Abstract

In this study, twenty-four oleanolic acid (OA) derivatives were rationally designed based on molecule docking studies and their VEGFR-2 inhibitory activities were tested by Homogeneous time-resolved fluorescence (HTRF) method in vitro. All of the synthesized compounds were identified as new compounds, and the structures of these compounds were determined by ¹H-NMR and ESI-MS. In the screening for VEGFR-2 inhibitors, compounds I₆ and I₇ exhibited excellent inhibitory effect. The results indicated that insertion of phenylurea group with a linker at position C-28 of OA can increase the activity against VEGFR-2 significantly.

中文翻译：

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基于齐墩果酸部分的VEGFR-2抑制剂的设计与合成

摘要

在这项研究中，基于分子对接研究合理设计了二十四种齐墩果酸（OA）衍生物，并通过均相时间分辨荧光（HTRF）方法体外测试了其对VEGFR-2的抑制活性。所有合成的化合物均被鉴定为新化合物，并通过¹ H-NMR和ESI-MS确定了这些化合物的结构。在筛选VEGFR-2抑制剂时，化合物I ₆ 和I ₇ 表现出优异的抑制作用。结果表明，在OA的C-28位插入具有连接基的苯基脲基团可以显着提高针对VEGFR-2的活性。