Background

The study aims to evaluate the potential of trifluoromethyl thioxanthene derivatives across various biological activities, including antioxidant properties, anti-amylase effects, pancreatic lipase inhibition, anticancer activity, and COX inhibition. This research offers insights into the therapeutic applications of these compounds for managing metabolic disorders and inflammation.

Method

Tertiary alcohols were synthesized using Grignard reagents and subsequently combined with L-cysteine, with their structures confirmed via NMR and IR spectroscopy.

Results

The results indicated compound 3 exhibited the highest antioxidant potential, with 46.6% at 80 µg/mL in the DPPH assay. Compound 4 showed moderate pancreatic lipase inhibition, exhibiting an IC₅₀ range of 100.6 to 277 µM. Compound 1 revealed potent anticancer activity against HeLa cells, with an IC₅₀ of 87.8 nM. Compound 2 showed a potent antioxidant and anti-amylase activity with IC₅₀ of 1.67 ± 0.5 and 60.2 ± 0.8 µM, respectively. Furthermore, the synthesized compounds 1, 3, and 4 displayed promising COX-2 inhibition with IC₅₀ values ranging from 6.5 to 27.4 nM, suggesting potential anti-inflammatory benefits.

Conclusions

This study highlights the significant biological activities of trifluoromethyl thioxanthene derivatives, positioning them as promising candidates for the treatment of cancer, metabolic disorders, and inflammation. These compounds demonstrated noteworthy antioxidant and enzyme inhibition properties, warranting further in vivo studies to confirm their therapeutic efficacy.

Title

Pharmaceuticals

Publisher

MDPI

Publisher Country

Switzerland

Indexing

Scopus

Impact Factor

4.0

Publication Type

Both (Printed and Online)

Volume

18

Year

2025

Pages

561