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.%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.
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