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2-Benzamido-N-(1H-benzodimidazol-2-yl)thiazole-4-carboxa mide derivatives as potent inhibitors of CK1 delta / epsilon
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2-Benzamido-N-(1H-benzodimidazol-2-yl)thiazole-4-carboxa mide derivatives as potent inhibitors of CK1 delta / epsilon
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Journal Article
2-Benzamido-N-(1H-benzodimidazol-2-yl)thiazole-4-carboxa mide derivatives as potent inhibitors of CK1 delta / epsilon
2012
Overview
In this study we identified two heterocyclic compounds (5 and 6) as potent and specific inhibitors of CK1 delta (IC sub(50) = 0.040 and 0.042 mu M, respectively). Whereas compound 5 exhibited fivefold higher affinity towards CK1 delta than to CK1 epsilon (IC sub(50) CK1 epsilon = 0.199 mu M), compound 6 also inhibited CK1 epsilon (IC sub(50) = 0.0326 mu M) in the same range as CK1 delta . Selected compound 5 was screened over 442 kinases identifying 5 as a highly potent and selective inhibitor of CK1 delta . X-ray analysis of 5 bound to CK1 delta demonstrated its binding mode. In addition, characterization of 5 and 6 in a cell biological approach revealed the ability of both compounds to inhibit proliferation of tumor cell lines in a dose and cell line specific manner. In summary, our optimizations lead to the development of new highly selective CK1 delta and epsilon specific inhibitors with biological activity.
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