612848-74-5Relevant academic research and scientific papers
INHIBITORS OF AKT ACTIVITY
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Page/Page column 35, (2008/06/13)
The instant invention provides for canthine analogs that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
Synthesis and biological evaluation of unnatural canthine alkaloids
Lindsley, Craig W.,Bogusky, Michael J.,Leister, William H.,McClain, Ray T.,Robinson, Ronald G.,Barnett, Stanley F.,Defeo-Jones, Deborah,Ross III, Charles W.,Hartman, George D.
, p. 2779 - 2782 (2007/10/03)
Employing a 'one-pot' microwave-assisted protocol, unnatural canthine alkaloids with biological activities beyond the natural products have been prepared. This report describes unnatural canthine alkaloid analogs as selective, allosteric Akt kinase inhibitors.
Allosteric Akt (PKB) inhibitors: Discovery and SAR of isozyme selective inhibitors
Lindsley, Craig W.,Zhao, Zhijian,Leister, William H.,Robinson, Ronald G.,Barnett, Stanley F.,Defeo-Jones, Deborah,Jones, Raymond E.,Hartman, George D.,Huff, Joel R.,Huber, Hans E.,Duggan, Mark E.
, p. 761 - 764 (2007/10/03)
This letter describes the development of two series of potent and selective allosteric Akt kinase inhibitors that display an unprecedented level of selectivity for either Akt1, Akt2 or both Akt1/Akt2. An iterative analog library synthesis approach quickly provided a highly selective Akt1/Akt2 inhibitor that induces apoptosis in tumor cells and inhibits Akt phosphorylation in vivo.
