Abstract
To investigate the role of the amide hydrogen of (-)-indolactam-V (1) and benzolactam-V8's on protein kinase C (PKC) binding and tumor promotion, 8-decylbenzolactone-V8 (6), a new lactone analogue of 8-decylbenzolactam-V8 (4), was synthesized from 2-nitrophenylpyruvic acid (7) in 11 steps. The PKC binding ability and tumor-promoting activities in vitro of 6 were much lower than those of 1 and 4, suggesting that the amide hydrogen of 1 and benzolactam-V8's plays a critical role in tumor promotion. However, it is noteworthy that 6 showed significant selectivity in the PKC isozyme surrogate binding.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antigens, Viral / metabolism
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Carcinogens / chemistry*
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Carcinogens / metabolism
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Carcinogens / pharmacology
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Humans
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Hydrogen / chemistry
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Indoles / chemistry*
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Indoles / metabolism*
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Indoles / pharmacology
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Kinetics
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Lactams / chemistry*
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Lactams / metabolism*
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Lactams / pharmacology
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Magnetic Resonance Spectroscopy
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Molecular Structure
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Protein Binding
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Protein Isoforms / metabolism
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Protein Kinase C / chemistry
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Protein Kinase C / metabolism*
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Radioligand Assay
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Superoxides / metabolism
Substances
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Antigens, Viral
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Carcinogens
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Epstein-Barr virus early antigen
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Indoles
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Lactams
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Protein Isoforms
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benzolactam V8-310
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Superoxides
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Hydrogen
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indolactam V
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Protein Kinase C