Evaluation of anti-glioma effects of benzothiazoles as efficient apoptosis inducers and DNA cleaving agents

SEVER B., Ciftci H.

MOLECULAR AND CELLULAR BIOCHEMISTRY, vol.478, no.5, pp.1099-1108, 2023 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 478 Issue: 5
  • Publication Date: 2023
  • Doi Number: 10.1007/s11010-022-04580-4
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, CAB Abstracts, Chemical Abstracts Core, EMBASE, MEDLINE, Veterinary Science Database
  • Page Numbers: pp.1099-1108
  • Keywords: Benzothiazole, Glioma, Apoptosis, DNA cleavage activity, Molecular docking studies, BLOOD-BRAIN-BARRIER, GLIOMA-CELLS, IN-VITRO, C6, GROWTH, DERIVATIVES, DAMAGE, ASSAY
  • Anadolu University Affiliated: Yes


Glioma is the fast-growing, aggressive, and prevalent brain cancer with a great level of morbidity and mortality. Current therapy is usually found insufficient for glioma treatment. In the course of our research attempting to identify effective anti-glioma agents, three benzothiazole derivatives (1-3) were examined on U251 glioma cells. Among these derivatives, compound 3 was found to have the strongest cytotoxic effect on glioma cells with an IC50 value of 9.84 +/- 0.64 mu M in reference to cisplatin (IC50 = 8.41 +/- 1.27 mu M). Further mechanism of anti-glioma effects of compound 3 was characterized by the determination of its apoptotic effects in glioma cells and DNA cleaving capacity. Compound 3 caused a significant apoptotic death of U251 cell line. Besides, this compound cleaved DNA with FeSO4, H2O2 and ascorbic acid system. Molecular docking results also showed that compound 3 possessed a significant binding potential to DNA via important pi-pi stacking interaction with DG-16. Some pharmacokinetic determinants of compound 3 complied with standard limits making it as an efficient bioavailable anti-glioma drug candidate for upcoming exploration.