2-Anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1
S Blanchard, CK Soh, CP Lee, A Poulsen… - Bioorganic & medicinal …, 2012 - Elsevier
Bioorganic & medicinal chemistry letters, 2012•Elsevier
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.
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.
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.
Elsevier
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