Project/scholarship details
- Project/scholarship ID
111060
- Reference
PTDC/QUI-QUI/111060/2009
- FundRef URI
- Funder
FCT - Fundação para a Ciência e a Tecnologia, I.P.
- Funder's country
Portugal
- Funding program
5876-PPCDTI
- Funding amount
134,529.00 €
- Start date
2010-12-24
- End date
2014-06-23
Documents
Synthesis and evaluation of tumor cell growth inhibition of Methyl 3-Amino-6-[(...
Queiroz, Maria João R. P.; Calhelha, Ricardo C.; Silva, Luís A. Vale; Pinto, Eugénia; Almeida, Gabriela M.; Vasconcelos, M. HelenaThe methyl 3-amino-6-bromothieno[3,2-b]pyridine-2-carboxylate, recently reported by some of us, was reacted in Sonogashira couplings with several (hetero)arylacetylenes. The growth inhibitory activity of the novel methyl 3-amino-6-[(hetero)arylethynyl]thieno[3,2-b]pyridine-2-carboxylates obtained was evaluated on three human tumor cell lines (MCF-7, NCI-H460, A375-C5). The para-methoxyphenyl and the ortho and p...
Anti-hepatocellular carcinoma activity using human HepG2 cells and hepatotoxici...
Abreu, Rui M. V.; Ferreira, Isabel C. F. R.; Calhelha, Ricardo C.; Lima, Raquel T.; Vasconcelos, M. Helena; Adega, Filomena; Chaves, RaquelHepatocellular carcinoma (HCC) is a highly complex cancer, resistant to commonly used treatments and new therapeutic agents are urgently needed. A total of thirty-two thieno[3,2-b]pyridine derivatives of two series: methyl 3-amino-6-(hetero)arylthieno[3,2-b]pyridine-2-carboxylates (1a-1t) and methyl 3-amino-6-[(hetero)arylethynyl]thieno[3,2-b]pyridine-2-carboxylates (2a-2n), previously prepared by some of us, w...
1-Aryl-3-[4-(thieno[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as VEGFR2 tyrosine kin...
Queiroz, Maria João R. P.; Peixoto, Daniela; Soares, Pedro; Abreu, Rui M. V.; Froufe, Hugo J. C.; Calhelha, Ricardo C.; Ferreira, Isabel C. F. R.Foundation for the Science and Technology (FCT–Portugal) for financial support through the NMR Portuguese network (Bruker 400 Avance III-Univ Minho). FCT and FEDER (European Fund for Regional Development)-COMPETE/QREN/EU for financial support through the research unities PEst-C/QUI/UI686/2011 and PEst-OE/AGR/UI0690/2011, the research project PTDC/QUI- QUI/111060/2009 and the post-Doctoral grant attributed to R....
Synthesis of novel 1-Aryl-3-[2-,3- Or 4-(Thieno[3,2-b]Pyridin-7-Ylthio)Phenyl]U...
Peixoto, Daniela; Queiroz, Maria João R. P.; Abreu, Rui M. V.; Froufe, Hugo J. C.; Calhelha, Ricardo C.; Ferreira, Isabel C. F. R.Vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase is involved in cancer and in angiogenesis. Herein, we report the synthesis of novel1-aryl-3-[2-, 3- or 4-{thieno[3,2-b ]pyridin-7-ylthio) phenyl]ureas as VEGFR2 inhibitors by promoting the regioselective attack of the thiol group of the 4-aminothiophenol in the chlorine nucleophilic displacement on 7-chlorothieno[3,2-b]pyridine 1, obtaining ...
1-Aryl-3-[4-(thieno[3,2-d]pyrimidin-4-yloxy)phenyl]ureas as VEGFR2 inhibitors: ...
Peixoto, Daniela; Calhelha, Ricardo C.; Soares, Pedro; Abreu, Rui M. V.; Froufe, Hugo J. C.; Ferreira, Isabel C. F. R.; Costa, Raquel; Soares, RaquelAcknowledgments:To the FCT–Portugal for financial support through the PTNMR network. To FCT and COMPETE/QREN/EU for financial support through the research unities PEst-C/QUI/UI686/2011, PEst-OE/AGR/UI0690/2011, PEst-OE/SAU/UI0038/2011, the research project PTDC/QUI-QUI/111060/2009 and the post-Doctoral grant attributed to R.C.C. (SFRH/BPD/68344/2010) also financed by POPH and FSE.
Synthesis of Tetracyclic systems and (Thio)Ureas from Aminodi(Hetero)Arylamines...
Queiroz, Maria João R. P.; Peixoto, Daniela; Calhelha, Ricardo C.Foundation for the Science and Technology (FCT–Portugal) for financial support through the Portuguese NMR network (Bruker 400 Avance III-Univ Minho). FCT and FEDER (European Fund for Regional Development)-COMPETE/QREN/EU for financial support through the research centre PEst-C/QUI/UI686/2011, the research project PTDC/QUI-QUI/111060/2009 and the post-doctoral grant of R.C.C. SFRH/BPD/68344/2010.
Aminodi(hetero)arylamines in the thieno[3,2-b]pyridine series: synthesis, effec...
Calhelha, Ricardo C.; Ferreira, Isabel C. F. R.; Peixoto, Daniela; Abreu, Rui M. V.; Silva, L. A. Vale; Pinto, Eugénia; Lima, Raquel T.Three aminodi(hetero)arylamines were prepared via a palladium-catalyzed C-N Buchwald-Hartwig coupling of methyl 3-aminothieno[3,2-b]pyridine-2-carboxylate with different bromonitrobenzenes, followed by reduction of the nitro groups of the coupling products to the corresponding amino compounds. The aminodi(hetero)arylamines thus obtained were evaluated for their growth inhibitory effect on four human tumor cell ...
Fluorescence studies on new potential antitumoral 1,3-diarylurea derivatives in...
Rodrigues, Ana Rita O.; Mendes, Pedro M. F.; Castanheira, Elisabete M. S.; Coutinho, Paulo J. G.; Peixoto, Daniela; Queiroz, Maria João R. P.Magnetic nanoparticles of magnetite and of nickel core with silica shell were prepared and either covered with a lipid bilayer or entrapped in liposomes, forming magnetoliposomes. New potential antitumoral 1,3-diarylurea derivatives of thieno[3,2-b]pyridines were then encapsulated in liposomes and magnetoliposomes and their photophysical behavior was investigated.; Fundação para a Ciência e a Tecnologia (FCT), ...
Synthesis of 2-(hetero)arylthieno[2,3-b] or [3,2-b]pyridines from 2,3-dihalopyr...
Peixoto, Daniela; Begouin, Agathe; Queiroz, Maria João R. P.A simple and efficient three-step methodology is described for the first time for the synthesis of 2-(hetero)arylthieno[2,3-b] or [3,2-b]pyridines. The first step is a Sonogashira coupling from 3-bromo-2-chloropyridine or 2-bromo-3-chloropyridine with several (hetero)arylalkynes to obtain the corresponding 2- or 3-chloro(hetero)arylethynylpyridines. These were cyclized by treatment with Na2S affording the expec...
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; dos 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-blpyridine, using copper (C-O) or palladium (C N) catalyzed couplings, respectively, of the 7-bromothieno[3,2-blpyridine, also prepared, with ortho, meta and para fluoro or methoxy phenols and anilines. The compounds obtained were evaluated for their growth inhibitory act...
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