RT info:eu-repo/semantics/article
T1 Novel phosphine sulphide gold(i) complexes: topoisomerase I inhibitors and antiproliferative agents
A1 Martín Encinas, Endika
A1 Conejo Rodríguez, Verónica
A1 Miguel García, Jesús Ángel
A1 Martínez de Ilarduya Martínez de Ilarduya, Jesús María
A1 Rubiales, Gloria
A1 Knudsen, Birgitta Ruth
A1 Palacios, Francisco
A1 Alonso Pérez, Concepción Estibaliz
K1 Gold complexes
K1 Complejos de oro
K1 Topoisomerase
K1 Topoisomerasa
AB This work describes the synthesis of the gold(I) complexes of phosphine sulphides. The formation of these new derivatives has been confirmed by X-ray crystallography. The coordination of gold(I) with the sulphur atom of the phosphine sulphides favors the inhibition of topoisomerase I as well as a high cytotoxicity of the gold(I)-complexed compounds against the cancer line A549 with IC50 values in the nanomolar range and IC50 values below 5 μM against the SKOV3 cell line. It should be noted that the cytotoxicities observed for the new gold(I) complexes are higher than those observed for phosphine sulphide ligands before binding to gold. Furthermore, the results also indicate that the presence of a nitrogenated heterocycle, such as tetrahydroquinoline or quinoline, is also necessary for the TopI inhibition to be maintained. In addition, no toxicity was observed when the non-cancerous lung fibroblast cell line (MRC5) was treated with the new phosphine sulphide gold(I) complexes prepared.
PB Royal Society of Chemistry
SN 1477-9234
YR 2020
FD 2020
LK https://uvadoc.uva.es/handle/10324/52800
UL https://uvadoc.uva.es/handle/10324/52800
LA eng
NO Dalton Transactions, 2020, vol. 49, n. 23. p. 7852-7861
NO Producción Científica
DS UVaDOC
RD 20-oct-2024