Diarylureas and Diarylamides with Oxazolo[5,4-d]pyrimidine Scaffold as Angiogenesis Inhibitors
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- 作者：Ya-Hui Deng ; Ji-Ping Liu ; Yi-Juan Cheng ; Yu Liu and Li-Ping Sun
- 刊名：Chemistry & Biodiversity
- 出版年：2016
- 出版时间：September 2016
- 年：2016
- 卷：13
- 期：9
- 页码：1230-1239
- 全文大小：2357K
- ISSN：1612-1880
文摘
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.