Abstract
7-Methoxy-8-decynyl-benzolactam-V8 4 is synthesized using a catalytic asymmetric alkylation reaction as a key step. This compound shows potent activity to three PKC isozymes tested (Ki =45.6, 91.1, and 121.3 nM to PKCalpha, delta, and epsilon, respectively), indicating that introduction of a suitable substituent at the 7-position of 8-decynyl-benzolactam-V8 only slightly reduces the PKC binding affinity.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Binding, Competitive
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Carcinogens / chemical synthesis
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Carcinogens / metabolism
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / metabolism
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Inhibitory Concentration 50
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Isoenzymes / antagonists & inhibitors
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Lactams / chemical synthesis*
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Lactams / metabolism*
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Lyngbya Toxins / chemistry
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Phorbol 12,13-Dibutyrate / metabolism
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Protein Binding
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Protein Kinase C / antagonists & inhibitors*
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Protein Kinase C / metabolism*
Substances
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Carcinogens
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Enzyme Inhibitors
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Isoenzymes
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Lactams
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Lyngbya Toxins
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benzolactam V8-310
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teleocidins
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Phorbol 12,13-Dibutyrate
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Protein Kinase C