Maria-João R. P. Queiroz
University of Minho, Portugal
Title: Synthesis and evaluation of new thienopyrimidine/pyridine derivatives as antitumoral and/or antiangiogenics
Biography
Biography: Maria-João R. P. Queiroz
Abstract
New thieno[3,4-d]pyrimidines and thieno[3,2-b]pyridines were prepared, fully characterized, and evaluated as antitumor compounds against various human tumor cell lines and/or as antiangiogenics using HUVECs (Human Endothelial Vein Umbilical Cells) that express the VEGFR2 (Vascular Endothelium Growth Factor Receptor-2) which is a trans-membrane tyrosine kinase receptor involved in angiogenesis. Some of our compounds were shown to be active against several human tumor cell lines with low to moderate IC50 values and for the most promising compounds the effects on the cell cycle profile and the induction of apoptosis were studied. The toxicity of these compounds was also studied using a primary porcine liver cell culture established by our group. Some of the compounds prepared, suggested by rational design, were shown to be inhibitors of the phosphorylation of the intracellular domain of tyrosine kinase of the VEGFR2. This mechanism of action of the evaluated anti-proliferation of HUVECs by the BrdU assay in the presence of the compounds was confirmed using western Blott.
