Wynne Aherne G, Garrett MD, Collins I. Bioorg Med Chem 18 707-718 (2010)
  4. Synthesis and evaluation of c-Src kinase inhibitory activity of pyridin-2(1H)-one derivatives. Chand K, Prasad S, Tiwari RK, Shirazi AN, Kumar S, Parang K, Sharma SK. Bioorg Chem 53 75-82 (2014)
  5. Discovery of potent vascular endothelial growth factor receptor-2 inhibitors. Papakyriakou A, Katsarou ME, Belimezi M, Karpusas M, Vourloumis D. ChemMedChem 5 118-129 (2010)
  6. Vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors: development and validation of predictive 3-D QSAR models through extensive ligand- and structure-based approaches. Ragno R, Ballante F, Pirolli A, Wickersham RB, Patsilinakos A, Hesse S, Perspicace E, Kirsch G. J Comput Aided Mol Des 29 757-776 (2015)
  7. A Simple and Efficient Approach for the Synthesis of 2-Aminated Quinazoline Derivatives via Metal Free Oxidative Annulation. Pandya AN, Villa EM, North EJ. Tetrahedron Lett 58 1276-1279 (2017)
  8. Discovery of amido-benzisoxazoles as potent c-Kit inhibitors. Kunz RK, Rumfelt S, Chen N, Zhang D, Tasker AS, Bürli R, Hungate R, Yu V, Nguyen Y, Whittington DA, Meagher KL, Plant M, Tudor Y, Schrag M, Xu Y, Ng GY, Hu E. Bioorg Med Chem Lett 18 5115-5117 (2008)
  9. Investigation of a novel molecular descriptor for the lead optimization of 4-aminoquinazolines as vascular endothelial growth factor receptor-2 inhibitors: application for quantitative structure-activity relationship analysis in lead optimization. Kawakami JK, Martinez Y, Sasaki B, Harris M, Kurata WE, Lau AF. Bioorg Med Chem Lett 21 1371-1375 (2011)
  10. Design, Synthesis, and Evaluation of the Kinase Inhibition Potential of Pyridylpyrimidinylaminophenyl Derivatives. Manchanda P, Parshad B, Kumar A, Tiwari RK, Shirazi AN, Parang K, Sharma SK. Arch Pharm (Weinheim) 350 (2017)


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