College of Chemistry and Chemical Engineering, Fuzhou University, Fujian, 350108, P. R. China.
Med Chem. 2013 Jun 1;9(4):545-52. doi: 10.2174/1573406411309040008.
Eight new emodin derivatives that contain large conjugative system have been synthesized and their anticancer activities also have been evaluated. The result shows that large conjugative system can not enhance the anticancer activities of emodin derivatives, but the introduction of an alkylating center can make emodin derivative effective against cancer cell lines. Compound 12 has the highest alkylating ability, but its anticancer activity is not remarkable, which indicates that there is not a direct correlation between the chemical reactivity of the alkylating agent and the toxic effects.
已经合成了 8 种含有大共轭体系的新型大黄素衍生物，并对它们的抗癌活性进行了评价。结果表明，大共轭体系不能增强大黄素衍生物的抗癌活性，但引入烷化中心可以使大黄素衍生物对癌细胞系有效。化合物 12 具有最高的烷化能力，但它的抗癌活性并不显著，这表明烷化剂的化学反应性与毒性之间没有直接的相关性。
