Novel pyrazole derivatives: Synthesis and evaluation of anti-angiogenic activity |
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Authors: | Michael S. Christodoulou Sandra Liekens Konstantinos M. Kasiotis Serkos A. Haroutounian |
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Affiliation: | 1. Chemistry Laboratory, Agricultural University of Athens, Iera Odos 75, Athens 11855, Greece;2. Rega Institute for Medical Research, Minderbroedersstraat 10, B-3000 Leuven, Belgium;3. Benaki Phytopathological Institute, 8 St. Delta Street, Athens, Kifissia 14561, Greece |
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Abstract: | 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. |
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