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Rapid assembly of diverse and potent allosteric Akt inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Mar 15; Vol. 18 (6), pp. 2211-4. Date of Electronic Publication: 2007 Oct 17. - Publication Year :
- 2008
-
Abstract
- This paper describes the rapid assembly of four different classes of potent Akt inhibitors from a common intermediate. Among them, a pyridopyrimidine series displayed the best intrinsic and cell potency against Akt1 and Akt2. This series also showed a promising pharmacokinetic profile and excellent selectivity over other closely related kinases.
- Subjects :
- Animals
Apoptosis drug effects
Caspases metabolism
Dogs
Female
Humans
Male
Metabolic Clearance Rate
Molecular Structure
Ovarian Neoplasms metabolism
Phosphorylation drug effects
Prostatic Neoplasms metabolism
Protein Kinase Inhibitors pharmacokinetics
Proto-Oncogene Proteins c-akt metabolism
Structure-Activity Relationship
TNF-Related Apoptosis-Inducing Ligand pharmacology
Tumor Cells, Cultured
Allosteric Site
Ovarian Neoplasms drug therapy
Prostatic Neoplasms drug therapy
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors pharmacology
Proto-Oncogene Proteins c-akt antagonists & inhibitors
Pyridines chemistry
Pyrimidines chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18296048
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.10.023