具有表皮生长因子受体抑制活性的喹唑啉衍生物研究进展有机化学.pdfVIP

DOI: 10.6023/cjoc1108061 综述与进展 有机化学 Chinese Journal of Organic Chemistry REVIEW 具有表皮生长因子受体抑制活性的喹唑啉衍生物研究进展 张 英 王培义 胡德禹 金林红 杨 松* (贵州大学精细化工研究中心 绿色农药与农业生物工程国家重点实验室培育基地与教育部重点实验室 贵阳 550025) 摘要 综述了近十年来具有表皮生长因子受体(EGFR)抑制活性的喹唑啉衍生物的国内外研究进展, 按照喹唑啉环上不 同位置上的取代基类型分为四类, 介绍了化合物不同位置上取代基对此类化合物生物活性的影响, 并对其发展趋势和 应用前景作了展望. 关键词 表皮生长因子受体; 喹唑啉; 生物活性 Research Progress on Quinazoline Derivatives with Epidermal Growth Factor Receptor Inhibiting Bioactivity Zhang, Ying Wang, Peiyi Hu, Deyu Jin, Linhong Yang, Song* (State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering , Center for Research and Develop- ment of Fine Chemicals, Guizhou University, Guiyang 550025) Abstract The progress on quinazoline derivatives with epidermal growth factor receptor (EGFR) inhibiting bioactivity is reviewed in this paper. Quinazoline compounds are classified to four types according to different substituent groups at differ- ent ring position. The effects of substituent groups at different ring positions on the bioactivities are discussed. And the devel- opment tendency as well as the prospect of quinazoline derivatives as epidermal growth factor receptor tyrosine kinase inhibi- tors is summarized. Keywords epidermal growth factor receptor; quinazoline; bioactivity 表皮生长因子受体(EGFR)是一种受体酪氨酸激酶, 和埃罗替尼 OSI-774 (Tarceva)[17～22]等因其良好的抗癌 能激活并诱导癌细胞增殖、存活和迁移的信号路径, 从 活性已经商品化. 然而, 它们对癌细胞生长仅产生抑制 而导致各种表皮癌(如皮肤癌、乳腺癌、卵巢癌以及和