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Gold(I) Bis(1,2,3-triazol-5-ylidene) Complexes as Promising Selective Anticancer Compounds

2021; American Chemical Society; Volume: 64; Issue: 21 Linguagem: Inglês

10.1021/acs.jmedchem.1c01021

1520-4804

Jonas F. Schlagintweit, Christian Jakob, Nicola L. Wilke, Marie Ahrweiler, Corazon Frias, Jerico Frias, Marcel König, Eva‐Maria H. J. Esslinger, Fernanda Marques, João Franco Machado, Robert M. Reich, Tânia S. Morais, João D. G. Correia, Aram Prokop, Fritz E. Kühn,

Metal complexes synthesis and properties

The synthesis and antiproliferative activity of Mes- and iPr-substituted gold(I) bis(1,2,3-triazol-5-ylidene) complexes in various cancer cell lines are reported, showing nanomolar IC50 values of 50 nM (lymphoma cells) and 500 nM (leukemia cells), respectively (Mes < iPr). The compounds exclusively induce apoptosis (50 nM to 5 μM) instead of necrosis in common malignant blood cells (leukemia cells) and do not affect non-malignant leucocytes. Remarkably, the complexes not only overcome resistances against the well-established cytostatic etoposide, cytarabine, daunorubicin, and cisplatin but also promote a synergistic effect of up to 182% when used with daunorubicin. The present results demonstrate that gold(I) bis(1,2,3-triazol-5-ylidene) complexes are highly promising and easily modifiable anticancer metallodrugs.