Zinc complexes with the third-generation quinolone antibacterial drugs levofloxacin and sparfloxacin have been synthesized characterized. The deprotonated quinolones act as bidentate ligands coordinated to zinc ion through pyridone a carboxylato oxygen atom. crystal structures of [bis(aqua)bis(levofloxacinato)zinc(II)], 1, [bis(sparfloxacinato)(1,10-phenanthroline)zinc(II)], 3, determined by X-ray crystallography. biological activity has evaluated examining their ability bind calf-thymus DNA...

Continuing the study of physicochemical and biological properties ruthenium-quinolone adducts, four novel complexes with general formula [Ru([9]aneS3)(dmso-κS)(quinolonato-κ2O,O)](PF6), containing quinolones levofloxacin (1), nalidixic acid (2), oxolinic (3), cinoxacin (4), were prepared characterized in solid state as well solution. Contrary to their organoruthenium analogues, these are generally relatively stable aqueous solution substitution dimethylsulfoxide (dmso) ligand is slow not...

Inspired by the emergence of resistance to currently available antifungal therapy and great potential metal complexes for treatment various diseases, we synthesized three new silver(I) containing clinically used azoles as ligands, [Ag(ecz)

With the aim of exploring anticancer properties organometallic compounds with bioactive ligands, Ru(arene) antibacterial quinolones nalidixic acid (2) and cinoxacin (3) were synthesized, their physicochemical compared to those chlorido(η(6)-p-cymene)(ofloxacinato-κ(2)O,O)ruthenium(II) (1). All undergo a rapid ligand exchange reaction from chlorido aqua species. 2 3 are significantly more stable than 1 minor conversion an unreactive [(cym)Ru(μ-OH)(3)Ru(cym)](+) species (cym = η(6)-p-cymene)....

An organometallic ruthenium complex of quinolone antibacterial agent ofloxacin, [(η6-p-cymene)RuCl(O,O-oflo)]·2.8H2O (1·2.8H2O), was isolated, and its crystal structure determined. In this “piano-stool” complex, is bidentately coordinated to the metal through ring carbonyl one carboxylic oxygen atoms. Interactions title with DNA were studied by spectroscopic methods [electronic, fluorescence, circular dichroism (CD)] atomic force microscopy (AFM). It established that electrostatic attraction...

The organoruthenium clioquinol complex induces copper-independent cell death in leukaemia cells by proteasome-independent inhibition of the NFκB signalling pathway.

With the aim of assessing whether ruthenium(II) compounds with meridional geometry might be utilized as potential antitumor agents, a series new, water-soluble, monofunctional complexes general formula mer-[Ru(L3)(N-N)X][Y]n (where L3 = 2,2′:6′,2″-terpyridine (tpy) or 4′-chloro-2,2′:6′,2″-terpyridine (Cl-tpy), N-N 1,2-diaminoethane (en), 1,2-diaminocyclohexane (dach), 2,2′-bipyridine (bpy); X Cl dmso-S; Y Cl, PF6, CF3SO3; n 1 2, depending on nature X) were synthesized. All fully...

A series of organoruthenium(II) chlorido complexes with fluorinated O,O-ligands [(η(6)-p-cymene)Ru(F3C-acac-Ar)Cl] (1a-6a) and their respective 1,3,5-triaza-7-phosphaadamantane (pta) derivatives [(η(6)-p-cymene)Ru(F3C-acac-Ar)pta]PF6 (1b-6b) were synthesized fully characterized in both solution solid state. All inactive against nonmalignant keratinocytes but displayed variable activity cancer cell models (ovarian, osteosarcoma). Compounds a ligand containing the 4-chlorophenyl substituent...

The β‐diketone scaffold is a key intermediate in the synthesis of COX‐2 inhibitors, type non‐steroidal anti‐inflammatory agents coxib family, which have also been shown to excellent anticancer potential at preclinical stage research. Moreover, it present family natural products named curcuminoids. Both and their synthetic analogues possess interesting antibacterial, neuroprotective properties. Coordination compounds curcuminoids with platinum‐group metals as are hot topic current research,...

Recognizing that metal ions play an important role in modifying the pharmacological properties of known organic-based drugs, present manuscript addresses complexation antifungal agent voriconazole (vcz) with biologically relevant silver(I) ion as a strategy for development new antimycotics. The synthesized complexes vcz were characterized by mass spectrometry, IR, UV–Vis and NMR spectroscopy single-crystal X-ray diffraction analysis. crystallographic results showed {[Ag(vcz)(H2O)]CH3SO3}n...

The Fe-based langasites are the only reported compounds presenting a magnetic ordering in this rich family, besides being well known for piezoelectric properties and optical activity. structural, magnetic, dielectric of Fe-langasite compounds, with various substitution nonmagnetic cations, have been studied x-ray neutron-diffraction, magnetostatic measurements, M\"ossbauer spectroscopy, measurements. title (trigonal space group $P321$) display helical order signatures frustration below...

The interaction of Zn(II) with the quinolone antibacterial drug flumequine (Hflmq) in presence or absence an N,N′-donor heterocyclic ligand, 2,2′-bipyridine (bipy), is being investigated. Interaction equimolar quantities ZnCl2 and results formation a structurally characterized [Zn(flmq)(bipy)Cl] (2) complex, while excess leads to [Zn(flmq)2(bipy)] (3) compound. reaction complex [Zn(flmq)2(H2O)2] (1). In all these complexes, deprotonated bidentate flumequinato ligands are coordinated zinc...

The thionated derivative of the antibacterial agent nalidixic acid and its organoruthenium complex were prepared, their crystal structures determined. aqueous stability was studied and, unlike case for nalidixicato complex, increased ruthenium in solution observed with only a minor degree thionalidixicato ligand dissociated within 1 week. While derivatization caused activity against E. coli to decrease, cytotoxicity three cancer cell lines significantly inhibitory potency two enzymes...

The interaction of cobalt(<sc>ii</sc>)–oxolinato complexes with DNA and albumins was investigated spectroscopic physicochemical techniques molecular docking calculations.

Nine organoruthenium complexes with azole antifungal agents (L) clotrimazole (ctz), tioconazole (tcz), and miconazole (mcz) the general formulas [(η6-p-cymene)RuCl2(L)], [(η6-p-cymene)RuCl(L)2]Cl, [(η6-p-cymene)Ru(L)3](PF6)2 were prepared characterized by NMR, HRMS, IR, UV–vis, X-ray crystallography. Herein, we report first crystal structure of a metal complex as well ligand itself bis-clotrimazole hexafluorophosphate salt. The possess pseudooctahedral geometry typical for...

Abstract The purpose of this work was to screen the antitumor actions two metal organoruthenium-8-hydroxyquinolinato (Ru-hq) complexes find a potential novel agent for bone, lung and breast chemotherapies. We showed that ruthenium compounds (1 2) impaired cell viability human bone (MG-63), (A549) (MCF7) cancer cells with greater selectivity specificity than cisplatin. Besides, 1 2 decreased proliferation, migration invasion on monolayers at lower concentrations (2.5–10 μM). In addition, both...

Zinc pyrithione (1a), together with its analogues 1b-h and ruthenium complex 2a, were synthesised evaluated for the stability in biologically relevant media anti-SARS-CoV-2 activity. revealed potent vitro inhibition of cathepsin L (IC50=1.88 ± 0.49 µM) PLPro (IC50=0.50 0.07 µM), enzymes involved SARS-CoV-2 entry replication, respectively, as well antiviral replication properties an ex vivo system derived from primary human lung tissue. complexes expressed comparable inhibition. On contrary,...

Abstract From the point of view medicinal chemistry, thiosemicarbazones are interesting molecules as they exhibit various biological activities, such antitumor, antifungal, antibacterial, antiviral, and antileukemic properties, their synthesis is deeply investigated. However, using 2‐methylthiosemicarbazide a starting compound to prepare new 1,2,4‐triazolidine‐3‐thione compounds via 2‐methylthiosemicarbazone cyclization has not been reported yet. Therefore, fifteen were synthesized during...

A series of 16 Pt(<sc>ii</sc>) complexes with 8-hydroxyquinolines and sulfoxide/phosphine ligands were synthetized, characterized evaluated for cytotoxic embryotoxic activity.

Lysosomal cysteine peptidase cathepsin B (catB) is an important tumor-promoting factor involved in tumor progression and metastasis representing a relevant target for the development of new antitumor agents. In present study, we synthesized 11 ruthenium compounds bearing either clinical agent nitroxoline that was previously identified as potent selective reversible inhibitor catB activity or its derivatives. We demonstrated organoruthenation viable strategy obtaining highly effective...