Novel pyrazole derivatives: synthesis and evaluation of anti-angiogenic activity.
The synthesis of a series of novel trisubstituted pyrazole derivatives and their PIFA-mediated conversion to molecules bearing the fused pyrazolo[4,3-c]quinoline ring system is reported. The anti-angiogenic activity of these compounds was evaluated by using in vitro assays for endothelial cell proliferation and migration, and in the chicken chorioallantoic membrane (CAM) assay. Compounds containing the fused pyrazolo[4,3-c]quinoline motifs emerged as potent anti-angiogenic compounds, which also had the ability to inhibit the growth of human breast (MCF-7) and cervical (Hela) carcinoma cells in vitro.
Christodoulou
Michael S
MS
Chemistry Laboratory, Agricultural University of Athens, Iera Odos 75, Athens 11855, Greece.
Liekens
Sandra
S
Kasiotis
Konstantinos M
KM
Haroutounian
Serkos A
SA
D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D045744:Cell Line, Tumor; D002465:Cell Movement; D002645:Chickens; D049033:Chorioallantoic Membrane / Q000187:drug effects; D054697:Cytostatic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D042783:Endothelial Cells / Q000166:cytology / Q000187:drug effects; D006801:Humans; D051379:Mice; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011804:Quinolines / Q000737:chemistry
D020533:Angiogenesis Inhibitors; D054697:Cytostatic Agents; D011720:Pyrazoles; D011804:Quinolines