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http://hdl.handle.net/10261/157837
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dc.contributor.author | Cortés, Roldán | - |
dc.contributor.author | Cascante, Marta | - |
dc.date.accessioned | 2017-11-29T10:41:35Z | - |
dc.date.available | 2017-11-29T10:41:35Z | - |
dc.date.issued | 2012-08 | - |
dc.identifier | doi: 10.1016/j.ejmech.2012.06.002 | - |
dc.identifier | issn: 0223-5234 | - |
dc.identifier.citation | European Journal of Medicinal Chemistry 54: 557-566 (2012) | - |
dc.identifier.uri | http://hdl.handle.net/10261/157837 | - |
dc.description.abstract | A series of seven-membered cyclometallated Pt(II) complexes containing a terdentate [C,N,N'] ligand (1a-1c and 2a-2c) have been developed as potential monofunctional DNA binding agents. By reactions of cis-[Pt(4-C 6H 4Me) 2(μ-SEt 2)] 2 or cis-[Pt(C 6H 5) 2(SMe 2) 2] with imines 2-ClC 6H 4CHNCH 2CH 2NMe 2 (b) or 2-F,6-ClC 6H 3CHNCH 2CH 2NMe 2 (c) the new compounds 1b, 1c and 2c were synthesized and characterized. Complex 1b and 1c were further characterized by X-ray crystallography. The cytotoxicity assessment of the seven-membered platinacycles 1 (1a-1c) and 2 (2a-2c) against a panel of human cancer cell lines (A549 lung, HCT116 colon, and MDA MB231 breast adenocarcinomas) revealed that the six cycloplatinated complexes exhibit a remarkable antiproliferative activity, even greater than cisplatin in the three human cancer cell lines. From a pharmacological point of view, platinacycles 1 (1a-1c) and 2 (2a-2c) may represent compounds for a new class of antitumor drugs. Electrophoretic DNA migration studies showed that all of them modify the DNA tertiary structure. Induction of S-G2/M arrest and apoptosis were also observed for one of the representative compounds (1c) of the series. © 2012 Elsevier Masson SAS. All rights reserved. | - |
dc.description.sponsorship | This work was supported by the Ministerio de Ciencia y Tecnología (projects CTQ2009-11501 and CTQ2009-07021/BQU) and the AGAUR, Generalitat de Catalunya (Grants 2009-SGR-1111, 2009SGR01308, 2006ITT-10007 and 2009CTP-00026). This study was also supported by the project SAF2011-25726 and by RD06/0020/0046 from Red Temática de Investigación Cooperativa en Cáncer (RTICC), Instituto de Salud Carlos III, both funded by the Ministerio de Ciencia e Innovación-Spanish government and European Regional Development Funds (ERDF) “Una manera de hacer Europa”. Marta Cascante acknowledges the support received through the prize “ICREA Academia”, funded by ICREA foundation-Generalitat de Catalunya. | - |
dc.publisher | Elsevier | - |
dc.relation.isversionof | Postprint | - |
dc.rights | closedAccess | - |
dc.subject | Anticancer drugs | - |
dc.subject | Cytotoxicity | - |
dc.subject | Cancer | - |
dc.subject | Platinum(II) | - |
dc.subject | Cyclometallated compounds | - |
dc.subject | Seven-membered platinacycles | - |
dc.title | Seven-membered cycloplatinated complexes as a new family of anticancer agents. X-ray characterization and preliminary biological studies | - |
dc.type | artículo | - |
dc.identifier.doi | 10.1016/j.ejmech.2012.06.002 | - |
dc.relation.publisherversion | https://www.doi.org/10.1016/j.ejmech.2012.06.002 | - |
dc.date.updated | 2017-11-29T10:41:35Z | - |
dc.description.version | Peer Reviewed | - |
dc.language.rfc3066 | eng | - |
dc.contributor.funder | Ministerio de Ciencia y Tecnología (España) | - |
dc.contributor.funder | Generalitat de Catalunya | - |
dc.contributor.funder | Ministerio de Ciencia e Innovación (España) | - |
dc.contributor.funder | European Commission | - |
dc.relation.csic | Sí | - |
dc.identifier.funder | http://dx.doi.org/10.13039/501100002809 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100000780 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100004837 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100006280 | es_ES |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairetype | artículo | - |
item.grantfulltext | none | - |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | No Fulltext | - |
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