Gold(I) Bis(1,2,3-triazol-5-ylidene) Complexes as Promising Selective Anticancer Compounds.
In: Journal of medicinal chemistry, Jg. 64 (2021-11-11), Heft 21, S. 15747-15757
academicJournal
Zugriff:
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 IC 50 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.
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Gold(I) Bis(1,2,3-triazol-5-ylidene) Complexes as Promising Selective Anticancer Compounds.
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Autor/in / Beteiligte Person: | Schlagintweit, JF ; Jakob, CHG ; Wilke, NL ; Ahrweiler, M ; Frias, C ; Frias, J ; König, M ; Esslinger, EHJ ; Marques, F ; Machado, JF ; Reich, RM ; Morais, TS ; Correia, JDG ; Prokop, A ; Kühn, FE |
Zeitschrift: | Journal of medicinal chemistry, Jg. 64 (2021-11-11), Heft 21, S. 15747-15757 |
Veröffentlichung: | Washington Dc : American Chemical Society ; <i>Original Publication</i>: [Easton, Pa.] : American Chemical Society, [c1963-, 2021 |
Medientyp: | academicJournal |
ISSN: | 1520-4804 (electronic) |
DOI: | 10.1021/acs.jmedchem.1c01021 |
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