Biological Evaluation of Xanthene and Thioxanthene Derivatives as Antioxidant, Anticancer, and COX Inhibitors.

ACS Omega

Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, P.O. Box 7, P400 Nablus, Palestine.

Published: October 2023

Xanthene and thioxanthene analogues have been investigated for their potential as anticancer and anti-inflammatory agents. Additionally, cysteine analogues have been found to possess antioxidant, anti-inflammatory, and anticancer activities due to their role in cellular redox balance, scavenging of free radicals, and involvement in nucleophilic reactions and enzyme binding sites. In this study, we synthesized a library of tertiary alcohols derived from xanthene and thioxanthene, and further, some of these compounds were coupled with cysteine. The objective of this research was to explore the potential anticancer, antioxidant, and anti-inflammatory activities of the synthesized compounds. The synthesized compounds were subjected to test for anticancer, antioxidant, and anti-inflammatory activities. Results indicated that compound exhibited excellent inhibition activity (IC = 9.6 ± 1.1 nM) against colon cancer cells (Caco-2), while compound showed good inhibition activity (IC = 161.3 ± 41 nM) against hepatocellular carcinoma (Hep G2) cells. Compound demonstrated potent antioxidant inhibition activity (IC = 15.44 ± 6 nM), and compound exhibited potent anti-inflammatory activity with cyclooxygenase-2 (COX-2) inhibition IC (4.37 ± 0.78 nM) and high selectivity for COX-2 (3.83). In conclusion, certain synthesized compounds displayed promising anticancer activity and anti-inflammatory effects. Nevertheless, additional research is necessary to create more analogues, develop a more distinct comprehension of the structure-activity relationship (SAR), and perform in vivo experiments to evaluate the pharmacokinetic and pharmacodynamic characteristics of the compounds under examination. Such research may pave the way for the development of novel therapeutic agents with potential applications in cancer and inflammatory diseases.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10586285PMC
http://dx.doi.org/10.1021/acsomega.3c05695DOI Listing

Publication Analysis

Top Keywords

xanthene thioxanthene
12
antioxidant anti-inflammatory
12
synthesized compounds
12
inhibition activity
12
potential anticancer
8
anticancer antioxidant
8
anti-inflammatory activities
8
compound exhibited
8
anticancer
6
anti-inflammatory
6

Similar Publications

Article Synopsis
  • New organic luminophores called bis(tricyclic) aromatic enes (BAEs), featuring 6-6-6-membered frameworks like acridine and xanthene, display blue-to-green fluorescence in solid states and polymer films with high quantum yields.
  • These BAEs are synthesized through a palladium-catalyzed double cross-coupling reaction, producing microcrystals or powders that fluoresce brilliantly.
  • Theoretical calculations indicate that their light absorption involves π-π* transitions, with a distinct charge transfer occurring in the 10,10-dioxido-9-thioxanthene variant.
View Article and Find Full Text PDF

Early inhibition of the ATM/p53 pathway reduces the susceptibility to atrial fibrillation and atrial remodeling following acute myocardial infarction.

Cell Signal

October 2024

Graduate School of Dalian Medical University, Dalian 116000, Liaoning Province, China; State Key Laboratory of Frigid Zone Cardiovascular Disease, Department of Cardiovascular Surgery, General Hospital of Northern Theater Command, Shenyang 110016, Liaoning Province, China. Electronic address:

Atrial fibrillation (AF) emerges as a critical complication following acute myocardial infarction (AMI) and is associated with a significant increased risk of heart failure, stroke and mortality. Ataxia telangiectasia mutated (ATM), a key player in DNA damage repair (DDR), has been implicated in multiple cardiovascular conditions, however, its involvement in the development of AF following AMI remains unexplored. This study seeks to clarify the contribution of the ATM/p53 pathway in the onset of AF post-AMI and to investigate the underlying mechanisms.

View Article and Find Full Text PDF

Background: Flupentixol and melitracen are being investigated for their potential effectiveness in managing persistent idiopathic facial pain (PIFP), based on their mechanisms of action as dopamine receptor antagonists and noradrenaline/serotonin reuptake inhibitors, respectively. The efficacy and safety of flupentixol and melitracen (FM) tablets in treating PIFP were retrospectively analyzed at our hospital.

Objectives: The aim of this study is to determine the effectiveness and safety of FM tablets in treating PIFP.

View Article and Find Full Text PDF

Background: To investigate the effect of raltitrexed + X-ray irradiation on esophageal cancer ECA109 cells and analyze the potential action mechanism.

Methods: The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to analyze the inhibitory effect of raltitrexed on cell proliferation. The effect of raltitrexed on radiosensitivity was studied through a clone-forming experiment.

View Article and Find Full Text PDF

In this study, a series of halogen-substituted thioxanthenes were synthesized because the most important and biologically active derivatives of xanthenes are thioxanthenes. In order to obtain new thioxanthene derivatives, first, the starting molecules were synthesized by the appropriate reaction methods in two steps. The intramolecular Friedel-Crafts alkylation (FCA) method was used to convert the prepared three aromatic substituted starting alcohol compounds to their corresponding thioxanthenes by cyclization.

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!