Novel half-sandwich iridium(III) complexes with aminomethyl(diphenyl)phosphine derived from fluoroloquinolones (IrPCp, IrPSf, IrPLm, IrPNr) were being studied as possible anticancer chemotherapeutics with potency higher than that of the other well-known metal-based...

Herein we present the synthesis of new complexes based on ruthenium(II) (Ru(η6-p-cymene)Cl2PPh2CH2OH (RuPOH), Ru(η6-p-cymene)Cl2P(p-OCH3Ph)2CH2OH (RuMPOH)) and iridium(III) (Ir(η5-Cp*)Cl2P(p-OCH3Ph)2CH2OH (IrMPOH), Ir(η5-Cp*)Cl2PPh2CH2OH (IrPOH) containing phosphine ligands with/without methoxy motif on phenyl rings...

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Novel heteronuclear Ir III −Cu II coordination compounds ([Ir(η 5 -Cp*)Cl 2 Pcfx-Cu(phen)](NO 3 )•1.75(CH 3 OH)•0.75(H 2 O) (1), [Ir(η 5 -Cp*)Cl 2 Pnfx-Cu(phen)](NO 3 )•1.75(CH 3 OH) 4)) bearing phosphines derived from fluoroquinolones, namely, sparfloxacin (Hsfx), ciprofloxacin (Hcfx), lomefloxacin (Hlfx), and norfloxacin (Hnfx), have been synthesized and studied as possible anticancer chemotherapeutics. All compounds have been characterized by electrospray ionization mass spectrometry (ESI-MS), a number of spectroscopic methods (i.e., IR, fluorescence, and electron paramagnetic resonance (EPR)), cyclic voltammetry, variable-temperature magnetic susceptibility measurements, and X-ray diffractometry. The coordination geometry of Ir III in all complexes adopts a characteristic piano-stool geometry with the η 5 -coordinated and three additional sites occupied by two chloride and phosphine ligands, while Cu II ions in complexes 1 and 2 form a distorted square-pyramidal coordination geometry, and in complex 3, the coordination geometry around Cu II ions is a distorted octahedron. Interestingly, the crystal structure of [Ir(η 5 -Cp*)Cl 2 Plfx-Cu(phen)] features the one-dimensional (1D) metal−organic polymer. Liposomes loaded with redox-active and fluorescent [Ir(η 5 -Cp*)Cl 2 Pcfx-Cu(phen)] (1L) have been prepared to increase water solubility and minimize serious systemic side effects. It has been proven, by confocal microscopy and an inductively coupled plasma mass spectrometry (ICP-MS) analysis, that the liposomal form of compound 1 can be effectively accumulated inside human lung adenocarcinoma and human prostate carcinoma cells with selective localization in nuclei. A cytometric analysis showed dominance of apoptosis over the other cell death types. Furthermore, the investigated nanoformulations induced changes in the cell cycle, leading to S phase arrest in a dose-dependent manner. Importantly, in vitro anticancer action on three-dimensional (3D) multicellular tumor spheroids has been demonstrated.

Three new coordination polymers, one-dimensional ones [Co(5,6-(Me)2–bzim)2(dca)2] (1), [Co(5-Mebzim)2(dca)2]n (2) and two-dimensional polymer [Co(2-Mebzim)(dca)2]n (3), show DC magnetic data consistent with the S = 3/2 spin system with large zero-field...

A group of cytotoxic half-sandwich iridium(III) complexes with aminomethyl(diphenyl)phosphine derived from fluoroquinolone antibiotics exhibit the ability to (i) accumulate in the nucleus, (ii) induce apoptosis, (iii) activate caspase-3/7 activity, (iv) induce the changes in cell cycle leading to G2/M phase arrest, and (v) radicals generation. Herein, to elucidate the cytotoxic effects, we investigated the interaction of these complexes with DNA and serum proteins by gel electrophoresis, fluorescence spectroscopy, circular dichroism, and molecular docking studies. DNA binding experiments established that the complexes interact with DNA by moderate intercalation and predominance of minor groove binding without the capability to cause a double-strand cleavage. The molecular docking study confirmed two binding modes: minor groove binding and threading intercalation with the fluoroquinolone part of the molecule involved in pi stacking interactions and the Ir(III)-containing region positioned within the major or minor groove. Fluorescence spectroscopic data (HSA and apo-Tf titration), together with molecular docking, provided evidence that Ir(III) complexes can bind to the proteins in order to be transferred. All the compounds considered herein were found to bind to the tryptophan residues of HSA within site I (subdomain II A). Furthermore, Ir(III) complexes were found to dock within the apo-Tf binding site, including nearby tyrosine residues.

Four solution-stable copper(ii) complexes of pyridine and pyridine-based alcohols were investigated by spectroscopic and thermal methods; the magnetic and anticancer properties were discussed as well.