ATROPISOMERISM FOR INCREASED KINASE INHIBITOR SELECTIVITY
First Claim
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1. A method of inhibiting the growth of cancer cells comprising administering to a mammal having cancer a therapeutically effective amount of an atropisomerically stable atropisomer of Formula I or an enantiomer or salt thereof:
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Abstract
The invention provides a series of conformationally stable kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly interconverting parent compounds.
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20 Claims
- 1. A method of inhibiting the growth of cancer cells comprising administering to a mammal having cancer a therapeutically effective amount of an atropisomerically stable atropisomer of Formula I or an enantiomer or salt thereof:
- 17. A method of inhibiting the growth of cancer cells comprising administering to a mammal having cancer a therapeutically effective amount of an atropisomerically stable atropisomer comprising Formula IA or an enantiomer or salt thereof:
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20. A method to modulate the selectivity of a promiscuous kinase inhibitor that comprises a rotatable phenyl moiety comprising adding an atropisomerism rotational blocking moiety to the phenyl moiety of the inhibitor, thereby increasing or decreasing the selectivity of the kinase inhibitor for specific kinases.
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