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

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

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-07, Vol.22 (14), p.4528-4531
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	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
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Beschreibung
Zusammenfassung:	Four hinge-binding scaffolds have been explored for novel selective Aurora kinase inhibitors. The structure activity relationship, selectivity and pharmacokinetic profiles have been evaluated.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.05.125