6-(1-Alkenoyloxyalkyl)-5,8-dimethoxy-1,4-naphthoquinone derivatives: Synthesis and evaluation of antitumor activity
6-(1-Alkenoyloxyalkyl)-5,8-dimethoxy-1,4-naphthoquinone derivatives: Synthesis and evaluation of antitumor activity
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DOI：
10.1007/bf02976768
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发表时间：
1998-12
影响因子：
6.7
通讯作者：
Y. You;B. Ahn
中科院分区：
文献类型：
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作者：
Y. You;B. Ahn
合成了36个含酯键不饱和烷基侧链的5，8-二甲氧基-1，4-萘醌类化合物，并测定了它们对L1210细胞的杀伤活性和对荷S-180细胞的ICR小鼠的抗肿瘤活性。可以认识到，用烷酰取代烷酰并不能提高R1为甲基和丙基的萘醌(IV1∼24)的细胞毒性。相反，在具有R1=己基(IV25∼36)的化合物上引入烯基基官能团导致它们的细胞毒性增强。用烯基取代烷酰基可显著提高荷瘤小鼠的T/C值。
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 and antitumor activity against ICR mice bearing S-180 cells. It could be recognized that the cytotoxicities of naphthoquinones with R1being 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 R1=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.