P-糖蛋白介导的多药耐药逆转剂的构效关系

被引:1
作者
李斌
杨纯正
机构
[1] 中国医学科学院!天津,中国协和医科大学血液学研究所!天津
关键词
P-糖蛋白; 多药耐药逆转剂; 构效关系;
D O I
10.13220/j.cnki.jipr.2000.05.003
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
寻找高效、低毒、专属性的多药耐药逆转剂是肿瘤化疗中亟需解决的难题。但是由于其作用机制的本质仍不清楚 ,这一问题的解决很困难。鉴于 P-糖蛋白的重要作用 ,研究其介导的多药耐药逆转剂的构效关系有助于揭示多药耐药性的产生及其逆转机制 ,设计理想的可用于临床的逆转剂。本文概述了对多药耐药逆转剂构效关系研究方法的认识 ,总结了近来出现的一些逆转剂特定的构效关系 ,并介绍了这方面的研究状况。
引用
收藏
页码:264 / 268
页数:5
相关论文
共 19 条
[1]  
Substituted 4acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity. Chiba P,Holzer W,Landau M,et al. Journal of Medicinal Chemistry . 1998
[2]  
The role of drug-lipid interactions in the biological activity of modulators of multidrug resistance. Wadkins RM,Houghton PJ. Biochimica et Biophysica Acta . 1993
[3]  
Structure-activity relationships of antineoplastic agents in multidrug resistance. Selassie CD,Hansch C,Khwaja TA. Journal of Medicinal Chemistry . 1990
[4]  
Flavonoid-related modulators of multidrug resistance: synthesis,pharmacological activity, and structure activity relationships. Ferte J,Kuhnel JM,Chapuis G,et al. Journal of Medicinal Chemistry . 1999
[5]  
Structure-activity relationship studies on benzofuran analogs of propafenone-type modulators of tumor cell multidrug resistance. Ecker G,Chiba P,Hizler M,et al. Journal of Medicinal Chemistry . 1996
[6]  
Structural requirements for activity of propafenone-type modulators in P-glycoprotein-mediated multidrug resistance. Chiba P,Ecker G,Schmid D,et al. Molecular Pharmacology . 1996
[7]  
Structure-activity relationship studies on modulators of the multidrug transporter P-glycoprotein - an overview. Ecker G,Chiba P. Wiener Klinische Wochenschrift . 1995
[8]  
Studies on propafenone-type modulators of multidrug resistance Ⅲ: variations on the nitrogen. Chiba P,Hitzler M,Richter E,et al. Quantitative Structure Activity Relationships . 1997
[9]  
Synthesis and in vitro multidrug resistance modulating activity of a series of dihydrobenzopyrans and tetrahydroquinolines. Hiessbock R,Wolf C,Richter E,et al. Journal of Medicinal Chemistry . 1999
[10]  
A combined Hansch Free-Wilson approach as predictive tool in QSAR studies on propafenone-type modulators of multidrug resistance. Tmej C,Chiba P,Huber M,et al. Archiv der Pharmazie . 1998