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Identification of novel pyrrolopyrazoles as protein kinase C β II inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jan 01; Vol. 21 (1), pp. 584-7. Date of Electronic Publication: 2010 Oct 13. - Publication Year :
- 2011
-
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.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- High-Throughput Screening Assays
Protein Kinase C metabolism
Protein Kinase C beta
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors pharmacology
Pyrazoles chemical synthesis
Pyrazoles pharmacology
Structure-Activity Relationship
Protein Kinase C antagonists & inhibitors
Protein Kinase Inhibitors chemistry
Pyrazoles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21084194
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.10.032