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

Miloš Ilić, Janez Ilaš, Petra Dunkel, Péter Mátyus, Andrej Boháč, Sandra Liekens, Danijel Kikelj

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8 Citations (Scopus)

Abstract

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 (R2 = 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.

Original languageEnglish
Pages (from-to)160-170
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume58
DOIs
Publication statusPublished - Dec 1 2012

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Keywords

  • Angiogenesis
  • GPIIb/IIIa antagonist
  • Thrombin
  • Vascular endothelial growth factor

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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