Abstract
A series of shinjulactone C (1) derivatives (2-8) were synthesized and evaluated for their anti-tumor promoting effects against Epstein-Barr virus early antigen activation introduced by 12-O-tetradecanoylphorbol-13-acetate in Raji cells. The succinate and 3',3'-dimethylsuccinate derivatives of 1 exhibited higher inhibitory effects than 1. From the point of view of structure-activity relationships, the succinate derivatives (2, 4) demonstrated better potency than the glutarate derivatives (3, 5-8). As substituted moieties of 3'-position became bulky, the inhibitory effects of the glutarate derivatives (7, 8) significantly decreased.
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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Antineoplastic Agents, Phytogenic / isolation & purification
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Antineoplastic Agents, Phytogenic / pharmacology*
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Chemoprevention
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Dose-Response Relationship, Drug
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Epstein-Barr Virus Infections / prevention & control*
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Herpesvirus 4, Human / drug effects*
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Herpesvirus 4, Human / physiology
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Humans
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Inhibitory Concentration 50
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Lactones / isolation & purification
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Lactones / pharmacology*
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Plant Bark / chemistry
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Quassins / pharmacology*
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Structure-Activity Relationship
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Tetradecanoylphorbol Acetate / pharmacology
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Tumor Cells, Cultured
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Virus Activation / drug effects*
Substances
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Antigens, Viral
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Antineoplastic Agents, Phytogenic
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Epstein-Barr virus early antigen
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Lactones
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Quassins
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Tetradecanoylphorbol Acetate