Abstract
Through the analysis of X-ray crystallographic information and previous SAR studies, a novel series of protein kinase B (PKB/AKT) inhibitors was developed. The compounds showed nanomolar inhibition of AKT1 and were selective against cyclin-dependent kinase 2 (CDK2).
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
-
Amides / chemical synthesis
-
Amides / chemistry
-
Amides / pharmacology*
-
Chemistry Techniques, Synthetic
-
Crystallography, X-Ray
-
Cyclin-Dependent Kinase 2 / antagonists & inhibitors*
-
Cyclin-Dependent Kinase 2 / metabolism
-
Dose-Response Relationship, Drug
-
Drug Design*
-
Enzyme Inhibitors / chemical synthesis*
-
Enzyme Inhibitors / chemistry
-
Enzyme Inhibitors / pharmacology*
-
Models, Molecular
-
Molecular Structure
-
Proto-Oncogene Proteins c-akt / antagonists & inhibitors*
-
Proto-Oncogene Proteins c-akt / metabolism
-
Stereoisomerism
-
Structure-Activity Relationship
Substances
-
Amides
-
Enzyme Inhibitors
-
Proto-Oncogene Proteins c-akt
-
Cyclin-Dependent Kinase 2