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

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

Research output: Contribution to journalArticle

7 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 2012

Fingerprint

Benzoxazines
Angiogenesis Inhibitors
Thrombin
Assays
Chorioallantoic Membrane
Endothelial cells
Carboxylic Acids
Cell Movement
Chickens
Esters
Phosphotransferases
Endothelial Cells
Membranes
Molecules

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

Cite this

Novel 1,4-benzoxazine and 1,4-benzodioxine inhibitors of angiogenesis. / Ilić, Miloš; Ilaš, Janez; Dunkel, Petra; Mátyus, P.; Boháč, Andrej; Liekens, Sandra; Kikelj, Danijel.

In: European Journal of Medicinal Chemistry, Vol. 58, 12.2012, p. 160-170.

Research output: Contribution to journalArticle

Ilić, Miloš ; Ilaš, Janez ; Dunkel, Petra ; Mátyus, P. ; Boháč, Andrej ; Liekens, Sandra ; Kikelj, Danijel. / Novel 1,4-benzoxazine and 1,4-benzodioxine inhibitors of angiogenesis. In: European Journal of Medicinal Chemistry. 2012 ; Vol. 58. pp. 160-170.
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