Gold(I)–Coumarin–Caffeine‐Based Complexes as New Potential Anti‐Inflammatory and Anticancer Trackable Agents

Abstract

Three new gold(I)-coumarin-based trackable therapeutic complexes and two non-trackable analogues have been synthesised and fully characterised. They all display anti-proliferative properties on several types of cancer cell lines, including those of colon, breast, and prostate. Two complexes displayed significant anti-inflammatory effects; one displayed pro-inflammatory behaviour; this highlights the impact of the position of the fluorophore on the caffeine scaffold. Additionally, the three coumarin derivatives could be visualised in vitro by two-photon microscopy.

Coumarin‐Tagged Dinuclear Trithiolato‐Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity

“…Several gold(I) complexes bearing coumarin units were described. [28,47,49] For example gold(I) carbene complex H displayed poor photophysical properties (fluorescence quantum yield, Φ F = 2 %), the fluorescence quenching being attributed to a photo-induced electron transfer between the coumarin and the carbene. [47] Nevertheless fluorescence confocal microscopy demonstrated the uptake of H in the nuclei of A2780 (human ovarian cancer) cells (IC 50 = 12 μM) at a concentration of 50 μM.…”

“…However, the fluorescence intensity of the coumarin moiety was reduced by 90 % in this conjugate, thus no microscopy studies on cellular uptake were reported. Several gold(I) complexes bearing coumarin units were described . For example gold(I) carbene complex H displayed poor photophysical properties (fluorescence quantum yield, Φ F =2 %), the fluorescence quenching being attributed to a photo‐induced electron transfer between the coumarin and the carbene .…”

Development of a novel highly anti-proliferative family of gold complexes: Au(i)-phosphonium-phosphines

“…14 Gold(I) complexes were extensively studied by many researchers including our group. [15][16][17][18][19][20][21][22][23][24][25][26] Contrary to platinum derivatives, the main hypothesis concerning the mechanism of action of gold(I)-based phosphine complexes is the inhibition of thio and/or seleno-cysteine enzymes, such as thioredoxine reductases (TrxRs), via the coordination of gold center to thiols or selenols. TrxRs are in charge of the regulation of oxidative stress and their inhibition leads to the increase of ROS and to apoptosis.…”

Conception and Evaluation of Fluorescent Phosphine‐Gold Complexes: From Synthesis to in vivo Investigations

“…Moreover, it also presents interesting biological properties, either as an antibacterial or anti-inflammatory agent. [54][55][56][57][58] This last property is interesting because gold(I) complexes often also have anti-inflammatory properties. Knowing that some anticancer treatments induce inflammation phenomena which seem to be the cause of side effects, [59,60] the development of a drug with an anti-inflammatory effect should make it possible to limit such issues.…”