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

Zhiqin Ji; Yujia Dai; Cele Abad-Zapatero; Daniel H Albert; Jennifer J Bouska; Keith B Glaser; Patrick A Marcotte; Nirupama B Soni; Terry J Magoc; Kent D Stewart; Ru-Qi Wei; Steve K Davidsen; Michael R Michaelides

doi:10.1016/j.bmcl.2012.05.125

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

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4528-31. doi: 10.1016/j.bmcl.2012.05.125. Epub 2012 Jun 7.

Authors

Zhiqin Ji¹, Yujia Dai, Cele Abad-Zapatero, Daniel H Albert, Jennifer J Bouska, Keith B Glaser, Patrick A Marcotte, Nirupama B Soni, Terry J Magoc, Kent D Stewart, Ru-Qi Wei, Steve K Davidsen, Michael R Michaelides

Affiliation

¹ Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6100, USA. zhiqin.ji@abbott.com

PMID: 22727637
DOI: 10.1016/j.bmcl.2012.05.125

Abstract

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

MeSH terms

Animals
Aurora Kinases
Cell Line
Mice
Models, Molecular
Molecular Structure
Protein Kinase Inhibitors / chemical synthesis*
Protein Kinase Inhibitors / pharmacology
Protein Serine-Threonine Kinases / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Protein Kinase Inhibitors
Aurora Kinases
Protein Serine-Threonine Kinases