Ruthenium(II)-mercapto complexes induce cell damage via apoptosis pathway on ovarian cancer cells.

Ovarian cancer represents a leading cause of cancer-related deaths in women worldwide. Chemotherapeutic agents are usually employed to treat the patients, and Ruthenium(II)-based compounds have been investigated as possible substitutes for platinum drugs. In this work, we studied three different Ru(II)-phosphine-mercapto complexes (1-3) as potential cytotoxic agents against A2780 and A2780-cisR ovarian cancer cells.

Cytotoxic Ruthenium(II)-Diphosphine Complexes Affect the Mitochondrial Respiration of Lung Cancer Cells.

In this work, we studied six Ruthenium(II)-diphosphine compounds containing different mercapto ligands (N-S), with general formula [Ru(N-S)(dppm)]Cl (dppm=1,1-bis(diphenylphosphino)methane). These compounds were characterized by several techniques (NMR [H, P(H), and C], HRMS, IR, UV-Vis and XRD) and their purity confirmed by elemental analysis. DLS experiments revealed low diameters and polydispersity indexes, and positive log P values in n-octanol/PBS indicated their preference for the organic phase.

Terpyridine-based ruthenium complexes containing a 4,5-diazafluoren-9-one ligand with light-driven enhancement of biological activity.

There has been growing effort in the scientific community to develop new antibiotics to address the major threat of bacterial resistance. One promising approach is the use of metal complexes that provide broader opportunities. Among these systems, polypyridine-ruthenium(II) complexes have received particular attention as drug candidates.

Ru(II)-diphosphine/N,S-mercapto complexes and their anti-melanoma properties.

We have synthesized and characterized a novel series of ruthenium complexes with formulas [RuCl(N-S)(dppm)]PF (Ru1), [Ru(N-S)(dppm)]PF (Ru2), [Ru(N-S)(dppe)]PF (Ru3), [Ru(N-S)(dppen)]PF (Ru4), [Ru(N-S)(bpy)]PF (Ru5). In these formulas, N-S or S represents H2mq (2-mercapto-4(3)-quinazoline); dppe (1,2'-bis(diphenylphosphine)ethane), dppm (1,1'-bis(diphenylphosphine)methane), or dppen (1,2'-bis(diphenylphosphine)ethene); and bpy refers to 2,2'-bipyridine. We have also compared the cytotoxicity of cisplatin with these ruthenium complexes to murine melanoma cells (B16-F10), human melanoma cells (A-375), and the non-tumoral human keratinocyte cell line (HaCat).

Minimal Functionalization of Ruthenium Compounds with Enhanced Photoreactivity against Hard-to-Treat Cancer Cells and Resistant Bacteria.

Metallocompounds have emerged as promising new anticancer agents, which can also exhibit properties to be used in photodynamic therapy. Here, we prepared two ruthenium-based compounds with a 2,2'-bipyridine ligand conjugated to an anthracenyl moiety. These compounds coded and contain 2,2'-bipyridine or 1,10-phenathroline as auxiliary ligands, respectively, which provide quite a distinct behavior.

Exploring the potential of ruthenium(II)-phosphine-mercapto complexes as new anticancer agents.

The search for new metal-based anticancer drug candidates is a fundamental task in medicinal inorganic chemistry. In this work, we assessed the potential of two new Ru(II)-phosphine-mercapto complexes as potential anticancer agents. The complexes, with the formula [Ru(bipy)(dppen)(Lx)]PF [(1), HL1 = 2-mercapto-pyridine and (2), HL2 = 2-mercapto-pyrimidine, bipy = 2,2'-bipyridine, dppen = -1,2-bis(diphenylphosphino)-ethylene] were synthesized and characterized by nuclear magnetic resonance (NMR) [H, P(H), and C], high resolution mass spectrometry (HR-MS), cyclic voltammetry, infrared and UV-Vis spectroscopies.

Novel naphthoquinone-1H-1,2,3-triazole hybrids: Design, synthesis and evaluation as inductors of ROS-mediated apoptosis in the MCF-7 cells.

The search for novel anticancer drugs is essential to expand treatment options, overcome drug resistance, reduce toxicity, promote innovation, and tackle the economic impact. The importance of these studies lies in their contribution to advancing cancer research and enhancing patient outcomes in the battle against cancer. Here, we developed new asymmetric hybrids containing two different naphthoquinones linked by a 1,2,3-1H-triazole nucleus, which are potential new drugs for cancer treatment.

Cobalt(III)-pyen systems as potential carriers of β-ketoester-based ligands.

Two cobalt(III) complexes containing different β-ketoesters, namely [Co(L1)(pyen)](ClO)·HO (1) and [Co(L2)(pyen)](ClO) (2) (pyen = N,N'-bis(pyridin-2-ylmethyl)ethylenediamine; L1 = methylacetoacetate; L2 = ethyl 4-chloroacetoacetate) have been prepared and investigated as prototypes of bioreductive prodrugs. The presence of β-ketoester and pyen ligands in 1 and 2, as well as the perchlorate counterions, was supported by IR spectroscopy and CHN elemental analysis. The composition molecular structure of both complexes was confirmed by NMR spectroscopy and ESI mass spectrometry.

Spectroscopic, Electrochemical, and Biological Assays of Copper-Binding Molecules for Screening of Different Drugs and Plant Extracts against Neurodegenerative Disorders.

Neurodegenerative disorders, caused by prone-to-aggregation proteins, such as Alzheimer disease or Huntington disease, share other traits such as disrupted homeostasis of essential metal ions, like copper. In this context, in an attempt to identify Cu chelating agents, we study several organic compounds (ethylenediaminetetraacetic acid, phenylenediamine, metformin, salicylate, and trehalose) and organic extracts obtained from L., which has been used in Ayurvedic therapies and presented a broad spectrum of biological properties.

Antimycobacterial and anti-inflammatory activities of thiourea derivatives focusing on treatment approaches for severe pulmonary tuberculosis.

Tuberculosis (TB) remains a serious public health problem and one of the main concern is the emergence of multidrug-resistant and extensively resistant TB. Hyper-reactive patients develop inflammatory necrotic lung lesions that aggravate the pathology and facilitate transmission of mycobacteria. Treatment of severe TB is a major clinical challenge that has few effective solutions and patients face a poor prognosis, years of treatment and different adverse drug reactions.

Chalcones identify cTXNPx as a potential antileishmanial drug target.

With current drug treatments failing due to toxicity, low efficacy and resistance; leishmaniasis is a major global health challenge that desperately needs new validated drug targets. Inspired by activity of the natural chalcone 2',6'-dihydroxy-4'-methoxychalcone (DMC), the nitro-analogue, 3-nitro-2',4',6'- trimethoxychalcone (NAT22, 1c) was identified as potent broad spectrum antileishmanial drug lead. Structural modification provided an alkyne containing chemical probe that labelled a protein within the parasite that was confirmed as cytosolic tryparedoxin peroxidase (cTXNPx).

DNA-interacting properties of two analogous square-planar cis-chlorido complexes: copper versus palladium.

Two square-planar coordination compounds, namely [Cu(CPYA)Cl] (1) and [Pd(CPYA)Cl] (2), were prepared from the ligand 4-chloro-N-(pyridin-2-ylmethyl)aniline (CPYA) and two chloride salts, and were fully characterized, including by X-ray diffraction. Spectroscopic, electrophoretic and AFM studies revealed that the two isostructural compounds were interacting differently with DNA. In both cases, the initial interaction involves electrostatic contacts of the CPYA ligand in the minor groove (as suggested by molecular docking), but subsequent strong binding occurs with the palladium(II) complex 2, whereas the binding with the copper complex 1 is weaker and concentration dependent.

Evaluation of cobalt(III) complexes as potential hypoxia-responsive carriers of esculetin.

Differentiation between hypoxic and normoxic tissues have been exploited for the development of selective chemotherapeutic agents. In this context, cobalt(III)-based coordination compounds have been designed and investigated as prospective hypoxia-responsive drug delivery systems. Three cobalt(III) complexes, namely [Co(esc)(pyen)]ClO·(CHOH) (1) [Co(esc)(TPA)]ClO·3HO (2) and [Co(bipy)(esc)]ClO·2.