Abualhasan Murad, Haider Hussein, Odeh Ahmad, Daraghmeh Amer
Faculty of Pharmacy, An-Najah National University, Nablus 00970, Palestine.
Pharmaceuticals (Basel). 2025 Apr 11;18(4):561. doi: 10.3390/ph18040561.
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. Tertiary alcohols were synthesized using Grignard reagents and subsequently combined with L-cysteine, with their structures confirmed via NMR and IR spectroscopy. The results indicated compound exhibited the highest antioxidant potential, with 46.6% at 80 µg/mL in the DPPH assay. Compound showed moderate pancreatic lipase inhibition, exhibiting an IC range of 100.6 to 277 µM. Compound revealed potent anticancer activity against HeLa cells, with an IC of 87.8 nM. Compound showed a potent antioxidant and anti-amylase activity with IC of 1.67 ± 0.5 and 60.2 ± 0.8 µM, respectively. Furthermore, the synthesized compounds , , and displayed promising COX-2 inhibition with IC values ranging from 6.5 to 27.4 nM, suggesting potential anti-inflammatory benefits. 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.
该研究旨在评估三氟甲基噻吨衍生物在各种生物活性方面的潜力,包括抗氧化性能、抗淀粉酶作用、胰脂肪酶抑制、抗癌活性和COX抑制。这项研究为这些化合物在治疗代谢紊乱和炎症方面的应用提供了见解。使用格氏试剂合成叔醇,随后将其与L-半胱氨酸结合,并通过核磁共振和红外光谱确认其结构。结果表明,化合物在DPPH测定中在80 µg/mL时表现出最高的抗氧化潜力,为46.6%。化合物表现出中等程度的胰脂肪酶抑制作用,IC范围为100.6至277 µM。化合物对HeLa细胞显示出有效的抗癌活性,IC为87.8 nM。化合物分别具有有效的抗氧化和抗淀粉酶活性,IC分别为1.67±0.5和60.2±0.8 µM。此外,合成的化合物、和显示出有前景的COX-2抑制作用,IC值范围为6.5至27.4 nM,表明具有潜在的抗炎益处。这项研究突出了三氟甲基噻吨衍生物的显著生物活性,使其成为治疗癌症、代谢紊乱和炎症的有前景的候选物。这些化合物表现出值得注意的抗氧化和酶抑制特性,需要进一步的体内研究来证实其治疗效果。