2-anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1.
Bioorg Med Chem Lett
; 22(8): 2880-4, 2012 Apr 15.
Article
in En
| MEDLINE
| ID: mdl-22437109
ABSTRACT
A series of 2-anilino substituted 4-aryl-8H-purines were prepared as potent inhibitors of PDK1, a serine-threonine kinase thought to play a role in the PI3K/Akt signaling pathway, a key mediator of cancer cell growth, survival and tumorigenesis. The synthesis, SAR and ADME properties of this series of compounds are discussed culminating in the discovery of compound 6 which possessed sub-micromolar cell proliferation activity and 65% oral bioavailability in mice.
Full text:
1
Database:
MEDLINE
Main subject:
Purines
/
Protein Serine-Threonine Kinases
/
Small Molecule Libraries
/
Aniline Compounds
Limits:
Animals
/
Humans
Language:
En
Year:
2012
Type:
Article