Hodnett E M, Wongwiechintana C, Dunn W J, Marrs P
J Med Chem. 1983 Apr;26(4):570-4. doi: 10.1021/jm00358a021.
Twelve 1,4-naphthoquinones have been tested against the ascitic form of sarcoma 180 in Swiss mice. Statistical analysis shows that the most important molecular parameter determining their effectiveness in prolonging the life of mice bearing this tumor is their redox potentials. Although the toxicities of the compounds are also related to the redox potentials in the same way, the therapeutic indexes can be increased by adding substituents of greater lipophilicity. The naphthoquinones differ greatly in antitumor activities and may inhibit the growth of malignant cells by different mechanisms.
已对12种1,4 - 萘醌针对瑞士小鼠的肉瘤180腹水型进行了测试。统计分析表明,决定它们延长患该肿瘤小鼠寿命有效性的最重要分子参数是其氧化还原电位。尽管这些化合物的毒性也以同样的方式与氧化还原电位相关,但通过添加亲脂性更强的取代基可以提高治疗指数。萘醌的抗肿瘤活性差异很大,可能通过不同机制抑制恶性细胞的生长。