2. Academic Validation
  3. Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity

Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity

  • Bioorg Med Chem Lett. 2009 Feb 1;19(3):834-6. doi: 10.1016/j.bmcl.2008.12.017.
Yiwei Li 1,  Jun Liang,  Tony Siu,  Essa Hu,  Michael A Rossi,  Stanley F Barnett,  Deborah Defeo-Jones,  Raymond E Jones,  Ronald G Robinson,  Karen Leander,  Hans E Huber,  Sachin Mittal,  Nicholas Cosford,  Peppi Prasit
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., 770 Sumneytown Pike, WP14-2, West Point, PA 19486, USA. yiwei_li@merck.com
PMID: 19097777 DOI: 10.1016/j.bmcl.2008.12.017
Abstract

A series of [1,2,4]triazolo[3,4-f][1,6]naphthyridine allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been shown to have potent dual Akt1 and 2 cell potency. The representative compound 13 provided potent inhibitory activity against Akt1 and 2 in vivo in a mouse model.

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