11-脱氧18α-和18β-甘草次酸类抗癌复合物的制备和结构表征

doi:A

天然产物研究与开发 ›› 2012, Vol. 24 ›› Issue (5): 648-652.doi: A

11-脱氧18α-和18β-甘草次酸类抗癌复合物的制备和结构表征

木合布力•阿布力孜，闵杰，郑大成，马红艳，热娜•卡斯木*

新疆医科大学药学院药物化学有机教研室，乌鲁木齐 830011

收稿日期:2011-06-27 出版日期:2012-05-25 发布日期:2012-06-12
基金资助:
国家自然科学基金项目（30960461）资助。

Preparation and Characterization of Anticancer Conjugates 11-deoxo-18α and 18β-Glycyrrhetinic Acid Derivatives

Mourboul ABLISE, MIN Jie, ZHENG Da-cheng, MA Hong-yan, Rena KASIM*

Department of Medicinal and Organic Chemistry, College of Pharmacy, Xinjiang Medical University, Urumqi 830011, China

Received:2011-06-27 Online:2012-05-25 Published:2012-06-12

摘要/Abstract

摘要： 为寻找新型肝靶向抗癌前药，将具有肝靶向特征的天然分子甘草次酸的半合成衍生物与抗癌药环磷酰胺的活性代谢物氮芥磷酰二氯偶联制成11-脱氧甘草次酸类两个目标化合物和7个中间体。化合物的化学结构用常规光谱分析法进行鉴定，对合成工艺、理化性质和光谱特征进行系统描述。本研究对甘草次酸类新型肝靶向抗癌前药的药理活性筛选奠定基础。

关键词: 11-脱氧甘草次酸类；氢化还原；构型转化；11-脱氧18&alpha, -和18&beta, -甘甲磷酰氮芥酯；结构表征

Abstract: To obtain new anticancer prodrugs on the bases of hepatocell targeting property of natural product glycyrrhetinic acid and its semi-synthetic derivatives, we prepared two conjugated products by the route of coupling 11-deoxo-glycyrrhetinic acid derivatives with nitrogen mustard dichlorophosphate (the active metabolite of anticancer drug cyclophosphamide). The structure of two target compounds and 7 intermediate products was characterized by routine spectrometric methods; the technologies of preparation and physical-chemical properties were studied. This work may provide substantial bases for further pharmacological screening of new anticancer products from glycyrrhetinic acid derivatives with hep-directing potency.

Key words: 18β-glycyrrhetinic acid, chemical reduction, epimerization, 11-deoxo-18&alpha, and 18β-methy glycyrrhetinic acid-phosphorus nitrogen mustard ester, characterization

中图分类号:

R284.2

木合布力阿布力孜，闵杰，郑大成，马红艳，热娜卡斯木. 11-脱氧18α-和18β-甘草次酸类抗癌复合物的制备和结构表征[J]. 天然产物研究与开发, 2012, 24(5): 648-652.

Mourboul ABLISE, MIN Jie, ZHENG Da-cheng, MA Hong-yan, Rena KASIM. Preparation and Characterization of Anticancer Conjugates 11-deoxo-18α and 18β-Glycyrrhetinic Acid Derivatives[J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2012, 24(5): 648-652.

参考文献

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11-脱氧18α-和18β-甘草次酸类抗癌复合物的制备和结构表征

Preparation and Characterization of Anticancer Conjugates 11-deoxo-18α and 18β-Glycyrrhetinic Acid Derivatives

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