Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity

  • Bioorg Med Chem Lett. 2008 Jan 1;18(1):49-53. doi: 10.1016/j.bmcl.2007.11.015.
Zhijian Zhao  1 ,  Ronald G Robinson ,  Stanley F Barnett ,  Deborah Defeo-Jones ,  Raymond E Jones ,  George D Hartman ,  Hans E Huber ,  Mark E Duggan ,  Craig W Lindsley
Affiliations
  • 1. Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck & Co., PO Box 4, West Point, PA 19486, USA. [email protected]
PMID: 18054229 DOI: 10.1016/j.bmcl.2007.11.015
Abstract

This letter describes the development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved aqueous solubility (approximately 18 mg/mL) that translates into enhanced cell activity and Caspase-3 induction.

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