Abstract
Synthetic routes towards highly substituted eight membered ring heterocycles fused to aryl rings such as the dibenzo[b,f]azocine system are still lacking. Herein, we present a convenient convergent synthetic route towards this heterocyclic class of compounds with possible variations at positions 4, 7, and 11. One member of a library of dibenzo[b,f]azocines with different substituents at position 11 was identified to inhibit protein kinase A activity (IC(50)=122microM) but not protein kinase C.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Azocines / chemical synthesis*
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Azocines / chemistry
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Azocines / pharmacology*
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Drug Evaluation, Preclinical
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Enzyme Activation / drug effects
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Molecular Structure
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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Protein Kinases / drug effects*
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Stereoisomerism
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Structure-Activity Relationship
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Substrate Specificity
Substances
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Azocines
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Protein Kinase Inhibitors
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Protein Kinases