| Publication Type |
Journal Article |
| Title |
Gold(I) Bis(1,2,3-triazol-5-ylidene) Complexes as Promising Selective Anticancer Compounds |
| Authors |
Jonas F. Schlagintweit Christian H. G. Jakob Nicola L. Wilke Marie Ahrweiler Corazon Frias Jerico Frias Marcel Koenig Eva-Maria H. J. Esslinger Fernanda M. Marques Joao F. Machado Robert M. Reich Tânia S. Morais Joao D. G. Correia Aram Prokop Fritz E. Kuehn |
| Groups |
BIOIN |
| Journal |
JOURNAL OF MEDICINAL CHEMISTRY |
| Year |
2021 |
| Month |
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|
| Volume |
64 |
| Number |
21 |
| Pages |
15747-15757 |
| Abstract |
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 mu M) 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. |
| DOI |
http://dx.doi.org/10.1021/acs.jmedchem.1c01021 |
| ISBN |
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| Publisher |
|
| Book Title |
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| ISSN |
0022-2623 |
| EISSN |
1520-4804 |
| Conference Name |
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| Bibtex ID |
WOS:000718382200016 |
| Observations |
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