1.
Bioorg Med Chem Lett
; 22(14): 4528-31, 2012 Jul 15.
Article
in English
| MEDLINE
| ID: mdl-22727637
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.
Subject(s)
Protein Kinase Inhibitors/chemical synthesis , Protein Serine-Threonine Kinases/antagonists & inhibitors , Animals , Aurora Kinases , Cell Line , Mice , Models, Molecular , Molecular Structure , Protein Kinase Inhibitors/pharmacology , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 21(18): 5620-4, 2011 Sep 15.
Article
in English
| MEDLINE
| ID: mdl-21778056
ABSTRACT
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.