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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Summary: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.