Abstract
A series of 1,3-disubstituted pyrrolo[2,3-b]quinoxalines has been designed for the potential inhibition of PDE4 without inhibiting luciferase. A ligand/PTC (phase transfer catalyst) free intramolecular Heck cyclization strategy was used to prepare these compounds, some of which showed significant inhibition of PDE4B (IC50≈ 5-14 μM) and growth inhibition of oral cancer cells (CAL 27) but not inhibition of luciferase in vitro. They also showed acceptable safety profiles but no apoptosis in zebrafish embryos.
MeSH terms
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Animals
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Binding Sites
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Catalysis
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Cell Proliferation / drug effects
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Embryo, Nonmammalian / drug effects
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Enzyme Activation / drug effects
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Humans
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Ligands
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Luciferases / metabolism
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Molecular Structure
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Mouth Neoplasms / drug therapy*
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Phosphodiesterase 4 Inhibitors / chemical synthesis*
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Phosphodiesterase 4 Inhibitors / chemistry
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Phosphodiesterase 4 Inhibitors / pharmacology*
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Quinoxalines / chemical synthesis*
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Quinoxalines / chemistry
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Quinoxalines / pharmacology*
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Zebrafish / embryology
Substances
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Ligands
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Phosphodiesterase 4 Inhibitors
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Quinoxalines
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Luciferases