893422-47-4Relevant articles and documents
Allosteric inhibitors of Akt1 and Akt2: A naphthyridinone with efficacy in an A2780 tumor xenograft model
Bilodeau, Mark T.,Balitza, Adrienne E.,Hoffman, Jacob M.,Manley, Peter J.,Barnett, Stanley F.,Defeo-Jones, Deborah,Haskell, Kathleen,Jones, Raymond E.,Leander, Karen,Robinson, Ronald G.,Smith, Anthony M.,Huber, Hans E.,Hartman, George D.
supporting information; experimental part, p. 3178 - 3182 (2009/04/11)
A series of naphthyridine and naphthyridinone allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been optimized to have potent dual activity against the activated kinase as well as the activation of Akt in cells. One molecu
Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors
Siu, Tony,Liang, Jun,Arruda, Jeannie,Li, Yiwei,Jones, Raymond E.,Defeo-Jones, Deborah,Barnett, Stanley F.,Robinson, Ronald G.
scheme or table, p. 4186 - 4190 (2009/04/07)
This paper describes the improvement of cell potency in a class of allosteric Akt 1 and 2 inhibitors. Key discoveries include identifying the solvent exposed region of the molecule and appending basic amines to enhance the physiochemical properties of the
INHIBITORS OF AKT ACTIVITY
-
, (2010/11/25)
The instant invention provides for substituted naphthyridine compounds 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.
INHIBITORS OF AKT ACTIVITY
-
Page/Page column 42; 45-46, (2010/11/08)
The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.