目前抗血管生成治疗是抗肿瘤研究的热点。血管内皮生长因子（VEGF）是刺激血管生成的重要因子之一，血管内皮生长因子受体（VEGFR）在肿瘤新生血管中高表达，因此成为肿瘤靶向治疗的理想靶点。以VEGF、VEGFR为靶点的抗肿瘤药物除了常见的单克隆抗体药物阿伐斯汀外，小分子抑制剂舒尼替尼、索拉非尼等也已经广泛使用；另外，一些具有上市潜力的药物，如范得他尼、西地尼布、瓦他拉尼、阿西替尼等也值得关注。已上市和正在进行临床研究的VEGFR小分子抑制剂按结构大致分为6类：喹啉及喹唑啉类、哒嗪类、吲唑类、咪唑和吡咯嘧啶类、吲哚类和其他结构等。对VEGF、VEGFR的生物学功能，其代表性的小分子抑制剂研究进行综述。

Recently, the anti-angiogenic therapy is a hot focus for antitumor research. The vascular endothelial growth factor (VEGF) is one of the most important angiogenesis stimulators. The vascular endothelial growth factor receptor (VEGFR) is high expressed in the new vessels of tumor tissues, so the antiangiogenic therapy aiming at VEGFR becomes an ideal treatment method. Besides the monoclonal antibody drug Avastin, the small-molecule inhibitors such as sunitinib and sorafenib are already widely used in the antitumor therapy aimed at VEGF and VEGFR. Moreover, it is also worth attention to some clinical drugs with potential market acceptance (vandetanib, cediranib, vatalanib, axtinib, et al). For the drugs on the market and VEGFR-targeted small-molecule inhibitors in clinical study, we roughly divided them into six kinds on structures including quinoline and quinazoline, pyridazine, indazole, imidazole, pyrrolo[2,3-d]pyrimidine, indole, and others. The recent studies of the biologyical function of VEGF and VEGFR and their representative small-molecule inhibitors are reviewed in this paper.

国家重大新药创制专项（2011ZX09401-009）