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

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

Affiliation

  • 1 Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck & Co., PO Box 4, West Point, PA 19486, USA. zhijian_zhao@merck.com
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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