环氧合酶-2抑制剂类抗肿瘤药物研究进展  

Advances in Research on COX-2 Inhibitors as Antitumor Drugs

作　　者：黄晓静[1] 姚和权[1] 吴晓明[1] 徐进宜[1] 

机构地区：[1]中国药科大学药学院药物化学教研室,南京210009

出　　处：《药学与临床研究》2013年第3期251-256,共6页Pharmaceutical and Clinical Research

基　　金：国家自然科学基金项目(No.81273377)

摘　　要：环氧合酶-2(COX-2)在肿瘤发生、发展、转移、凋亡抑制及促进血管生成等方面发挥着重要作用,已成为肿瘤防治的新靶点;越来越多的COX-2抑制剂及其衍生物进入到临床前和临床研究中,发挥着一定的抗肿瘤作用。本文对近年来以COX-2抑制剂,特别是以塞来昔布和尼美舒利为先导物进行结构修饰和改造,从而寻找新型抗肿瘤活性化合物的研究进展作一综述。As a new target for cancer chemotherapy,cyclooxygenase-2（COX-2） seems to associate with tumor initiation and progression,increased angiogenesis,tumor invasion and promotion of tumor cell resistance to apoptosis.Several preclinical and clinical studies have established potent anti-cancer activity of COX-2 inhibitors and their derivatives.In this paper,recent reports on the compounds with antitumor properties,which were synthesized via lead optimization of existing COX-2 inhibitors,especially celecoxib and nimesulide,are reviewed.

关 键 词：COX-2抑制剂 抗肿瘤 塞来昔布 尼美舒利 先导物优化 

分 类 号：R979.1[医药卫生—药品]