1094629-01-2Relevant academic research and scientific papers
Novel pyrazole derivatives: Synthesis and evaluation of anti-angiogenic activity
Christodoulou, Michael S.,Liekens, Sandra,Kasiotis, Konstantinos M.,Haroutounian, Serkos A.
, p. 4338 - 4350 (2010)
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.
PIFA-mediated synthesis of novel pyrazoloquinolin-4-ones as potential ligands for the estrogen receptor
Christodoulou, Michael S.,Kasiotis, Konstantinos M.,Fokialakis, Nikolas,Tellitu, Imanol,Haroutounian, Serkos A.
experimental part, p. 7100 - 7102 (2009/04/10)
A facile and efficient preparation of pyrazoloquinolin-4-ones, as potential ligands for the estrogen receptor, via a PIFA [phenyliodine(III)bis(trifluoroacetate)] promoted cyclization reaction with overall yields up to 29% over six steps is described. The employed strategy, based on an electrophilic amidation reaction as the key step of the synthesis, allows the generation of a diverse array of derivatives.
