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Epidermal growth factor receptor inhibitory activity of new potential antitumor di(hetero)arylethers and di(hetero)arylamines in the thieno[3,2-b]pyridine series

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dc.contributor.authorCalhelha, Ricardo C.
dc.contributor.authorPeixoto, Daniela
dc.contributor.authorSoares, Pedro
dc.contributor.authorFerreira, Isabel C.F.R.
dc.contributor.authorAbreu, Rui M.V.
dc.contributor.authorQueiroz, Maria João R.P.
dc.date.accessioned2014-03-27T16:23:52Z
dc.date.available2014-03-27T16:23:52Z
dc.date.issued2013
dc.description.abstractThienopyridine skeleton has been reported as having interesting biological activity, namely as antitumorals [1] and antiangiogenics [2]. The Epidermal Growth Factor Receptor (EGFR) exists in the cell surface and is activated by binding its specific ligands. The inhibition of its intracellular tyrosine kinase domain prevents the signaling pathways of cellular proliferation [3]. In our research group we have prepared the di(hetero)arylethers 1a-f and the di(hetero)arylamines 2a-f functionalizing the 7-position of the thieno[3,2-b]pyridine in good to high yields, using copper (C-O) or palladium (C-N) catalyzed couplings, like presented below.The di(hetero)arylethers 1a-f and di(hetero)arylamines 2a-f series were evaluated for EGFR tyrosine kinase inhibition activity. Compounds for series 1 presented practically no or very weak inhibition activity while compounds 2 presented good inhibition activity, with the most potent compounds 2e presenting a IC50 value of 40 nM. These compounds can be view as good starting points for the synthesis of even more potent EGFR inhibitors.por
dc.description.sponsorshipFoundation for the Science and Technology (FCT–Portugal) for financial support through the Portuguese NMR network (Bruker 400 Avance III-Univ Minho). To FCT and FEDER-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.C.C. (SFRH/BPD/68344/2010) also financed by POPH and FSE.por
dc.identifier.citationCalhelha, Ricardo C.; Peixoto, Daniela; Soares, Pedro; Ferreira, Isabel C.F.R.; Abeu, Rui M.V.; Queiroz, Maria-João R.P. (2013). Epidermal growth factor receptor inhibitory activity of new potential antitumor di(hetero)arylethers and di(hetero)arylamines in the thieno[3,2-b]pyridine series. In 1st International Symposium on Profiling. Almada. ISBN 978-989-98415-5-0por
dc.identifier.isbn978-989-98415-5-0
dc.identifier.urihttp://hdl.handle.net/10198/9396
dc.language.isoengpor
dc.peerreviewedyespor
dc.relationPEst-C/QUI/UI686/2011
dc.relationStrategic Project - UI 690 - 2011-2012
dc.titleEpidermal growth factor receptor inhibitory activity of new potential antitumor di(hetero)arylethers and di(hetero)arylamines in the thieno[3,2-b]pyridine seriespor
dc.typeconference object
dspace.entity.typePublication
oaire.awardTitleStrategic Project - UI 690 - 2011-2012
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876-PPCDTI/PTDC%2FQUI-QUI%2F111060%2F2009/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/SFRH/SFRH%2FBPD%2F68344%2F2010/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/PEst-OE%2FAGR%2FUI0690%2F2011/PT
oaire.citation.conferencePlaceCaparica – Portugalpor
oaire.citation.title1st International Symposium on Profilingpor
oaire.fundingStream5876-PPCDTI
oaire.fundingStreamSFRH
oaire.fundingStream6817 - DCRRNI ID
person.familyNameCalhelha
person.familyNameFerreira
person.familyNameAbreu
person.givenNameRicardo C.
person.givenNameIsabel C.F.R.
person.givenNameRui M.V.
person.identifier144781
person.identifier.ciencia-idF313-E3CE-554E
person.identifier.ciencia-id9418-CF95-9919
person.identifier.ciencia-id0F19-0DE2-12A2
person.identifier.orcid0000-0002-6801-4578
person.identifier.orcid0000-0003-4910-4882
person.identifier.orcid0000-0002-7745-8015
person.identifier.ridJ-2172-2014
person.identifier.ridE-8500-2013
person.identifier.scopus-author-id6507978333
person.identifier.scopus-author-id36868826600
person.identifier.scopus-author-id7003290613
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccesspor
rcaap.typeconferenceObjectpor
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