Literature DB >> 18550373

The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity.

Tony Siu1, Yiwei Li, Johnny Nagasawa, Jun Liang, Lida Tehrani, Peter Chua, Raymond E Jones, Deborah Defeo-Jones, Stanley F Barnett, Ronald G Robinson.   

Abstract

This letter details the attenuation of hERG in a class of Akt inhibitors through heteroatom insertions into aromatic rings. The development of a cell-active dual Akt 1 and 2 inhibitors devoid of hERG activity is discussed using structure-activity relationships.

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Year:  2008        PMID: 18550373     DOI: 10.1016/j.bmcl.2008.05.084

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Inhibition of Akt with small molecules and biologics: historical perspective and current status of the patent landscape.

Authors:  Margrith E Mattmann; Sydney L Stoops; Craig W Lindsley
Journal:  Expert Opin Ther Pat       Date:  2011-06-02       Impact factor: 6.674

2.  Core Replacements in a Potent Series of VEGFR-2 Inhibitors and Their Impact on Potency, Solubility, and hERG.

Authors:  Nello Mainolfi; James Powers; Erik Meredith; Jason Elliott; Karl G Gunderson; Stephen Poor; Fang Liu; Karen Anderson
Journal:  ACS Med Chem Lett       Date:  2016-03-16       Impact factor: 4.345

3.  A 2D-QSAR and Grid-Independent Molecular Descriptor (GRIND) Analysis of Quinoline-Type Inhibitors of Akt2: Exploration of the Binding Mode in the Pleckstrin Homology (PH) Domain.

Authors:  Noreen Akhtar; Ishrat Jabeen
Journal:  PLoS One       Date:  2016-12-30       Impact factor: 3.240

  3 in total

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