【摘 要】
：
A series of N-(4-hydroxy-3-mercaptonaphthalen-1-yl)amides were synthesized and investigated for their antiangiogenic activity by application of tube formation assay using HUVECs1,the rat thoracic aort
【机 构】
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Department of Medicinal Chemistry,School of Pharmaceutical Sciences,Shandong University,44 West Cult
【出 处】
：
第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
A series of N-(4-hydroxy-3-mercaptonaphthalen-1-yl)amides were synthesized and investigated for their antiangiogenic activity by application of tube formation assay using HUVECs1,the rat thoracic aorta rings test2 and kinase inhibition assay3.Among these compounds,compound 4 inhibited in vitro angiogenesis markedly in both tube formation assay and the rat thoracic aorta rings test by treatment with which at 0.1 and 1μM,respectively.Further kinase assay study showed that compound 4 had good VEGFR2,ALK,AKT1 and ABL inhibitory activity and moderate EGFR and PDGFR-β inhibitory activities.The data support the further investigation of this class of compounds as potential antiangiogenic and anticancer therapeutics.
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