New copper-based complexes with quinoxaline N1,N4-dioxide derivatives, potential antitumoral agents.

J Inorg Biochem

Cátedra de Química Inorgánica, Facultad de Química, Universidad de la República, Gral Flores 2124, C.C. 1157, 11800 Montevideo, Uruguay.

Published: January 2008

Taking into account our previous studies on cytotoxic metal compounds, new copper complexes with 3-aminoquinoxaline-2-carbonitrile N1,N4-dioxide derivatives as ligands were synthesized and characterized by different spectroscopic methods. The hypoxic selective cytotoxicity towards V79 cells and the superoxide dismutase-like activity of the complexes were determined and related to physicochemical properties of the compounds. In particular, the copper(II) complex with 3-amino-6-chloro-7-fluoroquinoxaline-2-carbonitrile N1,N4-dioxide showed cytotoxic selectivity in hypoxia being the most lipophilic compound of the series. On the contrary, the complex with 3-aminoquinoxaline-2-carbonitrile N1,N4-dioxide was cytotoxic but not selective and that with 3-amino-7-chloro-6-methoxy-quinoxaline-2-carbonitrile N1,N4-dioxide was not cytotoxic towards V79 cells neither in oxia nor in hypoxia in the assayed conditions. The sigmam Hammett substituent electronic descriptor was related to the effect in hypoxic conditions and the SOD-like activity was correlated to the effect in normoxia.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.jinorgbio.2007.07.028DOI Listing

Publication Analysis

Top Keywords

n1n4-dioxide cytotoxic
12
n1n4-dioxide derivatives
8
3-aminoquinoxaline-2-carbonitrile n1n4-dioxide
8
v79 cells
8
n1n4-dioxide
5
copper-based complexes
4
complexes quinoxaline
4
quinoxaline n1n4-dioxide
4
derivatives potential
4
potential antitumoral
4

Similar Publications

Pharmacological Management of IgG4-Related Disease: From Traditional to Mechanism-Based Targeted Therapies.

Drugs Aging

January 2025

Division of Rheumatology, Department of Internal Medicine, Keio University School of Medicine, 35 Shinanomachi, Shinjuku-ku, Tokyo, 160-8582, Japan.

IgG4-related disease (IgG4-RD) is an immune-mediated disorder characterized by organ enlargement and dysfunction. The formation of tertiary lymphoid tissues (TLTs) in affected organs is crucial for understanding IgG4-RD, as T follicular helper (Tfh) 2 cells within TLTs drive IgG4+B cell differentiation, contributing to mass formation. Key cytokines IL-4 and IL-10, produced by Tfh2 cells, are essential for this process.

View Article and Find Full Text PDF

β-secretase (BACE1) is instrumental in amyloid-β (Aβ) production, with overexpression noted in Alzheimer's disease (AD) neuropathology. The interaction of Aβ with the receptor for advanced glycation endproducts (RAGE) facilitates cerebral uptake of Aβ and exacerbates its neurotoxicity and neuroinflammation, further augmenting BACE1 expression. Given the limitations of previous BACE1 inhibition efforts, the study explores reducing BACE1 expression to mitigate AD pathology.

View Article and Find Full Text PDF

Exposure to vanadium (V) occurs through the ingestion of contaminated water, polluted soil, V-containing foods and medications, and the toxicity and absorption during the small intestine phase after oral ingestion play crucial roles in the ultimate health hazards posed by V. In this study, the human colon adenocarcinoma (Caco-2) cells were selected as an intestinal absorption model to investigate the uptake and cytotoxicity of vanadyl sulfate (VOSO) and sodium orthovanadate (NaVO). Our results confirmed the cytotoxic effects of V(IV) and V(V) and revealed a greater toxicity of V(IV) than V(V) towards Caco-2 cells.

View Article and Find Full Text PDF

SENP3 inhibition suppresses hepatocellular carcinoma progression and improves the efficacy of anti-PD-1 immunotherapy.

Cell Death Differ

January 2025

Division of Hepatobiliary and Transplantation Surgery, Department of General Surgery, Nanjing Drum Tower Hospital, the Affiliated Hospital of Medical School, Nanjing University, Nanjing, China.

The importance of SUMOylation in tumorigenesis has received increasing attention, and research on therapeutic agents targeting this pathway has progressed. However, the potential function of SUMOylation during hepatocellular carcinoma (HCC) progression and the underlying molecular mechanisms remain unclear. Here, we identified that SUMO-Specific Peptidase 3 (SENP3) was upregulated in HCC tissues and correlated with a poor prognosis.

View Article and Find Full Text PDF

Although the antiallergic properties of compounds such as CAPE, Melatonin, Curcumin, and Vitamin C have been poorly discussed by experimental studies, the antiallergic properties of these famous molecules have never been discussed with calculations. The histamine-1 receptor (H1R) belongs to the family of rhodopsin-like G-protein-coupled receptors expressed in cells that mediate allergies and other pathophysiological diseases. In this study, pharmacological activities of FDA-approved second generation H1 antihistamines (Levocetirizine, desloratadine and fexofenadine) and molecules such as CAPE, Melatonin, Curcumin, Vitamin C, ADMET (Absorption, Distribution, Metabolism, Excretion, Toxicity) profiles, density functional theory (DFT), molecular docking, biological targets and activities were compared by calculating.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!