dc.creator | Recio Jiménez, Rocío | es |
dc.creator | Lerena Pérez, Patricia | es |
dc.creator | Pozo Torres, Esther | es |
dc.creator | Calderón Montaño, José Manuel | es |
dc.creator | Burgos Morón, Estefanía | es |
dc.creator | López Lázaro, Miguel | es |
dc.creator | Valdivia Giménez, Victoria Esther | es |
dc.creator | Pernia Leal, Manuel | es |
dc.creator | Mouillac, Bernard | es |
dc.creator | Organero, Juan Ángel | es |
dc.creator | Khiar, Noureddine | es |
dc.creator | Fernández Fernández, Inmaculada | es |
dc.date.accessioned | 2021-11-26T14:22:56Z | |
dc.date.available | 2021-11-26T14:22:56Z | |
dc.date.issued | 2021 | |
dc.identifier.citation | Recio Jiménez, R., Lerena Pérez, P., Pozo Torres, E., Calderón Montaño, J.M., Burgos Morón, E., López Lázaro, M.,...,Fernández Fernández, I. (2021). Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity. Journal of Medicinal Chemistry, 64 (14), 10350-10370. https://doi.org/10.1021/acs.jmedchem.1c00793. | |
dc.identifier.issn | 0022-2623 | es |
dc.identifier.issn | 1520-4804 | es |
dc.identifier.uri | https://hdl.handle.net/11441/127707 | |
dc.description.abstract | NK1R antagonists, investigated for the treatment of several pathologies, have shown encouraging results in the treatment of several cancers. In the present study, we report on the synthesis of carbohydrate-based NK1R antagonists and their evaluation as anticancer agents against a wide range of cancer cells. All of the prepared compounds, derived from either-arabinose, have shown high affinity and NK1R antagonistic activity with a broad-spectrum anticancer activity and an important selectivity, comparable to Cisplatin. This strategy has allowed us to identify the galactosyl derivative 14α , as an interesting hit exhibiting significant NK1R antagonist effect (kinact0.209 ± 0.103 μM) and high binding affinity for NK1R (IC50= 50.4 nM,Ki= 22.4 nM by measuring the displacement of [125I] SP from NK1R). Interestingly, this galactosyl derivative has shown marked selective cytotoxic activity against 12 different types of cancer cell lines. | es |
dc.description.sponsorship | Ministerio de Economía y Competitividad CTQ2016-78580-C2- 2-R, CTQ2016-78580-C2-1-R, CTQ2017-86655-R, PID2019-104767RB-I00 | es |
dc.description.sponsorship | Ministerio de Ciencia e Innovación PID2019-104767RB-I00 | es |
dc.description.sponsorship | Junta de Andalucía P06-FQM-01852, CV20-04221, FQM-313, FQM-102 | es |
dc.format | application/pdf | es |
dc.format.extent | 21 p. | es |
dc.language.iso | eng | es |
dc.publisher | American Chemical Society | es |
dc.relation.ispartof | Journal of Medicinal Chemistry, 64 (14), 10350-10370. | |
dc.rights | Attribution-NonCommercial-NoDerivatives 4.0 Internacional | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | * |
dc.title | Carbohydrate-Based NK1R Antagonists with Broad-Spectrum Anticancer Activity | es |
dc.type | info:eu-repo/semantics/article | es |
dcterms.identifier | https://ror.org/03yxnpp24 | |
dc.type.version | info:eu-repo/semantics/publishedVersion | es |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | es |
dc.contributor.affiliation | Universidad de Sevilla. Departamento de Química Orgánica y Farmacéutica | es |
dc.contributor.affiliation | Universidad de Sevilla. Departamento de Farmacología | es |
dc.relation.projectID | CTQ2016-78580-C2- 2-R | es |
dc.relation.projectID | CTQ2016-78580-C2-1-R | es |
dc.relation.projectID | CTQ2017-86655-R | es |
dc.relation.projectID | PID2019-104767RB-I00 | es |
dc.relation.projectID | PID2019-104767RB-I00 | es |
dc.relation.projectID | P06-FQM-01852 | es |
dc.relation.projectID | CV20-04221 | es |
dc.relation.projectID | FQM-313 | es |
dc.relation.projectID | FQM-102 | es |
dc.relation.projectID | CSIC-COV19-047 | es |
dc.relation.publisherversion | https://doi.org/10.1021/acs.jmedchem.1c00793 | es |
dc.identifier.doi | 10.1021/acs.jmedchem.1c00793 | es |
dc.journaltitle | Journal of Medicinal Chemistry | es |
dc.publication.volumen | 64 | es |
dc.publication.issue | 14 | es |
dc.publication.initialPage | 10350 | es |
dc.publication.endPage | 10370 | es |
dc.contributor.funder | Consejo Superior de Investigaciones Científicas (CSIC) CSIC-COV19-047 | es |
dc.description.awardwinning | Premio Anual Publicación Científica Destacada de la US. Facultad de Farmacia | |