Diarylureas and Diarylamides with Oxazolo[5,4‐d]pyrimidine Scaffold as Angiogenesis Inhibitors |
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| Authors: | Ya‐Hui Deng Ji‐Ping Liu Yi‐Juan Cheng Yu Liu Li‐Ping Sun |
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| Affiliation: | 1. Jiangsu Key Laboratory of Drug Design & Optimization, China Pharmaceutical University, Nanjing, P. R. China;2. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, P. R. China;3. School of Life Science and Technology, China Pharmaceutical University, Nanjing, P. R. China;4. +86 2583271445+86 2583271160;5. +86 2583271445+86 2583271351 |
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| Abstract: | A series of oxazolopyrimidine‐based ureas and amides were designed, synthesized, and biologically evaluated for their antiproliferative and antiangiogenic activities. These compounds were identified to exhibit inhibitory activities against human umbilical vein endothelial cells (HUVEC) in vitro. Among these compounds, compound 22 effectively inhibited the migration and capillary‐like tube formation of human umbilical vein endothelial cells. It also exhibited a concentration‐dependent inhibition on capillary sprouting from the rat aorta rings. Preliminary mechanistic studies revealed that compound 22 suppressed protein kinases activation, by decreasing PI3K and ERK 1/2 phosphorylation. These results support the further investigation of this class of compounds as potential anticancer agents. |
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| Keywords: | Oxazolopyrimidines Ureas Amides Antiproliferative activity Antiangiogenesis Anticancer agents |
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