Browsing by Author "Akkoc, Senem"

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A Benzimidazolium Salt Induces Apoptosis and Arrests Cells at Sub-G1 Phase in Epithelial Ovarian Cancer Cells
(Springer, 2024) Akar, Sakine; Cakir, Mustafa; Ozkol, Halil; Akkoc, Senem; Ozdem, Berna
BackgroundOvarian cancer, also known as a silent killer, is the deadliest gynecological cancer in women worldwide. Epithelial ovarian cancers constitute the majority of ovarian cancers, and diagnosis can be made in advanced stages, which greatly reduces the likelihood of treatment and lowers the survival rate. For the treatment of epithelial ovarian cancers, the search for synthetic agents as well as agents of natural origin continues. The effects of 1-(2-cyanobenzyl)-3-(4-vinylbenzyl)-1H-benzo[d]imidazole-3-ium chloride (BD), a benzimidazole derivative, were investigated on epithelial ovarian cancer cells.Methods and resultsIn our study, the effects of BD on proliferation, colony formation, cell death by apoptosis and the cell cycle in A2780 and A2780 Adriamycin (ADR) ovarian cancer cell lines were investigated. Proliferation was examined with cell viability analysis, colony formation and apoptosis with Annexin V staining and cell cycle analyses with PI staining, respectively. As a result of the analyses, BD inhibited cell proliferation and colony formation, induced apoptosis and cell death at 48 h in A2780 and A2780 ADR cells at 10.10 and 10.36 mu M concentrations, respectively. In addition, A2780 and A2780ADR cells were arrested in the Sub-G1 phase of the cell cycle.ConclusionsBD suppresses cancer cell progression by showing antiproliferative effects on ovarian cancer cells. Further analyses are required to determine the mechanism of action of this agent and to demonstrate its potential as a suitable candidate for the treatment of epithelial ovarian cancer.
A Benzimidazolium Salt Induces Apoptosis and Arrests Cells at Sub-G1 Phase in Epithelial Ovarian Cancer Cells (Vol 51, 66, 2024)
(Springer, 2024) Akar, Sakine; Cakir, Mustafa; Ozkol, Halil; Akkoc, Senem; Ozdem, Berna
Molecular Hybrid Design, Synthesis, in Vitro Cytotoxicity, in Silico Adme and Molecular Docking Studies of New Benzoate Ester-Linked Arylsulfonyl Hydrazones
(Mdpi, 2024) Ergan, Erdem; Cakmak, Resit; Basaran, Eyup; Mali, Suraj N.; Akkoc, Senem; Annadurai, Sivakumar
In this paper, we present the synthesis and characterization of two known sulfonyl hydrazides (1 and 2) and their new sulfonyl hydrazone derivatives (9-20), as well as in vitro and in silico investigations of their cytotoxic properties against human lung (A549) and human breast (MCF-7) cancer cell lines. The target compounds (9-20) obtained in high yields were synthesized for the first time by a multi-step reaction, and their structures were confirmed by elemental analysis and various spectral techniques, including FT-IR, 1H-, and 13C-NMR. The antiproliferative profiles of these compounds (1, 2, and 9-20) in this study were determined at concentrations of 200, 100, 50, and 25 mu M against selected cancer cell lines for 72 h using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method. Except for compounds 1 and 2, other compounds (9-20) demonstrated cytotoxic activity at concentrations lower than 200 mu M. The newly synthesized compounds (9-20) demonstrated antiproliferative activities at a micromolar level, with IC50 values in the range of 29.59-176.70 mu M for the A549 cell line and 27.70-170.30 mu M for the MCF-7 cell line. Among these compounds, compound 15 (IC50 = 29.59 mu M against A549 cell line and IC50 = 27.70 mu M against MCF-7 cell line) showed the highest cytotoxic activity against these two cancer cell lines compared to the reference drug cisplatin (IC50 = 22.42 mu M against A549 cell line and IC50 = 18.01 mu M against MCF-7 cell line). From docking simulations, to establish a plausible binding mode of compounds, we noticed that compound 15 demonstrated the highest affinity (-6.8508 kcal/mol) for estrogen receptor-beta (ERbeta) compared to others, suggesting promising ERbeta binding potential. Most compounds followed Lipinski's rule of five, with acceptable logP values. Additionally, all had mixed gastrointestinal absorption and limited blood-brain barrier permeability. Overall, our study proposed new sulfonyl hydrazones as a potential class of anticancer agents.
A Newly Synthesized Benzimidazolium Salt: 1-(2 Chloride as a Potential Anticancer Agent for Colon Cancer Treatment, in Vitro Study
(Wiley, 2025) Bitgen, Nazmiye; Cakir, Mustafa; Akkoc, Senem; Donmez-Altuntas, Hamiyet
Colon cancer is one of the most common cancer-related deaths. Drug resistance is one of the biggest challenges in cancer treatment. Numerous pharmacological and biochemical investigations have documented the benzimidazole ring's anticancer, anti-inflammatory, and antioxidant properties. Within the scope of our project, the effect of newly synthesized benzimidazolium salt (BS) on cell proliferation was tested with MTT assay, and its effect on apoptosis and cell cycle was tested with annexin V and PI in the two different colon cancer cell lines (HT-29 and DLD-1). Our study examined the expressions of some genes related to apoptosis and, additionally, caspase activities with the multicaspase kit.BS showed an antiproliferative effect at lower doses in HT-29 colon cancer cells. When HT-29 cells were exposed to a 20 mu M dosage, they showed increased caspase activity and apoptosis compared to DLD-1 cells. HT-29 accumulated in the G2/M phase of the cell cycle, whereas DLD-1 cells accumulated more in the S phase. In HT-29 cells, colony formation was inhibited; however, in DLD-1 cells, this effect was insufficient.Based on the apoptosis-death pathway, BS is expected to have anti-cancer effects. As a result of this work, this chemical was thoroughly examined in two different colon cancer cell lines, and additional, more comprehensive initiatives are being planned in light of the information obtained from this study.