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首页> 外文期刊>Bioorganic and medicinal chemistry >Synthesis and evaluation of N-(benzofuran-5-y1) aromaticsulfonamide derivatives as novel HIF-1 inhibitors that possess anti-angiogenic potential
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Synthesis and evaluation of N-(benzofuran-5-y1) aromaticsulfonamide derivatives as novel HIF-1 inhibitors that possess anti-angiogenic potential

机译：Synthesis and evaluation of N-(benzofuran-5-y1) aromaticsulfonamide derivatives as novel HIF-1 inhibitors that possess anti-angiogenic potential

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摘要

Hypoxia-inducible factor-1 (HIF-1) as a key mediator in tumor metastasis, angiogenesis, and poor patient prognosis has been recognized as an important cancer drug target. A novel series of N-(benzofuran-5-yl) aromaticsulfonamide derivatives were synthesized and evaluated as HIF-1 inhibitor. Among these compounds, 7q exhibited specific inhibitory effects on HIF-1 by downregulating the expression of HIF-1 alpha under hypoxic conditions. It inhibited the HIF-1 transcriptional activity (IC50 = 12.5 +/- 0.7 mu M) and secretion of VEGF (IC50 = 18.8 mu M) in MCF-7 cells. Meanwhile, it also significantly suppressed hypoxia-induced migration of HUVEC cells in nontoxic concentrations. Additionally, tube formation assay demonstrated its anti-angiogenesis activity. Finally, the in vivo study indicated that compound 7q could retard angiogenesis in CAM model. These findings supported the HIF-1 inhibitory effect and anti-angiogenic potential of this class of compounds as HIF-1 inhibitor. (C) 2016 Published by Elsevier Ltd.

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