大黄素衍生物的合成及抗癌活性

通过对大黄素的C6位进行化学修饰, 设计合成了7个含氮杂环的大黄素衍生物和3个含季铵盐基团的大黄素衍生物. 通过红外光谱、 ¹H NMR和质谱表征了所制备化合物的结构, 并测试了它们对白血病细胞Molt-4和淋巴瘤细胞CA46的体外抑制活性. 其中化合物8, 9a+9b, 20a, 20b和20c均显示出比大黄素更高的抗癌活性, 表明苯并咪唑基团和季铵盐基团是大黄素提高抗癌活性的有效药效团.

Synthesis and Anticancer Activity Evaluation of Derivatives of Emodin

In order to improve the anticancer activity of emodin, seven emodin derivatives containing nitrogen heterocycle and three emodin derivatives containing quaternary ammonium salt were designed and synthesized by suitable modification at C6 position of emodin, their structures were characterized by IR, 1H NMR and MS and their activities against leukemia cell line Molt-4 and lymphoma cell line CA46 in vitro were tested by MTT method. Thereinto, compounds 8, 9a+9b, 20a, 20b and 20c show higher anticancer activities than emodin, which indicates that benzimidazole and quaternary ammonium salt are good pharmacophores for the anticancer activity of emodin. We propose to introduce many such pharmacophores into emodin to improve the anticancer activity of emodin in further.