A Thiophene Derivative, 2‐Bromo‐5‐(2‐(methylthio)phenyl)thiophene, Has Effective Anticancer Potential with Other Biological Properties

Abstract

Thiophene derivatives are studied intensively due to their anticancer, antimicrobial, antioxidant and some other clinically important properties. In this study, the biological properties of a new thiophene derivative, so called BMPT, with a moderate drug score of 0.29 were tested. BMPT showed selective cytotoxicity for LnCap, HepG2 and Caco‐2 cancer cell lines with EC50 values of 138.573 μM, 185.931 μM, and 108.657 μM, respectively, but not on the control cell line HEK293. The increased expressions were detected for caspase3, caspase8, caspase9 and Bax; but Bcl‐2 expressions were decreased at cancer cell lines. BMPT decreased the total thiol content and total GST activities at HepG2 47 % and 40 %, respectively, and, molecular docking supported inhibitory models for GSTP1‐1, GSTA1‐1 and GSTM2‐2 were mixed, uncompetitive and uncompetitive, respectively. BMPT also showed potent antibacterial activity against Staphylococcus aureus. Related with its selective inhibition on GST activities, BMPT is proposed to have significant apoptotic effect leaded by changes, especially, in caspase 3, Bcl‐2 and Bax expressions.

The effects of different Charleston pepper cultivars on the demographic parameters and the antioxidant levels of Myzus persicae (Sulzer, 1776) (Hemiptera: Aphididae)

“…As a result, the cells enter apoptosis. In other words, reducing the GSH level of cells predisposes those cells to apoptosis and/or directly induces cell death (Yılmaz et al, 2022). When we evaluated our results according to GST-CDNB, and total thiol (GSH) levels, the lowest total thiol, and the lowest GST activity were determined in M. persicae individuals fed with the Kanyon cultivar.…”

Synthesis, Characterization, Molecular Docking and in vitro Anticancer Screening of Some Novel Thiophene Derivatives

“…[20][21][22][23][24][25][26][27][28][29] So In our recent studies we unfolded our research to findings insides of synthesis and biological studies of thiophene derivatives. [30][31][32][33][34][35][36] A novel substituted thiophene analogues were designed, synthesized and screened for anticancer activity against U87-MG cell line. All these novel compounds are chemically synthesized in fewer steps.…”

“…Also there is lot of research on the medicinal significance of thiophen [20–29] . So In our recent studies we unfolded our research to findings insides of synthesis and biological studies of thiophene derivatives [30–36] . A novel substituted thiophene analogues were designed, synthesized and screened for anticancer activity against U87‐MG cell line.…”