WoS İndeksli Yayınlar Koleksiyonu
Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/6
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Article 1,2,4-Triazole Conjugates as HEGFR Inhibitors: Synthesis, Anticancer Evaluation, and in Silico Studies(Wiley-V C H Verlag GmbH, 2026) Bulbul, Bahadir; Kulabas, Necla; Gurboga, Merve; Ozakpinar, Ozlem Bingol; Cakmak, Ummuhan; Tuncay, Fulya Oz; Kucukguzel, IlkayA series of novel 1,2,4-triazole-acetamide derivatives was synthesized and evaluated for anticancer and hEGFR inhibitory activity. The compounds were obtained via multistep synthesis and characterized by spectroscopic methods. Cytotoxicity was tested against PC-3, MCF-7, A549, and K562 cell lines. Compounds <bold>18</bold>, <bold>19</bold>, and especially <bold>24</bold> showed notable antiproliferative effects, with compound <bold>24</bold> exhibiting higher selectivity and potency than gefitinib. It also induced apoptosis and inhibited migration in A549 and PC-3 cells, while selectively promoting invasion in PC-3, suggesting EMT-related behavior. In vitro kinase assays revealed compound <bold>20</bold> as the most potent hEGFR inhibitor (IC50 = 43.8 +/- 1.3 nM). Molecular docking and 200 ns molecular dynamics simulations confirmed its stable interaction with EGFR, particularly involving Cys797. These findings highlight compounds <bold>20</bold> and <bold>24</bold> as promising candidates for further development as EGFR-targeted anticancer agents.Article The Relation Between Personality Traits and Chemotherapy Symptoms of Cancer Patients(Marmara Univ, Inst Health Sciences, 2025) Özkan, İlknur; Taylan, Seçil; Eroglu, Nermın; Kolac, NurcanObjective:This study is important as it is one of the first studies to evaluate the relationship between personality traits and symptoms. Methods:This study was planned as descriptive and cross-sectional. The study was conducted with 468 patients who were voluntary to participate in the study and applied to the chemotherapy unit in a private oncology hospital in Istanbul between January-June 2019. Data were obtained using the Patient Information Form, Chemotherapy Symptom Assessment Scale (C-SAS), and Big Five Inventory. Results:The data were evaluated on computer environment. The mean age of the patients was 59.46±11.78 years, 59.8% are female, 35.7% were secondary school graduate, and 36.5% were housewives.When the mean scores of the big five inventory were examined, it was found that the mean scores were 29.72±3.38 in Extraversion subscale, 28.31±5.62 in Agreeableness subscale, 27.14±4.44 in Conscientiousness subscale, 25.26±3.31 in Neuroticism subscale, and 28.31±5.62 in Openness subscale. One-unit increase in neuroticism was determined to increase post-treatment nausea by 1.14 times, diarrhea by 1.28 times, change in sexual life by 1.14 times, feeling pessimistic and sad by 1.071 times, and feeling anxious and distressed by 1.08 times. Conclusion:It was observed that the personality traits of cancer patients were correlated with the symptoms they experienced related to chemotherapy and the symptoms decreased with the increase of openness, extraversion, agreeableness and conscientiousness characteristics and the symptoms increased with the increase of neuroticism characteristic.These results indicated that healthcare professionals should consider personnel characteristics of cancer patients while evaluating the symptoms they experienced and providing care.Article Citation - WoS: 7Citation - Scopus: 5Synthesis and Evaluation of Novel Metacetamol Derivatives With Hydrazone Moiety as Anticancer and Antimicrobial Agents(Wiley-v C H verlag Gmbh, 2023) Senkardes, Sevil; Atlihan, Irem; Cayir, Elif; Tiber, Pinar Mega; Orun, Oya; Nigiz, Seyma; Kucukguzel, S. Guniz; Mega Tiber, PınarBy exploiting the wide biological potential of the hydrazone scaffold, a series of hydrazone derivatives were synthesized, starting from N-(3-hydroxyphenyl)acetamide (metacetamol). The structures of the compounds were determined using IR, H-1 and C-13-NMR, and mass spectroscopic methods. The obtained molecules (3 a-j) were evaluated for their anticancer potential against MDA-MB-231 and MCF-7 breast cancer cell lines. According to the CCK-8 assay, all tested compounds showed moderate to potent anticancer activity. Among them, N-(3-(2-(2-(4-nitrobenzylidene)hydrazinyl)-2-oxoethoxy)phenyl)acetamide (3 e) was found to be the most effective derivative with an IC50 value of 9.89 & mu;M against MDA-MB-231 cell lines. This compound was further tested for its potential effects on the apoptotic pathway. Molecular docking studies was also carried out for 3 e in the colchicine binding pocket of tubulin. Additionally, compound 3 e also demonstrated effective antifungal activity, particularly against Candida krusei (MIC=8 & mu;g/ml), indicating that nitro group at the 4(th) position of the phenyl ring was the most preferable substituent for both cytotoxic and antimicrobial activity. Our preliminary findings suggest that compound 3 e could be exploited as a leading structure for further anticancer and antifungal drug development.Article Citation - WoS: 7Citation - Scopus: 6The Potential Role of Boron in the Modulation of Gut Microbiota Composition: an in Vivo Pilot Study(Mdpi, 2024) Senturk, Nermin Basak; Kasapoglu, Burcu; Sahin, Eray; Ozcan, Orhan; Ozansoy, Mehmet; Ozansoy, Muzaffer Beyza; Sahin, FikrettinBackground/Objectives: The role of the gut microbiome in the development and progression of many diseases has received increased attention in recent years. Boron, a trace mineral found in dietary sources, has attracted interest due to its unique electron depletion and coordination characteristics in chemistry, as well as its potential role in modulating the gut microbiota. This study investigates the effects of inorganic boron derivatives on the gut microbiota of mice. Methods: For three weeks, boric acid (BA), sodium pentaborate pentahydrate (NaB), and sodium perborate tetrahydrate (SPT) were dissolved (200 mg/kg each) in drinking water and administered to wild-type BALB/c mice. The composition of the gut microbiota was analyzed to determine the impact of these treatments. Results: The administration of BA significantly altered the composition of the gut microbiota, resulting in a rise in advantageous species such as Barnesiella and Alistipes. Additionally, there was a decrease in some taxa associated with inflammation and illness, such as Clostridium XIVb and Bilophila. Notable increases in genera like Treponema and Catellicoccus were observed, suggesting the potential of boron compounds to enrich microbial communities with unique metabolic functions. Conclusions: These findings indicate that boron compounds may have the potential to influence gut microbiota composition positively, offering potential prebiotic effects. Further research with additional analyses is necessary to fully understand the interaction between boron and microbiota and to explore the possibility of their use as prebiotic agents in clinical settings.Review Citation - WoS: 7Citation - Scopus: 8Recent Progress on Apoptotic Activity of Triazoles(Bentham Science Publ Ltd, 2021) Cikla-Suzgun, P.; Kucukguzel, S. G.Apoptosis is often called programmed cell death and is defined as a self-directed cell destruction process. It is different from necrosis due to the activation of caspases during this process. Apoptosis is directly related to cancer progression and plays a vital role in carcinogenesis; all cytotoxic drugs and radiation therapy programs initiate apoptosis in tumor cells. Today, studies show that heterocyclic compounds that contain triazole functionality have anticancer activities; triazoles are 5 membered rings, which contain two carbon and three nitrogen atoms. Therefore, many researchers have synthesized these small active compounds as target structures and evaluated their apoptotic activities. The present review describes recent medicinal aspects of triazoles as anticancer agents that have been reported during the past few years. We hope that the bioactivity of triazole derivatives will be beneficial for the rational design of a new generation of small molecule drugs.