大黄素甲醚衍生物的合成及抗肿瘤活性的研究

Synthesis and Anti-tumor Activities of Pyhscion Derivatives

以天然大黄素甲醚为母体,经过化学修饰得到两种大黄素甲醚的衍生物。通过1HNMR、IR、MS和元素分析确定其结构。选择血管内皮癌(Ks),口腔底癌(KBv)和乳腺癌(MCF-7/s)3种人癌细胞株,采用标准MTT法测定了大黄素甲醚及其衍生物的细胞毒性。结果表明,6-甲基-1,8-二[[2-(二甲基氨基)乙基]-氨基]-3-甲氧基-9,10-蒽醌对Ks和KBv表现出很强的细胞毒性。

Two new pyhseion derivatives were synthesized. The structures were confirmed by l HNMR, IR, MS and elemental analyses. Their cytotoxicity in vitro against three tumor cell lines（ Ks, KBv, MCF-7/s） were evaluated by standard MTT assay. The-results indicated that 6-methy-1,8-di-[ [2-（ dimethyl- aminomethy） ethyl-amino]-3-methoxy-9,10-anthraquonone dis- played much better potent cytotoxieity against Ks and KBv cell lines.