Evaluation of the antiangiogenic effects of 2-aryl-3-bromoquinolin-4(1H)-ones and a NCH3-4-oxo derivative.
2-Aryl-3-bromoquinolin-4(1H)-ones and 2-aryl-3-bromo-1-methylquinolin-4(1H)-one were evaluated for their antiangiogenic effects. Results showed that the 2-aryl-3-bromoquinolin-4(1H)-ones (QNHFBr and QNHClBr), and the 3-bromo-2-(4-chlorophenyl)-1-methylquinolin-4(1H)-one (QNMeClBr) reduced endothelial cell numbers in an assay of cell proliferation, showing increased cytotoxicity at higher doses. The compounds also inhibited neovessel growth in an ex vivo assay of angiogenesis. Furthermore, low levels of proangiogenic factors, namely, basic fibroblast growth factor (bFGF) and vascular endothelial growth factor/placental growth factor (VEGF/PlGF) were obtained in cultures treated with these compounds. Thus, the tested compounds, QNHFBr, QNHClBr, and QNMeClBr exhibit antiangiogenic activity.
Department of Anatomy and Physiology, Private Bag X04, University of Pretoria, Onderstepoort, South Africa. peace.mabeta@up.ac.za
Peace
P
Mabeta
Roland
R
Auer
Malose Jack
MJ
Mphahlele
D020533:Angiogenesis Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000473:pathology; D049109:Cell Proliferation / Q000187:drug effects; D042783:Endothelial Cells / Q000166:cytology / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D055806:Microvessels / Q000166:cytology / Q000187:drug effects*; D015394:Molecular Structure; D009389:Neovascularization, Pathologic / Q000517:prevention & control*; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
C541776:3-bromo-2-(4-chlorophenyl)-1-methylquinolin-4(1H)-one; C541777:3-bromo-2-(4-chlorophenyl)quinolin-4(1H)-one; C541778:3-bromo-2-(4-fluorophenyl)quinolin-4(1H)-one; D020533:Angiogenesis Inhibitors; D015363:Quinolones