Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors

• Published in: Bioorganic & medicinal chemistry letters Vol. 22; no. 14; pp. 4528 - 4531
• Main Authors: Ji, Zhiqin, Dai, Yujia, Abad-Zapatero, Cele, Albert, Daniel H., Bouska, Jennifer J., Glaser, Keith B., Marcotte, Patrick A., Soni, Nirupama B., Magoc, Terry J., Stewart, Kent D., Wei, Ru-Qi, Davidsen, Steve K., Michaelides, Michael R.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 15.07.2012; Elsevier
• Subjects: Animals; Anticancer drug; Aurora kinase inhibitor; Aurora Kinases; Biological and medical sciences; Cell Line; enzyme inhibitors; Hinge-binding scaffold; Medical sciences; Mice; Models, Molecular; Molecular Structure; pharmacokinetics; Pharmacology. Drug treatments; Protein Kinase Inhibitors - chemical synthesis; Protein Kinase Inhibitors - pharmacology; protein-serine-threonine kinases; Protein-Serine-Threonine Kinases - antagonists & inhibitors; scaffolding proteins; Structure-Activity Relationship; structure-activity relationships; Hinge-binding scaffold; Anticancer drug; Aurora kinase inhibitor; Antineoplastic agent; Signal transduction; Enzyme; Transferases; Non-specific serine/threonine protein kinase; Enzyme inhibitor; Selectivity
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2012.05.125

Four hinge-binding scaffolds have been explored for novel selective Aurora kinase inhibitors. The structure activity relationship, selectivity and pharmacokinetic profiles have been evaluated.