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

Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., 3535 General Atomics Court, San Diego, CA 92129, USA.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.42). 08/2008; 18(14):4186-90. DOI: 10.1016/j.bmcl.2008.05.085
Source: PubMed


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.

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