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  • Title: Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors.
    Author: Woods KW, Fischer JP, Claiborne A, Li T, Thomas SA, Zhu GD, Diebold RB, Liu X, Shi Y, Klinghofer V, Han EK, Guan R, Magnone SR, Johnson EF, Bouska JJ, Olson AM, de Jong R, Oltersdorf T, Luo Y, Rosenberg SH, Giranda VL, Li Q.
    Journal: Bioorg Med Chem; 2006 Oct 15; 14(20):6832-46. PubMed ID: 16843670.
    Abstract:
    A series of heteroaryl-pyridine containing inhibitors of Akt are reported. The synthesis and structure-activity relationships are discussed, leading to the discovery of a indazole-pyridine analogue (K(i)=0.16 nM). These compounds bind in the ATP binding site, are potent, ATP competitive, and reversible inhibitors of Akt activity. No selectivity amongst the Akt isoforms is observed for this analogue, but there is good selectivity against an panel of other kinases. It is least selective for other members of the AGC family of kinases but is nonetheless 40-fold selective for Akt over PKA. The compound shows cellular activity and significantly slows tumor growth in vivo.
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