Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2

  • Bioorg Med Chem Lett. 2011 Sep 15;21(18):5191-6. doi: 10.1016/j.bmcl.2011.07.056.
Kate S Ashton  1 ,  David J St Jean Jr ,  Steve F Poon ,  Matthew R Lee ,  John G Allen ,  Shiwen Zhang ,  Julie A Lofgren ,  Xiaoling Zhang ,  Christopher Fotsch ,  Randall Hungate
Affiliations
  • 1. Chemistry Research and Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA. [email protected]
PMID: 21824779 DOI: 10.1016/j.bmcl.2011.07.056
Abstract

Through the analysis of X-ray crystallographic information and previous SAR studies, a novel series of protein kinase B (PKB/Akt) inhibitors was developed. The compounds showed nanomolar inhibition of Akt1 and were selective against cyclin-dependent kinase 2 (CDK2).

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