Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 12, Pages 4338-4350Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.04.076
Keywords
Pyrazole; Pyrazolo[4,3-c]quinoline; Angiogenesis; Endothelial cell proliferation and migration; CAM assay; Inhibition of tumor growth
Funding
- Flemish FWO [G. 0486.08]
- Concerted Actions [05/19]
- Centers of Excellence [05/15]
- COST action [CM 602]
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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. (C) 2010 Elsevier Ltd. All rights reserved.
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