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有机硼化合物的药理活性及构效关系研究进展
引用本文:王震宇,周伟澄.有机硼化合物的药理活性及构效关系研究进展[J].药学进展,2009,33(6):241-246.
作者姓名:王震宇  周伟澄
作者单位:上海医药工业研究院创新药物与制药工艺国家重点实验室,上海,200437
基金项目:上海市科学技术委员会科研计划 
摘    要:综述具有药理活性的有机硼化合物及其构效关系的研究进展,包括硼酸类抗肿瘤化合物、含硼杂环类及硼烷类抗感染化合物、硼酸类凝血酶抑制剂以及硼酸类二肽基肽酶抑制剂等。并重点介绍了已上市抗肿瘤药物硼替佐米的药理作用机制、合成方法、药效及临床研究。

关 键 词:有机硼化合物  硼替佐米  药理活性  构效关系

Progress of Studies on Pharmacological Activity and Structure-activity Relationship of Organic Boron Compounds
WANG Zhen-yu,ZHOU Wei-cheng.Progress of Studies on Pharmacological Activity and Structure-activity Relationship of Organic Boron Compounds[J].Progress in Pharmaceutical Sciences,2009,33(6):241-246.
Authors:WANG Zhen-yu  ZHOU Wei-cheng
Institution:(State Key Lab of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China)
Abstract:The recent progress of studies on bioactive organic boron compounds, including anti-tumor agents, antibacterial agents, thrombin inhibitors and dipeptidyl peptidase IV inhibitors, and their structure-activity relationship was reviewed. The mechanism, synthesis, pharmacodynamics and clinic trial of the launched anti-tumor drug bortezomib were emphatically introduced.
Keywords:organic boron compound  bortezomib  pharmacological activity  structure-activity relationship
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