Improved Antiproliferative Activity and Fluorescence of a Dinuclear Gold(I) Bisimidazolylidene Complex via Anthracene-Modification.
Christian H G JakobBruno DominelliJonas F SchlagintweitPauline J FischerFranziska SchudererRobert M ReichFernanda MarquesJoão D G CorreiaFritz E KühnPublished in: Chemistry, an Asian journal (2020)
A straightforward modification route to obtain mono- and di-substituted anthroyl ester bridge functionalized dinuclear Au(I) bis-N-heterocyclic carbene complexes is presented. The functionalization can be achieved starting from a hydroxyl-functionalized ligand precursor followed by transmetallation of the corresponding Ag complex or via esterification of the hydroxyl-functionalized gold complex. The compounds are characterized by NMR-spectroscopy, ESI-MS, elemental analysis and SC-XRD. The mono-ester Au complex shows quantum yields around 18%. In contrast, the corresponding syn-di-ester Au complex, exhibits significantly lower quantum yields of around 8%. Due to insufficient water solubility of the di-ester, only the mono-ester complex has been tested regarding its antiproliferative activity against HeLa- (cervix) and MCF-7- (breast) cancer cell lines and a healthy fibroblast cell line (V79). IC50 values of 7.26 μM in the HeLa cell line and 7.92 μM in the MCF-7 cell line along with selectivity indices of 8.8 (HeLa) and 8.0 (MCF-7) are obtained. These selectivity indices are significantly higher than those obtained for the reference drugs cisplatin or auranofin.
Keyphrases
- quantum dots
- sensitive detection
- breast cancer cells
- ms ms
- magnetic resonance
- molecular dynamics
- computed tomography
- biofilm formation
- molecular docking
- cystic fibrosis
- cell death
- energy transfer
- cell cycle arrest
- cell proliferation
- contrast enhanced
- preterm birth
- pi k akt
- wound healing
- silver nanoparticles
- liquid chromatography
- walled carbon nanotubes