Abstract
A novel series of pyrrolopyrazole-based protein kinase C β II inhibitors has been identified from high-throughput screening. Herein, we report our initial structure-activity relationship studies with a focus on optimizing compound ligand efficiency and physicochemical properties, which has led to potent inhibitors with good cell permeability.
Copyright © 2010 Elsevier Ltd. All rights reserved.
MeSH terms
-
High-Throughput Screening Assays
-
Protein Kinase C / antagonists & inhibitors*
-
Protein Kinase C / metabolism
-
Protein Kinase C beta
-
Protein Kinase Inhibitors / chemical synthesis
-
Protein Kinase Inhibitors / chemistry*
-
Protein Kinase Inhibitors / pharmacology
-
Pyrazoles / chemical synthesis
-
Pyrazoles / chemistry*
-
Pyrazoles / pharmacology
-
Structure-Activity Relationship
Substances
-
Protein Kinase Inhibitors
-
Pyrazoles
-
Protein Kinase C
-
Protein Kinase C beta