Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors—Hit to lead exploration

Autor:	Paul Lyne, Patrick Brassil, Ann White, Jason Breed, Mei Su, Dorin Toader, Yan Yu, Sonya Zabludoff, Jon Read, James W. Janetka, Chun Deng, Dingwei Yu, Vibha Oza, Susan Ashwell, Zheng Xiaolan, Nicholas John Newcombe, Candice Horn, Martin Pass, Peter J. H. Webborn, Ludo Otterbien, Heather Haye, Jay Ezhuthachan, Anna L Valentine, Sian Roswell
Rok vydání:	2010
Předmět:	Models Molecular animal structures High-throughput screening genetic processes Clinical Biochemistry Pharmaceutical Science Computational biology Crystallography X-Ray environment and public health Biochemistry Structure-Activity Relationship Drug Discovery Structure–activity relationship CHEK1 Protein kinase A Protein Kinase Inhibitors Molecular Biology Kinase Drug discovery Chemistry Organic Chemistry Hit to lead Triazoles enzymes and coenzymes (carbohydrates) Checkpoint Kinase 1 Molecular Medicine biological phenomena cell phenomena and immunity Signal transduction Protein Kinases
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 20:5133-5138
ISSN:	0960-894X
Popis:	Checkpoint Kinase-1 (Chk1, CHK1, CHEK1) is a Ser/Thr protein kinase that mediates cellular responses to DNA-damage. A novel class of Chk1 inhibitors, triazoloquinolones/triazolones (TZ's) was identified by high throughput screening. The optimization of these hits to provide a lead series is described.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02edc1c68b5470ccac027b686d298564 https://doi.org/10.1016/j.bmcl.2010.07.015 Zobrazit plný text záznamu Full Text from ScienceDirect