Literature DB >> 23147077

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

Yoshito Terao1, Hideo Suzuki, Masato Yoshikawa, Hiroaki Yashiro, Shiro Takekawa, Yasushi Fujitani, Kengo Okada, Yoshihisa Inoue, Yoshio Yamamoto, Hideyuki Nakagawa, Shuhei Yao, Tomohiro Kawamoto, Osamu Uchikawa.   

Abstract

Imidazo[1,2-a]pyridine derivatives were designed, synthesized, and evaluated as inhibitors of the apoptosis signal-regulating kinase 1 (ASK1). These were based on a benzothiazole derivative that was discovered from high-throughput screening of our compound library. As a result, we identified potent, selective, and orally bioavailable ASK1 inhibitors for wide range of therapeutic targets.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23147077     DOI: 10.1016/j.bmcl.2012.10.084

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


  14 in total

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

Authors:  Andrii Monastyrskyi; Simon Bayle; Victor Quereda; Wayne Grant; Michael Cameron; Derek Duckett; William Roush
Journal:  Bioorg Med Chem Lett       Date:  2017-12-13       Impact factor: 2.823

2.  Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure.

Authors:  Marion Lanier; Jason Pickens; Simone V Bigi; Erica L Bradshaw-Pierce; Alison Chambers; Zacharia S Cheruvallath; Derek Cole; Douglas R Dougan; Jacques Ermolieff; Tony Gibson; Petro Halkowycz; Aki Hirokawa; Anthony Ivetac; Joanne Miura; Evan Nunez; Mark Sabat; John Tyhonas; Haixia Wang; Xiaolun Wang; Steve Swann
Journal:  ACS Med Chem Lett       Date:  2017-02-08       Impact factor: 4.345

3.  ASK1 contributes to fibrosis and dysfunction in models of kidney disease.

Authors:  John T Liles; Britton K Corkey; Gregory T Notte; Grant R Budas; Eric B Lansdon; Ford Hinojosa-Kirschenbaum; Shawn S Badal; Michael Lee; Brian E Schultz; Sarah Wise; Swetha Pendem; Michael Graupe; Laurie Castonguay; Keith A Koch; Melanie H Wong; Giuseppe A Papalia; Dorothy M French; Theodore Sullivan; Erik G Huntzicker; Frank Y Ma; David J Nikolic-Paterson; Tareq Altuhaifi; Haichun Yang; Agnes B Fogo; David G Breckenridge
Journal:  J Clin Invest       Date:  2018-07-19       Impact factor: 14.808

Review 4.  Strategies for Improving Photodynamic Therapy Through Pharmacological Modulation of the Immediate Early Stress Response.

Authors:  Daniel J de Klerk; Mark J de Keijzer; Lionel M Dias; Jordi Heemskerk; Lianne R de Haan; Tony G Kleijn; Leonardo P Franchi; Michal Heger
Journal:  Methods Mol Biol       Date:  2022

5.  Crystal structures of ASK1-inhibtor complexes provide a platform for structure-based drug design.

Authors:  Onkar Singh; Anthony Shillings; Peter Craggs; Ian Wall; Paul Rowland; Tadeusz Skarzynski; Clare I Hobbs; Phil Hardwick; Rob Tanner; Michelle Blunt; David R Witty; Kathrine J Smith
Journal:  Protein Sci       Date:  2013-07-03       Impact factor: 6.725

6.  Inhibition of JNK and p38 MAPK phosphorylation by 5-(acetylamino)-4-oxo-6-phenyl-2-hexenoic acid methyl ester and 4-phenyl-butenoic acid decreases substance P-induced TNF-α upregulation in macrophages.

Authors:  Jacob D Lucrezi; Timothy J Burns; Diane F Matesic; Charlie D Oldham; Sheldon W May
Journal:  Int Immunopharmacol       Date:  2014-04-18       Impact factor: 4.932

7.  Antiproliferative activity of novel imidazopyridine derivatives on castration-resistant human prostate cancer cells.

Authors:  Sakthivel Muniyan; Yu-Wei Chou; Matthew A Ingersoll; Alexus Devine; Marisha Morris; Valerie A Odero-Marah; Shafiq A Khan; William G Chaney; Xiu R Bu; Ming-Fong Lin
Journal:  Cancer Lett       Date:  2014-07-19       Impact factor: 8.679

8.  Novel Imidazopyridine Derivatives Possess Anti-Tumor Effect on Human Castration-Resistant Prostate Cancer Cells.

Authors:  Matthew A Ingersoll; Anastesia S Lyons; Sakthivel Muniyan; Napoleon D'Cunha; Tashika Robinson; Kyle Hoelting; Jennifer G Dwyer; Xiu R Bu; Surinder K Batra; Ming-Fong Lin
Journal:  PLoS One       Date:  2015-06-29       Impact factor: 3.240

9.  CLK-dependent exon recognition and conjoined gene formation revealed with a novel small molecule inhibitor.

Authors:  Tyler Funnell; Shinya Tasaki; Arusha Oloumi; Shinsuke Araki; Esther Kong; Damian Yap; Yusuke Nakayama; Christopher S Hughes; S-W Grace Cheng; Hirokazu Tozaki; Misa Iwatani; Satoshi Sasaki; Tomohiro Ohashi; Tohru Miyazaki; Nao Morishita; Daisuke Morishita; Mari Ogasawara-Shimizu; Momoko Ohori; Shoichi Nakao; Masatoshi Karashima; Masaya Sano; Aiko Murai; Toshiyuki Nomura; Noriko Uchiyama; Tomohiro Kawamoto; Ryujiro Hara; Osamu Nakanishi; Karey Shumansky; Jamie Rosner; Adrian Wan; Steven McKinney; Gregg B Morin; Atsushi Nakanishi; Sohrab Shah; Hiroyoshi Toyoshiba; Samuel Aparicio
Journal:  Nat Commun       Date:  2017-02-23       Impact factor: 14.919

10.  Apoptosis signal-regulating kinase 1 inhibition attenuates human airway smooth muscle growth and migration in chronic obstructive pulmonary disease.

Authors:  Mathew S Eapen; Anudeep Kota; Howard Vindin; Kielan D McAlinden; Dia Xenaki; Brian G Oliver; Deepak A Deshpande; Sukhwinder Singh Sohal; Pawan Sharma
Journal:  Clin Sci (Lond)       Date:  2018-07-31       Impact factor: 6.124

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