TY - JOUR
T1 - Novel phosphine sulphide gold(i) complexes
T2 - topoisomerase I inhibitors and antiproliferative agents
AU - Martín-Encinas, Endika
AU - Conejo-Rodríguez, Verónica
AU - Miguel, Jesús A.
AU - Martínez-Ilarduya, Jesús M.
AU - Rubiales, Gloria
AU - Knudsen, Birgitta R.
AU - Palacios, Francisco
AU - Alonso, Concepción
PY - 2020
Y1 - 2020
N2 - 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 IC50values in the nanomolar range and IC50values 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.
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 IC50values in the nanomolar range and IC50values 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.
UR - https://www.scopus.com/pages/publications/85086506428
U2 - 10.1039/d0dt01467b
DO - 10.1039/d0dt01467b
M3 - Journal article
C2 - 32463416
AN - SCOPUS:85086506428
SN - 1477-9226
VL - 49
SP - 7852
EP - 7861
JO - Dalton Transactions
JF - Dalton Transactions
IS - 23
ER -