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Synthesis and evaluation of the antitumor potential of new aminated or methoxyl...
Calhelha, Ricardo C.; Campos, Joana F.; Peixoto, Daniela; Abreu, Rui M.V.; Ferreira, Isabel C.F.R.; Queiroz, Maria João R.P.Synthesis and evaluation of the antitumor potential of new aminated or methoxylated di(hetero)arylthioethers in the thieno[3,2-b]pyridine séries. In 1st Symposium on Medicinal Chemistry. Braga Several thienopyridines have already been described as inhibitors of cell proliferation using human tumor cells[1,2], highlighting the interest of studying their antitumorpotential. ln this work, we present the synthesis ...
Synthesis of new N-[3-(thieno[3,2-b]pyridine-7-ylthio)phenyl]benzamides as pote...
Campos, Joana F.; Begouin, Agathe; Peixoto, Daniela; Froufe, Hugo J.C.; Abreu, Rui M.V.; Ferreira, Isabel C.F.R.; Queiroz, Maria João R.P.Angiogenesis, the growth of new vessels from preexisting vasculature, is a critical step in tumor progression [1]. The tyrosine kinase Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) is a crucial mediator in angiogenesis since the VEGF, excreted by the tumor cells, binds to it activating several signaling pathways involved in cell survival and proliferation [2]. Recently thienopyridine derivatives showed...
New di(hetero)arylethers and di(hetero)arylamines in the thieno[3,2-b]pyridine ...
Queiroz, Maria João R.P.; Peixoto, Daniela; Calhelha, Ricardo C.; Soares, Pedro; Santos, Tiago; Lima, Raquel T.; Campos, Joana F.; Abreu, Rui M.V.New fluorinated and methoxylated di(hetero)arylethers and di(hetero)arylamines were prepared functionalizing the 7-position of the thieno[3,2-b]pyridine, using copper (C–O) or palladium (C–N) catalyzed couplings, respectively, of the 7-bromothieno[3,2-b]pyridine, also prepared, with ortho, meta and para fluoro or methoxy phenols and anilines. The compounds obtained were evaluated for their growth inhibitory act...
Virtual screening of thieno[3,2-b]pyridine arylthioether (hetero)aryltriazole d...
Calhelha, Ricardo C.; Begouin, Agathe; Campos, Joana F.; Ferreira, Isabel C.F.R.; Queiroz, Maria João R.P.; Abreu, Rui M.V.Recently we presented a series of thieno[3,2-d]pyrimidinc ether I ,3-diaryl ureas with potent VEGFR2 inhibit ion activity. The binding mode was analyzed and the compounds showed a type-11 tyrosine kinase inhibition mode, with the thienopyrimidine moiety forming a Hydrogen Bond (H-bond) with CYS919 residue and the urea moiety forming a H-bonds with key residues G LU885 and ASP I 046 of the kinase domain. In thi...
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