Küçükgüzel, Şükriye Güniz
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Kucckguzel, S. Guniz
Kucukguzel, S. Gueniz
Kucukguzel, S. Guniz
Küçükgüzel, Ş.G.
Küçükgüzel, Ş.güniz
Küçükgüzel, Sükriye Güniz
Kucukguzel, S. Gueniz
Kucukguzel, S. Guniz
Küçükgüzel, Ş.G.
Küçükgüzel, Ş.güniz
Küçükgüzel, Sükriye Güniz
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guniz.kucukguzel@fbu.edu.tr
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Eczacılık Meslek Bilimleri Bölümü
Eczacılık Meslek Bilimleri Bölümü
Eczacılık Meslek Bilimleri Bölümü
Eczacılık Meslek Bilimleri Bölümü
Eczacılık Meslek Bilimleri Bölümü
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Sustainable Development Goals
3
GOOD HEALTH AND WELL-BEING
16
Research Products
5
GENDER EQUALITY
1
Research Products
7
AFFORDABLE AND CLEAN ENERGY
1
Research Products
16
PEACE, JUSTICE AND STRONG INSTITUTIONS
1
Research Products
17
PARTNERSHIPS FOR THE GOALS
1
Research Products
Scholarly Output
23
Articles
23
Citation Count
105
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0
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Scholarly Output Search Results
Now showing 1 - 10 of 23
Article Citation - WoS: 10Citation - Scopus: 10Synthesis and Biological Evaluation of Novel Aryloxyacetic Acid Hydrazide Derivatives as Anticancer Agents(Taylor & Francis inc, 2021) Senkardes, Sevil; Erdogan, Omer; Cevik, Ozge; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri BölümüIn our continuing search for new anticancer agents, herein we report the synthesis of 2-(4-chloro-3-methylphenoxy)-N'-[(aryl)methylidene]acetohydrazides 3a-j and the evaluation of their anticancer activities on cell viability, morphological changes and caspase-3 activity in cancer cell lines including gastric cancer (MKN45), cervical cancer (HeLa) and breast cancer (MDA-MB-231) cells. 2-(4-chloro-3-methylphenoxy)-N'-[(4-phenylthiophen-2-yl)methylidene] acetohydrazide 3g presented the strongest growth inhibition against MKN45 gastric cancer cell lines with the IC50 value of 1.471 +/- 0.23 mu M. Moreover, compounds 3b and 3g showed high potency against the HeLa and MDA-MB-231 cell lines having IC50 in the range of 2.38-9.72 mu M. These compounds are more selective for the tested human cancer cells than for the mouse fibroblast cell line (NIH/3T3). As a result of the studies conducted in order to understand the molecular mechanism, compounds 3b and 3g enhanced expression of the caspase-3 pro-apoptotic proteins levels besides caspase-3 gene.Article Citation - WoS: 1Citation - Scopus: 1Synthesis, Molecular Docking Studies and Adme Prediction of Some New Albendazole Derivatives as Α-Glucosidase Inhibitors(Slovensko Kemijsko Drustvo, 2022) Senkardes, Sevil; Kulabas, Necla; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri BölümüA series of novel 2-(substituted arylidene)-N-(5-(propylthio)-2,3-dihydro-1H-benzo[d]imidazol-2-yl)hydrazine-1-carboxamide derivatives 3a-i were synthesized via condensation of N-(5-(propylthio)-1H-benzo[d]imidazol-2-yl) hydrazinecarboxamide (2), with the corresponding ketone or aldehydes. The chemical structures of the compounds prepared were confirmed by analytical and spectral data. The compounds were screened for their a-glucosidase inhibitory activity and all of them showed better inhibition than acarbose, except 3h. In particular, compound 3a proved to be the most active compound among all synthetic derivatives having IC50 value 12.88 +/- 0.98 mu M. Also, molecular docking studies were carried out for the compounds to figure out the binding interactions. Compound 3a has exhibited the highest binding energy (Delta G = -9.4 kcal/mol) and the most hydrogen bond interactions with active sites. Eventually, in silico studies were in good agreement with in vitro studies.Article Investigation of the Printability of Ethyl 2-[4 on Coated and Uncoated Papers](Wiley, 2025) Akgul, Ahmet; Kucukguzel, S. Guniz; Oktav, Mehmet; Rollas, Sevim; Eczacılık Meslek Bilimleri BölümüThere is a growing demand in the printing industry for pigment-based inks with excellent lightfastness and rub resistance qualities. In this work, a novel ink with the formulation ethyl 2-[4-(1,3,4-oxadiazole-2(3H)-thione-5-yl)phenylhydrazono]-3-oxobutyrate (OXKT) was prepared as a pigment and its printability was investigated for use in printing. The OXKT was synthesised, characterised then printed on uncoated and gloss-coated papers and Bristol cardboard. Physical tests and spectrophotometric measurements were carried out to determine the technical characteristics of the printed ink. Additionally, print quality, ink density and gloss were evaluated. The results showed that the proposed ink with the OXKT compound had acceptable rub resistance. Also, the gloss and light fastness values exceeded the acceptable rates for the printing industry because of their colour differences. However, more research needs to be conducted to improve light performance. Nevertheless, it is still possible for use in applications that do not stipulate strict light fastness values.Review Citation - WoS: 11Citation - Scopus: 9Thioethers: an Overview(Bentham Science Publ Ltd, 2022) Han, M. Ihsan; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri BölümüSpreading rapidly in recent years, cancer has become one of the causes of the highest mortality rates after cardiovascular diseases. The reason for cancer development is still not clearly understood despite enormous research activities in this area. Scientists are now working on the biology of cancer, especially on the root cause of cancer development. The aim is to treat the cancer disease and thus cure the patients. The continuing efforts for the development of novel molecules as potential anti-cancer agents are essential for this purpose. The main aim of this review was to present a survey on the medicinal chemistry of thioethers and provide practical data on their cytotoxicities against various cancer cell lines. The research articles published between 2001-2020 were consulted to prepare this review article; however, patent literature has not been included. The thioether-containing heterocyclic compounds may emerge as a new class of potent and effective anti-cancer agents in the future.Article Citation - WoS: 18Citation - Scopus: 20Design, Synthesis and Anticancer Activity Studies of Novel 4-Butylaminophenyl Hydrazide-Hydrazones as Apoptotic Inducers(Pergamon-elsevier Science Ltd, 2022) Han, M. Ihsan; Baysal, Ozge Deniz Yesil; Basaran, Guzide Satir; Sezer, Gulay; Telci, Dilek; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri BölümüIn this study, a series of the novel Tetracaine derivatives bearing hydrazide-hydrazone moiety were designed, synthesized, and evaluated for anticancer activity. The structures of these compounds were characterized by spectral (H-1-C-13 NMR, FT-IR, and HR-MS analyses) methods. All synthesized compounds (2a-1) were screened for anticancer activity against human hepatocellular carcinoma (HepG2) and lung carcinoma (A549) cell lines. Against HepG2 and A549 cell lines, among the synthesized compounds, 4-(Butylamino)-N'-[(2,4-dichlorophenyl)methylidene]benzohydrazide (2i) demonstrated the most potent anticancer activity with IC50 values 28 and 7 mu M, respectively. Possible cytotoxic effects of compounds (2a-1) on both normal human lung fibroblast (MCR-5) and normal human dermal fibroblast (HDF) cell lines were assessed. Inhibition of anti-apoptotic protein Bax and Bcl-2 was investigated in HepG2 and A549 cells treated with compound 2i using qRT-PCR. Apoptosis was also detected by Annexin V studies. The flow cytometric analysis results showed that compound 2i treatment of HepG2 and A549 cells significantly increased apoptotic cell populations while decreasing viabilities in these carcinomas in a dose-dependent manner after 72 h of incubation. (C) 2022 Elsevier Ltd. All rights reserved.Article Investigation of Novel Nimesulide Derivatives Against Breast Cancer(Academic Press Inc Elsevier Science, 2025) Birgul, Kaan; Atlihan, Irem; Dere, Damla; Yelekci, Kemal; Tiber, Pinar Mega; Orun, Oya; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri BölümüThis study focused on the synthesis of novel nimesulide semicarbazone derivatives and the evaluation of their cytotoxic potential against luminal-A (MCF-7) and triple-negative (MDA-MB-231) breast cancer cell lines. Additionally, their effects on mitochondrial membrane potential (MMP), apoptosis, and mitogen-activated protein kinase (MAPK) pathway modulation were investigated. Breast cancer remains the most prevalent malignancy among women, with luminal-A and triple-negative subtypes posing significant therapeutic challenges due to drug resistance and the lack of effective targeted treatments. The MAPK pathway plays a crucial role in breast cancer progression, making its inhibition a promising therapeutic approach. Non-steroidal anti-inflammatory drugs (NSAIDs), particularly nimesulide, have demonstrated anticancer potential beyond their well-established anti-inflammatory properties. Accordingly, the semicarbazone moiety was incorporated into the molecular scaffold to enhance the antiproliferative efficacy of nimesulide derivatives, as it has been reported to exhibit cytotoxic and apoptosis-inducing effects across various cancer cell lines. A series of nimesulide semicarbazone derivatives (5a-m) were synthesized through multi-step reactions and characterized using elemental analysis, FT-IR, 1H NMR, 13C NMR and Mass spectroscopy (5e). In silico studies were performed to predict their binding affinities to MAPK12. The cytotoxic effects of the synthesized compounds were assessed by determining IC50 values in MCF-7 and MDA-MB-231 cell lines (CCK8 test). Compounds exhibiting strong cytotoxic activity were further examined for their impact on MMP depolarization (JC-1 assay), apoptosis induction (Annexin V-FITC/PI staining), and MAPK pathway modulation (Western blotting of p-ERK and ERK protein). Molecular docking results indicated that the synthesized compounds exhibited favorable interactions with MAPK12, with compound 5e showing one of the highest binding affinity (-9.29 kcal/mol, Ki = 0.154 mu M). Cytotoxicity assays revealed that compound 5e had the lowest IC50 values (11.77 +/- 0.26 mu M in MCF-7; 20.72 +/- 0.25 mu M in MDA-MB-231), demonstrating significantly higher cytotoxicity than nimesulide. JC-1 assays confirmed that compound 5e induced MMP depolarization at higher concentrations, suggesting apoptosis activation. Flow cytometry analysis further validated a substantial increase in apoptotic cell populations following treatment with compound 5e. Western blot results showed a dose-dependent decrease in p-ERK levels in both MCF-7 and MDA-MB-231 cells, confirming MAPK pathway inhibition. These findings support that nimesulide-based semicarbazones, particularly compound 5e, exhibit potent antiproliferative and pro-apoptotic activity via MAPK pathway modulation, offering a promising avenue for the development of targeted breast cancer therapies.Article Citation - WoS: 1Citation - Scopus: 2Synthesis of New 4-Aminobenzoic Acid (paba) Hydrazide-hydrazone/Sulfonate Hybrids and Antimicrobial Evaluation With Ascorbic Acid/Salicylic Acid/n< Cysteine Combinations(Taylor & Francis Ltd, 2024) Han, M. Ihsan; Ince, Ufuk; Coskun, G. Pelin; Birgul, Kaan; Dogan, Sengul Dilem; Ashoorzadeh, Amir; Kucukguzel, S. Gueniz; Eczacılık Meslek Bilimleri BölümüOne of the most serious threats to human health is the increasing prevalence of drug-resistant pathogens. The development of new antibiotics capable of combating drug resistance is critical. In various bacteria and plant species, 4-aminobenzoic acid (PABA) is produced and used as a substrate for folate generation. In this study, a new series of PABA analogs were synthesized and evaluated for their antimicrobial activity. Thirteen novel compounds were prepared by linking PABA hydrazide to sulfonate esters via a hydrazone bridge (4a-m). The structures of these compounds were characterized by H-1 and C-13 NMR and FT-IR spectroscopy as well as by LC-MS. Following structural characterization, all compounds were tested for their antimicrobial activity against Staphylococcus aureus (ATCC 29213), Enterococcus faecium (ATCC 19434), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), and Candida albicans (ATCC 10231) strains. Four compounds were found to have moderate antimicrobial activity against the P. aeruginosa strain. These compounds, including 4e, 4f, 4g, and 4m, containing a hydrazide-hydrazone sulfonate functionality, showed the best MIC value of 64 mu g/mL. In addition, synergistic effects of ascorbic acid, salicylic acid, and N-acetyl cysteine (NAC) with synthesized compounds were also investigated. It was observed that the combination of compounds 4f and 4g with NAC showed antipseudomonal activity with MIC values of 32 mu g/mL and 16 mu g/mL, respectively, against the P. aeuriginosa strain. The antimicrobial activity of 4f and 4g was enhanced by two folds in combination with NAC. Our findings in this study can be crucial for the development of new potent antimicrobial agents. [GRAPHICS]Article Bir Tiyoeter-triazol Hibriti: Güçlü Metap2 Inhibitörü ve Prostat Kanseri için In Vivo Tümör Baskılayıcı Bileşiğin In Silico Çalışmaları ve In Vitro Mikrozomal Metabolizması(2023) Coşkun, Göknil Pelin; Ulgen, Mert; Birgül, Kaan; Evren, Asaf Evrim; Küçükgüzel, Ş.güniz; Eczacılık Meslek Bilimleri BölümüArka plan/amaç: Antikanser bir ilaç adayı bileşik olan ( S)-3-((2,4,6-trimetilfenil)tiyo)-4-(4-florofenil)-5-(1-(6-metoksinaftalen-2-)il) etil)-4H-1,2,4-triazol (SGK636), bileşiğinin in vitro mikrozomal metabolizması çalışılmış ve potansiyel S-oksidasyon ve S-dealkilasyon metabolitlerini belirlemek için NADPH ile güçlendirilmiş domuz mikrozomal preparatları kullanılarak incelenmiştir. Gereç ve Yöntemler: Bu çalışmada, sülfoksit metaboliti kromatografik ve spektroskopik yöntemlerle sentezlenmiş, saflaştırılmış ve karakterize edilmiştir. SGK636, S-oksidasyon ve S-dealkilasyon metabolitleri daha sonra ters fazlı bir LC-MS, UV spektroskopisi ve bir HP-TLC sistemi ile ayrılmıştır. In vitro mikrozomal metabolik deneylerin sonuçları, SGK636’nın, aynı Rt ve Rfx100 değerleri ve UV/ ile LC-MS, LC-MS/MS ve HP-TLC tarafından gözlemlenen karşılık gelen S-oksidasyon metabolitini (sülfoksit) ürettiğini göstermiştir. Otantik bileşiklerle karşılaştırıldığında MS spektrumlarında, herhangi bir S-dealkilasyon metaboliti tespit edilmemiştir. Bulgular: Mevcut sonuçlar moleküler doking ve moleküler dinamik çalışmalarla kanıtlanmıştır. Sülfoksidasyon işlemi tersine çevrilebilir olduğundan ve deneyimizdeki düşük miktarda sülfoksit metabolitini kısmen açıklayabildiğinden, sülfoksit bileşiği de inkübe edilmiştir. Substrata (SGK636) geri dönüşüm gözlenmemiş olup, karşılık gelen sülfon metabolitinin oluştuğu gözlenmiştir. SGK636’nın otooksidize olup olmadığını belirlemek için substrat ayrıca standart inkübasyon koşulları altında tampon içinde inkübe edilmiştir, ancak karşılık gelen sülfoksitte herhangi bir oto-oksidasyon gözlenmemiştir. Sülfona herhangi bir olası otooksidasyonu veya tekrar SGK636’ya indirgemeyi görmek için tampondaki SGK636-SO (sülfoksit) için bir stabilite çalışması da yapılmıştır. Her iki şekilde de dönüşüm gözlemlenmemiştir. Substrat, farmakolojik aktivitesi açısından bir avantaj olabilecek metabolik reaksiyonlara ve otooksidasyona karşı kararlı görünmektedir. Sonuç: Mevcut metabolik çalışma, SGK 636’nın S-oksidasyonuna uğradığını göstermektedir. Sorumlu oksidatif enzimi belirlemek için moleküler yerleştirme ve moleküler dinamik çalışmalar yapılmıştır. CYP3A4’ün S-oksidasyonundan sorumlu enzim olduğu bulunmuştur.Article Citation - WoS: 13Citation - Scopus: 11Synthesis of Some Novel Hydrazide-Hydrazones Derived From Etodolac as Potential Anti-Prostate Cancer Agents(Marmara Univ, 2022) Koc, Hande Cevher; Atlihan, Irem; Mega-Tiber, Pinar; Orun, Oya; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri Bölümü(R,S)-Etodolac [1,8-diethyl-1,3,4,9-tetrahydrapyrano(3,4-b)indole-1-acetic acid] is a nonsteroidal anti-inflammatory drug that contains carboxylic acid group with the structure of pyrano[3,4-h]indole. In this study, a series of novel (R,S)-Etodolac derivatives (3a-1) bearing hydrazide-hydrazone moiety were synthesized. The structures of these compounds were characterized by spectral (H-1-NMR and FT-IR analyses) methods. All synthesized compounds were screened for anticancer activity against androgen-independent prostate adenocarcinoma (PC-3, DU-145) and androgen-dependent prostate adenocarcinoma (LNCaP) cell lines by using WST-8 colorimetric method. This method was used for cell viability and cytotoxicity analysis. Compound 3b (SGK-720) [2-(1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-yl)acetic acid[(2,6-dichlorophenyl)methylene]hydrazides] showed 10.36, 5.24, 15.53 mu M anticancer activity against PC3, DU145, LNCaP cancer cell lines, respectively. According to JC-1 mitochondrial membrane potential test and Annexin V/PI staining, 3b was found to have apoptotic effect on these cancer cells. It is concluded that compound 3b containing 2,6-dichloro substituents may be one of the candidate molecules to cope with prostate cancer.Article Citation - WoS: 7Effect of Flurbiprofen Derivative (sgk597) on Cell Proliferation and Apoptosis of Breast Cancer Cell Lines(Istanbul Univ, Fac Pharmacy, 2022) Atlihan, Irem; Sevinc, Sevgi Kocyigit; Orun, Oya; Yilmaz, Ozgur; Kucukguzel, S. Guniz; Tiber, Pinar Mega; Eczacılık Meslek Bilimleri BölümüBackground and Aims: The incidence of breast cancer is increasing day by day, especially in women. The search for new drugs against breast cancer is the focus of attention in research. Breast cancer and prostate cancer have remarkable biological similarities. Therefore, the 4-(4-chlorophenyl)-3-(1-(2-fluoro-[1,1'-biphenyl]-4-yl)ethyl)-5-((4-fluorobenzyl)thio)-4H-1,2,4-triazole (SGK597) compound that is suppressing cell proliferation in prostate cancer, was studied in MCF-7 breast can-cer and MCF-10A mammary epithelial cell lines. Methods: The WST-8 method was used to determine cell viability and cytotoxicity of SGK597 in MCF-7 and MCF10-A cell lines. The JC-1 test was applied to determine changes in mitochondrial membrane potential. The protein expression levels of Bax, Bcl-2, and c-PARP associated with apoptosis were determined using Western blot analysis.Results: After 24 and 48 hours of incubation of SGK597, the IC50 values were 28.74 pM and 17.28 pM for MCF-7; 65.9 pM and 50.5 pM for MCF-10A, respectively. Mitochondrial membrane potential showed a tendency toward depolarization in MCF-7 cells as a result of increasing concentration of SGK597, while the same tendency was not seen for MCF-10A. As a result of western blot experiments, no increase in the Bax/Bcl-2 ratio and c-PARP expression level was observed, indicating no apoptosis.Conclusion: It was observed that the compound SGK597 suppressed MCF-7 cell proliferation. These results indicate that SGK597 may be a candidate compound for use as an anticancer agent. Keywords: Apoptosis, breast cancer, flurbiprofen, thioether, triazole
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