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Discovery of pyrrolopyrimidine inhibitors of Akt.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Oct 01; Vol. 20 (19), pp. 5607-12. Date of Electronic Publication: 2010 Aug 13. - Publication Year :
- 2010
-
Abstract
- The discovery and optimization of a series of pyrrolopyrimidine based protein kinase B (Pkb/Akt) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent inhibition of all three Akt isoforms and knockdown of phospho-PRAS40 levels in LNCaP cells and tumor xenografts.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Adaptor Proteins, Signal Transducing
Animals
Binding Sites
Cell Line
Crystallography, X-Ray
Drug Design
Drug Evaluation, Preclinical
High-Throughput Screening Assays
Humans
Mice
Phosphoproteins deficiency
Phosphoproteins genetics
Phosphoproteins metabolism
Protein Isoforms antagonists & inhibitors
Protein Isoforms metabolism
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors pharmacology
Protein Structure, Tertiary
Proto-Oncogene Proteins c-akt metabolism
Pyrimidines chemical synthesis
Pyrimidines pharmacology
Pyrroles chemical synthesis
Pyrroles pharmacology
Structure-Activity Relationship
Xenograft Model Antitumor Assays
Protein Kinase Inhibitors chemistry
Proto-Oncogene Proteins c-akt antagonists & inhibitors
Pyrimidines chemistry
Pyrroles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20810279
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.08.053