Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases

In an effort to discover Aurora kinase inhibitors, an HTS hit revealed an amide containing pyrrolopyrimidine compound. Replacement of the pyrrolopyrimidine residue with a thienopyrimidine moiety led to a series of potent and selective Aurora inhibitors.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-09, Vol.21 (18), p.5620-5624
Hauptverfasser:	McClellan, William J., Dai, Yujia, Abad-Zapatero, Cele, Albert, Daniel H., Bouska, Jennifer J., Glaser, Keith B., Magoc, Terry J., Marcotte, Patrick A., Osterling, Donald J., Stewart, Kent D., Davidsen, Steven K., Michaelides, Michael R.
Format:	Artikel
Sprache:	eng
Schlagworte:	amides Animals Anti-cancer Antineoplastic agents Aurora kinase Aurora Kinases Biological and medical sciences Dose-Response Relationship, Drug Drug Discovery enzyme inhibitors General aspects High-Throughput Screening Assays Hydrogen Bonding Medical sciences Mice Models, Molecular Molecular Structure Orally bioavailable Pharmacology. Drug treatments Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology protein-serine-threonine kinases Protein-Serine-Threonine Kinases - antagonists & inhibitors Protein-Serine-Threonine Kinases - metabolism pyrimidines Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology pyrrolopyrimidines Stereoisomerism Structure-Activity Relationship Thienopyrimidine
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Beschreibung
Zusammenfassung:	In an effort to discover Aurora kinase inhibitors, an HTS hit revealed an amide containing pyrrolopyrimidine compound. Replacement of the pyrrolopyrimidine residue with a thienopyrimidine moiety led to a series of potent and selective Aurora inhibitors.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.06.041