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Design and synthesis of VEGFR-2 inhibitors based on oleanolic acid moiety
Yan-Ling Song1, Peng-Bo Zhang1, Rui-Jie Tong1
1Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China.
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 I and I 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. [Formula: see text].
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