Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
Permanent URI for this collectionhttps://hdl.handle.net/11147/7148
Browse
2 results
Search Results
Article Design, Synthesis, and Evaluation of Anticancer Activities of 1,2-Diborolane Derivatives for Hepatocellular Carcinoma: an in Vitro and in Silico Study(Elsevier, 2026) Sahin, Yuksel; Antika, Gizem; Aktan, Cagdas; Metin, Kubilay; Ozgener, HuseyinHepatocellular carcinoma (HCC) is the most prevalent form of primary liver cancer and remains a major global health challenge due to limited treatment options and poor prognosis. Boron-containing compounds have garnered attention for their diverse biological activities, including pro-apoptotic effects in various types of cancer. In this study, we synthesized a panel of novel 1,2-N-substituted-1,2-diborolane derivatives and evaluated their antiproliferative, antimigratory, and apoptotic effects on hepatocellular carcinoma cell lines, HepG2 and Hep3B. Spectroscopic analyses confirmed the structural integrity of the synthesized compounds, revealing characteristic 1H-, 11B-, and 13C-NMR shifts consistent with boron-oxygen and boron-nitrogen bonding patterns. The derivatives, particularly compounds 2, 3, and 6, demonstrated potent and selective cytotoxicity toward HCC cells, with compound 3 exhibiting the lowest IC50 value (6.75 mu M) in HepG2 cells. Their time-dependent anti-proliferative effects were further supported by colony formation assays demonstrating long-term growth suppression, while wound healing assays revealed marked inhibition of HepG2 cell migration, indicating the compound's anti-metastatic potential. Our results demonstrate that the compound significantly induces apoptosis, modulates the expression of key apoptotic genes (Bax, Bcl-2, and caspase-3). In silico molecular docking further confirmed strong binding affinity to the anti-apoptotic Bcl-2 protein, supporting the proposed mechanism of action. These findings highlight the compound as a promising candidate for further preclinical evaluation in liver cancer therapy.Article Citation - WoS: 5Citation - Scopus: 5Effects of Diborolane Containing Oxo/Amine Compounds on Clinically Important Bacteria and Candida Species(Elsevier B.V., 2024) Şahin,Y.; Çoban,E.P.; Özgener,H.; Bıyık,H.H.; Sevincek,R.; Aygün,M.; Gürbüz,B.A good yield of 1,2-diborolanderivatives 2-8 was obtained from the reaction of 1,2-dichloro-1,2-diborolane 1 and R2NLi/ArNHLi/PhOLi/H2O. The structures of these new derivatives were characterized by nuclear magnetic resonance spectroscopy. The molecular structures of 4 and 7a were also determined using single-crystal X-ray diffraction. The antimicrobial activities of synthesized compounds were tested against clinically important Gram-positive, Gram-negative bacteria, and Candida species. The most effective substances were found to be compounds 2, 3, 4, 6 and 8 among the tested compounds. Therefore, the activity of these substances were investigated against Staphylococcus aureus ATCC 43300 and Enterococcus faecalis ATCC 51575, which form biofilms and have antibiotic resistance. Compound 2, 6 and 8 appears to be a promising candidate for potential antibacterial agents against these bacterial strains, especially given its potent activity against biofilm-forming and antibiotic resistant strains. The results indicate that these new materials will be evaluated as potential drugs against infectious diseases in the future. © 2024 Elsevier B.V.