Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells

Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells

Inspired by diverse marine bioactive compounds, the principle of molecular hybridization was applied to produce a series of new compounds combining diverse heterocyclic systems (oxa/thiazoles and tetrahydropyrans) via a triazole ring, attempting to increase the activity of individual building blocks. These new compounds exhibit a highly interesting antiproliferative activity against different human tumour cells and good selectivity when compared to normal cells. The formation of reactive oxygen species and the interaction with P-gp were also evaluated for the lead compounds.

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Bibliographic Details
Main Authors: Valdomir, Guillermo, Fernández, María de los Ángeles, Lagunes, Irene, Padrón, Juan I., Martín, Víctor S., Padrón, José M., Davyt, Danilo
Other Authors: Ministerio de Economía y Competitividad (España)
Format: artículo biblioteca
Published: Royal Society of Chemistry (UK) 2018-07-24
Subjects:Antiproliferative activity, Oxa/thiazole-tetrahydropyran, Tumour cells, Triazole-linked hybrids,
Online Access:http://hdl.handle.net/10261/183319
http://dx.doi.org/10.13039/501100000780
http://dx.doi.org/10.13039/501100003329
http://dx.doi.org/10.13039/100008725
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spelling dig-ipna-es-10261-1833192020-12-11T08:57:47Z Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells Valdomir, Guillermo Fernández, María de los Ángeles Lagunes, Irene Padrón, Juan I. Martín, Víctor S. Padrón, José M. Davyt, Danilo Ministerio de Economía y Competitividad (España) European Commission Agencia Nacional de Investigación e Innovación (Uruguay) Antiproliferative activity Oxa/thiazole-tetrahydropyran Tumour cells Triazole-linked hybrids Inspired by diverse marine bioactive compounds, the principle of molecular hybridization was applied to produce a series of new compounds combining diverse heterocyclic systems (oxa/thiazoles and tetrahydropyrans) via a triazole ring, attempting to increase the activity of individual building blocks. These new compounds exhibit a highly interesting antiproliferative activity against different human tumour cells and good selectivity when compared to normal cells. The formation of reactive oxygen species and the interaction with P-gp were also evaluated for the lead compounds. This research was supported by CSIC Grupos No. 654 and No. 983, PEDECIBA Química and the Spanish MINECO. Co-financed by the European Regional Development Fund (ERDF) (CTQ2014-56362-C2-1-P). G. V. would like to thank ANII (Agencia Nacional de Investigación e Innovación) for the award of a doctoral fellowship. Peer Reviewed 2019-06-04T15:31:33Z 2019-06-04T15:31:33Z 2018-07-24 2019-06-04T15:31:34Z artículo http://purl.org/coar/resource_type/c_6501 doi: 10.1039/c8nj02388c e-issn: 1369-9261 issn: 1144-0546 New Journal of Chemistry 42: 13784-13789 (2018) http://hdl.handle.net/10261/183319 10.1039/c8nj02388c http://dx.doi.org/10.13039/501100000780 http://dx.doi.org/10.13039/501100003329 http://dx.doi.org/10.13039/100008725 #PLACEHOLDER_PARENT_METADATA_VALUE# info:eu-repo/grantAgreement/MINECO/Plan Estatal de Investigación Científica y Técnica y de Innovación 2013-2016/CTQ2014-56362-C2-1-P Postprint https://doi.org/10.1039/C8NJ02388C Sí none Royal Society of Chemistry (UK)
institution IPNA ES
collection DSpace
country España
countrycode ES
component Bibliográfico
access En linea
databasecode dig-ipna-es
tag biblioteca
region Europa del Sur
libraryname Biblioteca del IPNA España
topic Antiproliferative activity
Oxa/thiazole-tetrahydropyran
Tumour cells
Triazole-linked hybrids
Antiproliferative activity
Oxa/thiazole-tetrahydropyran
Tumour cells
Triazole-linked hybrids
spellingShingle Antiproliferative activity
Oxa/thiazole-tetrahydropyran
Tumour cells
Triazole-linked hybrids
Antiproliferative activity
Oxa/thiazole-tetrahydropyran
Tumour cells
Triazole-linked hybrids
Valdomir, Guillermo
Fernández, María de los Ángeles
Lagunes, Irene
Padrón, Juan I.
Martín, Víctor S.
Padrón, José M.
Davyt, Danilo
Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells
description Inspired by diverse marine bioactive compounds, the principle of molecular hybridization was applied to produce a series of new compounds combining diverse heterocyclic systems (oxa/thiazoles and tetrahydropyrans) via a triazole ring, attempting to increase the activity of individual building blocks. These new compounds exhibit a highly interesting antiproliferative activity against different human tumour cells and good selectivity when compared to normal cells. The formation of reactive oxygen species and the interaction with P-gp were also evaluated for the lead compounds.
author2 Ministerio de Economía y Competitividad (España)
author_facet Ministerio de Economía y Competitividad (España)
Valdomir, Guillermo
Fernández, María de los Ángeles
Lagunes, Irene
Padrón, Juan I.
Martín, Víctor S.
Padrón, José M.
Davyt, Danilo
format artículo
topic_facet Antiproliferative activity
Oxa/thiazole-tetrahydropyran
Tumour cells
Triazole-linked hybrids
author Valdomir, Guillermo
Fernández, María de los Ángeles
Lagunes, Irene
Padrón, Juan I.
Martín, Víctor S.
Padrón, José M.
Davyt, Danilo
author_sort Valdomir, Guillermo
title Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells
title_short Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells
title_full Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells
title_fullStr Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells
title_full_unstemmed Oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells
title_sort oxa/thiazole-tetrahydropyran triazole-linked hybrids with selective antiproliferative activity against human tumour cells
publisher Royal Society of Chemistry (UK)
publishDate 2018-07-24
url http://hdl.handle.net/10261/183319
http://dx.doi.org/10.13039/501100000780
http://dx.doi.org/10.13039/501100003329
http://dx.doi.org/10.13039/100008725
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