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Bioorg Med Chem. 2011 Jan 1;19(1):448-57. doi: 10.1016/j.bmc.2010.11.010. Epub 2010 Nov 10.

Synthesis, in vitro and in vivo preliminary evaluation of anti-angiogenic properties of some pyrroloazaflavones.

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  • 1Department of Pharmaceutical Sciences, University of Padova, via F. Marzolo, 5, 35131 Padova, Italy. mariagrazia.ferlin@unipd.it


This work investigated the in vitro and in vivo anti-angiogenic activity of some pyrroloazaflavones, exactly 2-phenyl-1H-pyrrolo[2,3-h]quinolin-4(7H)ones, with vinblastine as reference compound. Growth inhibitory activity, migration, and capillary-like structures formation were determined in human umbilical vein endothelial cell cultures, and Matrigel plug assay was carried out to evaluate in vivo effects on angiogenesis. Collectively, our results indicate that some pyrroloazaflavone derivatives, at non-cytotoxic concentrations and like vinblastine are able: (i) to exert in vitro anti-angiogenic activity and (ii) to counteract in vitro and in vivo the pro-angiogenic effects of fibroblast growth factor-2 (FGF-2).

Copyright © 2010 Elsevier Ltd. All rights reserved.

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