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KMID : 0043319980210060738
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Archives of Pharmacal Research
1998 Volume.21 No. 6 p.738 ~ p.743
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6-(1-Alkenoyloxyalkyl)-5,8-dimethoxy-1,4-naphthoquinone Derivatives:Synthesis and Evaluation of Antitumor Activity
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You Young-Jae
Ahn Byung-Zun
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Abstract
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Thirty six 5,8-dimethoxy-1,4-naphthoquinone derivatives, which bear unsaturated alkyl side chain with ester bond, were synthesized and tested cytotoxic activity on L1210 cells a nd antitumor activity against ICR mice bearing S-180 cells. It could be recognized that the cytotoxicities of naphthoquinones with R1, being methyl and propyl (IV1~24) were not enhanced by replacing the alkanoyls with alkenoyls. In contrast, the introduction of the alkenoyl moieties on the compounds with =hexyl (IV25~36) resulted in the enhancement of their cytotoxicities. Replacement of alkanoyl group with an alkenoyl group generally increased the T/C value of the mice bearing S-180 cells.
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KEYWORD
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6-Substituted 5, 8-dimethoxy-1, 4-naphthoquinone, Esters of alkenoic acids, Anitiumor activity
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