| 新型骨靶向抗肿瘤大黄酚衍生物的合成 |
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| 引用本文： | 陈虹,王莹,白淑芳,冷玲,程卯生,吴可柱.新型骨靶向抗肿瘤大黄酚衍生物的合成[J].天津药学,2008,20(1):1-4. |
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| 作者姓名： | 陈虹 王莹 白淑芳 冷玲 程卯生 吴可柱 |
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| 作者单位： | 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 |
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| 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.
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| 关 键 词： | 骨靶向 抗肿瘤 大黄酚 合成 骨靶向 抗肿瘤药 大黄酚 酚衍生物 合成系 drug new type derivatives chrysophanol antitumor 四环素 对照药 阳性 程度 新化合物 显示 实验 结果 亲和性 类药物 |
| 文章编号： | 1006-5687（2008）01-0001-04 |
| 收稿时间： | 2007-07-08 |
| 修稿时间： | 2007年7月8日 |
Synthesis of antitumor chrysophanol derivatives for new type bone-target drug |
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| Chen Hong,Wang Ying,Bai Shufang,Leng Ling,Cheng Maosheng,Wu Kezhu.Synthesis of antitumor chrysophanol derivatives for new type bone-target drug[J].Tianjin Pharmacy,2008,20(1):1-4. |
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| Authors: | Chen Hong Wang Ying Bai Shufang Leng Ling Cheng Maosheng Wu Kezhu |
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| Abstract: | 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. |
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| Keywords: | Bone- target Antitumor Chrysophanol Synthesis |
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