Literature DB >> 29277458

Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors.

Andrii Monastyrskyi1, Simon Bayle2, Victor Quereda2, Wayne Grant2, Michael Cameron2, Derek Duckett2, William Roush3.   

Abstract

The development of a new series of apoptosis signal-regulating kinase 1 (ASK1) inhibitors is described. Starting from purine, pyrimidine and quinazoline scaffolds identified by high throughput screening, we used tools of structure-based drug design to develop a series of potent kinase inhibitors, including 2-arylquinazoline derivatives 12 and 23, with submicromolar inhibitory activities against ASK1. Kinetic analysis demonstrated that the 2-arylquinazoline scaffold ASK1 inhibitors described herein are ATP competitive.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Apoptosis signal-regulating kinase (ASK1); High throughput screening; Inhibitor; Kinase; Structure-based drug design

Mesh：

Substances：

Year:  2017        PMID： 29277458      PMCID： PMC5999544          DOI： 10.1016/j.bmcl.2017.12.026

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  27 in total

1.  Glide: a new approach for rapid, accurate docking and scoring. 2. Enrichment factors in database screening.

Authors:  Thomas A Halgren; Robert B Murphy; Richard A Friesner; Hege S Beard; Leah L Frye; W Thomas Pollard; Jay L Banks
Journal:  J Med Chem       Date:  2004-03-25       Impact factor: 7.446

2.  Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy.

Authors:  Richard A Friesner; Jay L Banks; Robert B Murphy; Thomas A Halgren; Jasna J Klicic; Daniel T Mainz; Matthew P Repasky; Eric H Knoll; Mee Shelley; Jason K Perry; David E Shaw; Perry Francis; Peter S Shenkin
Journal:  J Med Chem       Date:  2004-03-25       Impact factor: 7.446

3.  Extra precision glide: docking and scoring incorporating a model of hydrophobic enclosure for protein-ligand complexes.

Authors:  Richard A Friesner; Robert B Murphy; Matthew P Repasky; Leah L Frye; Jeremy R Greenwood; Thomas A Halgren; Paul C Sanschagrin; Daniel T Mainz
Journal:  J Med Chem       Date:  2006-10-19       Impact factor: 7.446

Review 4.  Pathophysiological roles of ASK1-MAP kinase signaling pathways.

Authors:  Hiroaki Nagai; Takuya Noguchi; Kohsuke Takeda; Hidenori Ichijo
Journal:  J Biochem Mol Biol       Date:  2007-01-31

5.  Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors.

Authors:  Yoshito Terao; Hideo Suzuki; Masato Yoshikawa; Hiroaki Yashiro; Shiro Takekawa; Yasushi Fujitani; Kengo Okada; Yoshihisa Inoue; Yoshio Yamamoto; Hideyuki Nakagawa; Shuhei Yao; Tomohiro Kawamoto; Osamu Uchikawa
Journal:  Bioorg Med Chem Lett       Date:  2012-10-23       Impact factor: 2.823

6.  Design of a phase 2 clinical trial of an ASK1 inhibitor, GS-4997, in patients with diabetic kidney disease.

Authors:  Joseph H Lin; Jenny J Zhang; Shao-Lee Lin; Glenn M Chertow
Journal:  Nephron       Date:  2014-12-17       Impact factor: 2.847

7.  ASK1 mediates apoptotic cell death induced by genotoxic stress.

Authors:  Z Chen; H Seimiya; M Naito; T Mashima; A Kizaki; S Dan; M Imaizumi; H Ichijo; K Miyazono; T Tsuruo
Journal:  Oncogene       Date:  1999-01-07       Impact factor: 9.867

8.  Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties.

Authors:  Mathieu Bibian; Ronald J Rahaim; Jun Yong Choi; Yoshihiko Noguchi; Stephan Schürer; Weimin Chen; Shima Nakanishi; Konstantin Licht; Laura H Rosenberg; Lin Li; Yangbo Feng; Michael D Cameron; Derek R Duckett; John L Cleveland; William R Roush
Journal:  Bioorg Med Chem Lett       Date:  2013-05-31       Impact factor: 2.823

9.  Regulation of the severity of neuroinflammation and demyelination by TLR-ASK1-p38 pathway.

Authors:  Xiaoli Guo; Chikako Harada; Kazuhiko Namekata; Atsushi Matsuzawa; Monsterrat Camps; Hong Ji; Dominique Swinnen; Catherine Jorand-Lebrun; Mathilde Muzerelle; Pierre-Alain Vitte; Thomas Rückle; Atsuko Kimura; Kuniko Kohyama; Yoh Matsumoto; Hidenori Ichijo; Takayuki Harada
Journal:  EMBO Mol Med       Date:  2010-12       Impact factor: 12.137

10.  Inhibition of apoptosis signal-regulating kinase 1 reduces myocardial ischemia-reperfusion injury in the mouse.

Authors:  Stefano Toldo; David G Breckenridge; Eleonora Mezzaroma; Benjamin W Van Tassell; John Shryock; Harsha Kannan; Dillon Phan; Grant Budas; Daniela Farkas; Edward Lesnefsky; Norbert Voelkel; Antonio Abbate
Journal:  J Am Heart Assoc       Date:  2012-10-25       Impact factor: 5.501
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