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Substituted 1,4-naphthoquinones vs. the ascitic sarcoma 180 of mice

作者:Ernest M. Hodnett, Chinda Wongwiechintana, William Jackson Dunn, P. S. MARRS · 发表于:Journal of Medicinal Chemistry · 年份:1983 · DOI:10.1021/jm00358a021 · 被引用次数:87 · 研究领域:Bioactive Compounds and Antitumor Agents、Cancer therapeutics and mechanisms、Organic Chemistry Cycloaddition Reactions

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.