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A series of phenanthrene alkaloids was synthesized from (+)-dicentrine by degradation with ethyl chloroformate in pyridine, base hydrolysis, and N-alkylation. The antitumor activities of these (+)-dicentrine analogues were investigated. Compounds 3, 4, 7, and 8 exhibited strong cytotoxic effects in colon adenocarcinoma, hepatoma, and epidermoid carcinoma cell lines and had more potential than (+)-dicentrine. The weaker activity of compounds 5 and 6 indicated that the elongation of alkyl chain on nitrogen atom reduced the activity.

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