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目的改善大黄素衍生物的水溶性问题,以期得到一些抗白血病活性较好的大黄素衍生物。方法以大黄素为原料,经过羟基保护、N-溴代丁二酰亚胺(NBS)参与的溴代反应、与叔胺成盐反应制得目标化合物。结果与结论合成了11个未见文献报道的大黄素衍生物,其结构经IR、1H-HNMR谱和元素分析确证。化合物3h、3i和3j对白血病细胞K562和Jurkat细胞株有较好的活性。
Objective To improve the water-soluble emodin derivatives, in order to obtain some anti-leukemia better emodin derivatives. Methods Emodin was used as raw material to make the target compound through the hydroxyl protection, the bromination reaction involving N-bromosuccinimide (NBS) and the salt formation reaction with tertiary amine. RESULTS AND CONCLUSION Eleven emodin derivatives were synthesized and their structures were confirmed by IR, 1H-NMR and elemental analysis. Compounds 3h, 3i and 3j have good activity on leukemia K562 and Jurkat cell lines.