Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors

ArticleinBioorganic & medicinal chemistry letters 18(14):4186-90 · August 2008with4 Reads
Impact Factor: 2.42 · DOI: 10.1016/j.bmcl.2008.05.085 · Source: PubMed

    Abstract

    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 molecules. Findings from the structure-activity relationships are discussed.