Dipartimento di Farmacia, University of Genoa, Viale Benedetto XV 3, 16132 Genova, Italy.
J Med Chem. 2012 Dec 27;55(24):10797-822. doi: 10.1021/jm301085w. Epub 2012 Nov 6.
The recent launch onto the market of five VEGFR inhibitors indicates the therapeutic value of these agents and the importance of the research in the field of angiogenesis inhibitors for future oncologic therapy. In this Perspective we briefly report the inhibitors that are in clinical use, while we dedicate two wider sections to the compounds that are in clinical trials and to the new derivatives appearing in the literature. We especially consider the medicinal chemistry aspect of the topic and report the structure-activity relationship studies and the binding mode of some inhibitors as well as the biological data of the compounds discovered in the past 5 years.
最近市场上推出的五种 VEGFR 抑制剂表明了这些药物的治疗价值,以及血管生成抑制剂在未来肿瘤治疗中的研究的重要性。在这篇观点文章中,我们简要地报告了目前临床应用的抑制剂,同时我们还专门用两个更大的部分来介绍临床试验中的化合物和文献中出现的新衍生物。我们特别考虑了这个主题的药物化学方面,并报告了一些抑制剂的结构-活性关系研究和结合模式,以及过去 5 年中发现的化合物的生物学数据。