Novel 1,4-benzoxazine and 1,4-benzodioxine inhibitors of angiogenesis

被引：11

作者：

Ilic, Milos ^{[2
]}

Ilas, Janez ^{[2
]}

Dunkel, Petra ^{[3
]}

Matyus, Peter ^{[3
]}

Bohac, Andrej ^{[4
]}

Liekens, Sandra ^{[1
]}

Kikelj, Danijel ^{[2
]}

机构：

[1] Catholic Univ Louvain, Rega Inst Med Res, B-3000 Louvain, Belgium

[2] Univ Ljubljana, Fac Pharm, SI-1000 Ljubljana, Slovenia

[3] Semmelweis Univ, Dept Organ Chem, H-1092 Budapest, Hungary

[4] Comenius Univ, Fac Nat Sci, Dept Organ Chem, Bratislava 84215, Slovakia

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 58卷

关键词：

Angiogenesis; Thrombin; GPIIb/IIIa antagonist; Vascular endothelial growth factor; ANTITHROMBOTIC COMPOUNDS; THROMBIN; METASTASIS; GROWTH; MECHANISM; THERAPY; CANCER; PI-88; CELLS;

D O I：

10.1016/j.ejmech.2012.10.001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Esters of 1,4-benzoxazine and 1,4-benzodioxine compounds 1 and 10, which combine thrombin inhibitory and GPIIb/IIIa antagonistic activity in one molecule are shown to inhibit endothelial cell migration and tube formation in vitro and angiogenesis in the chicken chorioallantoic membrane (CAM) assay. The corresponding carboxylic acids 1 (R-2 = H) and 11 were devoid of anti-angiogenic activity, most probably due to their insufficient entry into the cell. Although thrombin inhibition remains the most probable explanation for their inhibition of angiogenesis, VEGFR2 kinase assay suggest that other targets such as VEGFR2 might be involved. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：160 / 170

页数：11

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