新型骨靶向抗肿瘤大黄酚衍生物的合成  

Synthesis of antitumor chrysophanol derivatives for new type bone-target drug

作　　者：陈虹[1] 王莹[2] 白淑芳[1] 冷玲[1] 程卯生[2] 吴可柱[1] 

机构地区：[1]中国人民武装警察部队医学院,天津300162 [2]沈阳药科大学制药工程学院,沈阳110016

出　　处：《天津药学》2008年第1期1-4,共4页Tianjin Pharmacy

基　　金：国家自然科学基金资助项目(No.30371682)

摘　　要：目的:利用大黄蒽醌类化合物的抗肿瘤作用与趋骨性,将大黄酚抗肿瘤药5-氟脲嘧啶及其衍生物连接,合成系列新型骨靶向抗肿瘤衍生物。方法:合成大黄酚衍生物,MTT法测定其对肿瘤细胞增殖的抑制作用,用羟基磷灰石吸附试验评价该类药物的体外骨亲和性。结果:合成了21个大黄酚衍生物均为新化合物。实验显示所有化合物均有不同程度的骨亲和性,大部分化合物的亲和性高于阳性对照药四环素。结论:大黄酚衍生物具有良好的骨亲和性。OBJECTIVE This paper focused on the antitumor effect and bone affinity of anthraquinone components in rhubarb. Starting material chrysophanol was linked to 5 - fluorouracil and its derivatives were prepared a new series derivatives of bone - target antitumor compounds. METHODS All synthetic compounds were carried out the bone affinity assay with hydroxyapative adsorption experiment and their antitumor activity screened with MTT in vitro. RESULTS 21 chrysophanol derivatives, new compounds, were synthesized. The result showed that the bone affinity of most synthetic compounds were better than tetracycline. CONCLUSION Chrysophanol derivatives have better bone affinity.

关 键 词：骨靶向 抗肿瘤 大黄酚 合成 

分 类 号：R979.1[医药卫生—药品] R123.1[医药卫生—药学]