Literature DB >> 18447379

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

Essa Hu1, Andrew Tasker, Ryan D White, Roxanne K Kunz, Jason Human, Ning Chen, Roland Bürli, Randall Hungate, Perry Novak, Andrea Itano, Xuxia Zhang, Violeta Yu, Yen Nguyen, Yanyan Tudor, Matthew Plant, Shaun Flynn, Yang Xu, Kristin L Meagher, Douglas A Whittington, Gordon Y Ng.   

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.

Entities:  

Mesh：

Substances：

Year:  2008        PMID： 18447379     DOI： 10.1021/jm800188g

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  7 in total

1.  Type-II kinase inhibitor docking, screening, and profiling using modified structures of active kinase states.

Authors:  Irina Kufareva; Ruben Abagyan
Journal:  J Med Chem       Date:  2008-12-25       Impact factor: 7.446

2.  Diamine Ligands in Copper-Catalyzed Reactions.

Authors:  David S Surry; Stephen L Buchwald
Journal:  Chem Sci       Date:  2010       Impact factor: 9.825

3.  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.

Authors:  Joel K Kawakami; Yannica Martinez; Brandi Sasaki; Melissa Harris; Wendy E Kurata; Alan F Lau
Journal:  Bioorg Med Chem Lett       Date:  2011-01-14       Impact factor: 2.823

4.  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.

Authors:  Rino Ragno; Flavio Ballante; Adele Pirolli; Richard B Wickersham; Alexandros Patsilinakos; Stéphanie Hesse; Enrico Perspicace; Gilbert Kirsch
Journal:  J Comput Aided Mol Des       Date:  2015-07-21       Impact factor: 3.686

5.  tert-Butyl 2-(3-acetyl-amino-2-oxo-1,2-dihydro-1-pyrid-yl)acetate.

Authors:  N David Karis; Wendy A Loughlin; Ian D Jenkins; Peter C Healy
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-11-29

6.  A Simple and Efficient Approach for the Synthesis of 2-Aminated Quinazoline Derivatives via Metal Free Oxidative Annulation.

Authors:  Amit N Pandya; Eric M Villa; E Jeffrey North
Journal:  Tetrahedron Lett       Date:  2017-02-12       Impact factor: 2.415

7.  Elucidation of molecular targets of bioactive principles of black cumin relevant to its anti-tumour functionality - An Insilico target fishing approach.

Authors:  Amulyashree Sridhar; Sadegh Saremy; Biplab Bhattacharjee
Journal:  Bioinformation       Date:  2014-11-27
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.