You Y J, Ahn B Z
College of Pharmacy, Chungnam National University, Taejon, Korea.
Arch Pharm Res. 1998 Dec;21(6):738-43. doi: 10.1007/BF02976768.
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 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 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.
合成了36种带有含酯键不饱和烷基侧链的5,8-二甲氧基-1,4-萘醌衍生物，并测试了它们对L1210细胞的细胞毒性活性以及对携带S-180细胞的ICR小鼠的抗肿瘤活性。可以看出，R1为甲基和丙基的萘醌（IV1-24），用烯丙酰基取代烷酰基后其细胞毒性并未增强。相反，在R1 =己基的化合物（IV25-36）上引入烯丙酰基部分导致其细胞毒性增强。用烯丙酰基取代烷酰基通常会增加携带S-180细胞小鼠的T/C值。
