Evolution of a New Class of VEGFR-2 Inhibitors from Scaffold Morphing and Redesign

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• 作者：Nello Mainolfi ; Rajeshri Karki ; Fang Liu ; Karen Anderson
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：April 14, 2016
• 年：2016
• 卷：7
• 期：4
• 页码：363-367
• 全文大小：365K
• 年卷期：0
• ISSN：1948-5875

文摘

Anti-VEGF therapy is a clinically validated treatment for age-related macular degeneration (AMD). We have recently reported the discovery of oral VEGFR-2 inhibitors that are selectively distributed to the ocular tissues. Herein we report a further development of those compounds and in particular the validation of the hypothesis that aminoheterocycles such as aminoisoxazoles and aminopyrazoles could also function as effective “hinge” binding moieties leading to a new class of KDR (kinase insert domain containing receptor) inhibitors.