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  • Title: Azole-based inhibitors of AKT/PKB for the treatment of cancer.
    Author: Zeng Q, Allen JG, Bourbeau MP, Wang X, Yao G, Tadesse S, Rider JT, Yuan CC, Hong FT, Lee MR, Zhang S, Lofgren JA, Freeman DJ, Yang S, Li C, Tominey E, Huang X, Hoffman D, Yamane HK, Fotsch C, Dominguez C, Hungate R, Zhang X.
    Journal: Bioorg Med Chem Lett; 2010 Mar 01; 20(5):1559-64. PubMed ID: 20137943.
    Abstract:
    Through a combination of screening and structure-based rational design, we have discovered a series of N(1)-(5-(heterocyclyl)-thiazol-2-yl)-3-(4-trifluoromethylphenyl)-1,2-propanediamines that were developed into potent ATP competitive inhibitors of AKT. Studies of linker strand-binding adenine isosteres identified SAR trends in potency and selectivity that were consistent with binding interactions observed in structures of the inhibitors bound to AKT1 and to the counter-screening target PKA. One compound was shown to have acceptable pharmacokinetic properties and to be a potent inhibitor of AKT signaling and of in vivo xenograft tumor growth in a preclinical model of glioblastoma.
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