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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3
GOOD HEALTH AND WELL-BEING
0
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5
GENDER EQUALITY
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7
AFFORDABLE AND CLEAN ENERGY
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16
PEACE, JUSTICE AND STRONG INSTITUTIONS
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17
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23
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23
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105
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Now showing 1 - 10 of 23
Article Citation - WoS: 5Citation - Scopus: 3Synthesis 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; Eczacılık Meslek Bilimleri BölümüBy 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 Biological Activities of Etodolac-Based Hydrazone, Thiazolidinone and Triazole Derivatives on Breast Cancer Cell Lines MCF-7 and MDA-MB(Wiley, 2025) Sevinc, Sevgi Kocyigit; Cikla-Suzgun, Pelin; Tiber, Pinar Mega; Kucukguzel, S. Guniz; Orun, Oya; Eczacılık Meslek Bilimleri BölümüIn this study, several etodolac-based hydrazone, thiazolidinone, and triazole derivatives that we synthesized and characterized in our earlier research were tested against the hormone-responsive breast cell line MCF-7 and the triple-negative MDA-MB-231, as well as the murine origin fibroblast cell line L-929, at varying doses for their effects on cell viability and toxicity and for their inhibitory activity on cyclooxygenase-2 (COX-2)/prostaglandin E2 (PGE2) formation. Cell viability and apoptosis tests were utilized to assess the anti-cancer potential of etodolac and its derivatives after the cells were exposed to varied concentrations of synthesized compounds for three different time periods. ELISA and Western blot methods were used to detect protein levels. All synthesized compounds demonstrated higher anti-cancer activity at significantly lower doses compared to etodolac (half-maximal inhibitory concentration [IC50] of 0-50 mu M range in derivatives versus 0.5-1 mM range in etodolac). Except for SGK 242, which had a major toxic effect on all cells, the chemicals SGK 206 and SGK 217 had a twice-less impact on control murine L-929 fibroblasts. Similar to proliferation, low concentrations of SGK 206 and SGK 217 (25-50 mu M) significantly induced apoptosis in breast cancer cells but not in normal cells. Additionally, they inhibited COX-2 protein expression at 50 mu M, and SGK 206 inhibited PGE2 release more effectively than etodolac in cancer cells. The results of this study suggest that, in comparison to a healthy control group, the thiazolidinone derivative SGK 206 and the thiazolidinone derivative SGK 217 are more effective than etodolac when it comes to the breast cancer cell lines MCF-7 and MDA-MB-231. SGK 206 exhibits a low IC50 value, a distinct dose-response relationship, and strong apoptotic effects, particularly on MDA-MB-231 cells.Article Citation - WoS: 1Citation - Scopus: 1Evaluation of Hydrazide-Hydrazone and 4-Thiazolidinone Derivatives of Etodolac as Potential Anticancer Agents in Leukemia Cells(Bentham Science Publ Ltd, 2024) Tiber, Pinar Mega; Averbek, Sera; Sevinc, Sevgi Kocyigit; Kilinc, Olca; Suzgun, Pelin Cikla; Kucukguzel, S. Guniz; Orun, Oya; Eczacılık Meslek Bilimleri BölümüBackground Nonsteroidal anti-inflammatory drugs (NSAIDs), which are commonly used for their anti-inflammatory and analgesic properties, have also been found to prevent cancer. (+/-)(R,S) Etodolac is an NSAID that belongs to the class of cyclooxygenase-2 inhibitors. Various derivatives of etodolac are synthesized to boost its anti-proliferative action and lessen its potential negative effects. In our earlier studies, some novel derivatives of etodolac exhibited stronger cytotoxic effects on prostate cell lines and had similar effects on leukemia cells in pre-screening experiments.Objective Using the K562 leukemia cell line as a model, we sought to investigate the anti-cancer properties of a hydrazide-hydrazone derivative (SGK-205) and a 4-thiazolidinone derivative of etodolac (SGK-216).Materials and Methods In the current investigation, SGK-205 and SGK-216 compounds were administered to K562 cells for 24 and 48 hours at concentrations of 10, 25, 50, 75 and 100 mu M. Cell viability was assessed using the MTT test, and apoptosis by Annexin V-PI staining and mitochondrial membrane potential assays, together with mRNA expressions of apoptotic proteins. The levels of the proteins, HER2 and COX2, were also examined to evaluate COX2 inhibitory capacity.Results In K562 cells, there was a definite dose-dependent response to SGK-205 and SGK-216 compounds. Results from MTT viability tests, together with mitochondrial membrane potential measurements and Annexin V-PI staining, revealed that SGK-216 and SGK-205 significantly outperformed etodolac in terms of their apoptotic and anti-proliferative activities. The concentration range of 10-20 mu M for both chemicals was sufficient to start biological responses. Apoptosis was also investigated through the expressions of pro- and anti-apoptotic proteins. Additionally, gene expression research demonstrated SGK-205 to be a beneficial substitute to etodolac in lowering COX-2 and human epidermal growth factor receptor-2 (HER2) expression.Conclusion Our data indicated both derivatives to have higher anti-proliferative and apoptotic effects compared to etodolac. An overall assessment highlighting apoptotic induction potential, acceptable toxicity levels, a consistent dose-response relationship, and COX2 inhibitory actions, in particular, indicated SGK-205 as a viable novel therapeutic.Article Citation - WoS: 37Citation - Scopus: 35Synthesis and Anticancer Activity of Novel Hydrazone Linkage-Based Aryl Sulfonate Derivatives as Apoptosis Inducers(Springer Birkhauser, 2022) Senkardes, Sevil; Han, M. Ihsan; Gurboga, Merve; Ozakpinar, Ozlem Bingol; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri BölümüIn the present study, the various 28 hybrid molecules containing hydrazone and sulfonate moieties were synthesized and characterized by FTIR, H-1-NMR, C-13-NMR spectroscopy and LC-MS spectrometry, besides elemental analysis. The compounds were evaluated for their antiproliferative effects against six cancer cell lines, namely A549 (non-small cell lung cancer), MCF-7 (breast cancer), HT-29 (colorectal adenocarcinoma cancer), PC-3 (androgen-independent prostate adenocarcinoma), Hep3B (hepatocellular carcinoma cancer), and HeLa (epitheloid cervix carcinoma cancer). Among all the target compounds, compounds 4g and 4h exhibited more promising effects on MCF-7 cell lines (IC50 = 17.8 mu M and 21.2 mu M, respectively) with high selectivity. Further mechanistic studies proposed that compounds 4g and 4h induced apoptosis is mediated through the intrinsic apoptotic pathway with changes in mitochondrial membrane potential by finally activating caspase-9 and caspase-3. The results have been encouraging enough to merit further investigation. [GRAPHICS] .Article Citation - WoS: 1Citation - Scopus: 1Molecular Modelling Studies To Suggest Novel Scaffolds Against Sars-Cov Target Enzymes(Marmara University, 2021) Şahin, A.F.; Küçükgüzel, Ş.G.; Akdemir, A.; Eczacılık Meslek Bilimleri BölümüIn this study, molecular modelling study of previously synthesized compounds against SARS-CoV-2 target enzyme was performed. A subset of 156 compounds from an in-house database has been subjected to molecular modelling studies against the SARS-CoV-2 ADP-ribose phosphatase (ADRP, NSP3), Papain-like protease (PLpro ), and uridine specific endoribonuclease (NSP15) enzymes. We have identified one compound that is expected to inhibit the SARS-CoV-2 ADRP enzyme and one compound that is expected to inhibit the NSP15 enzyme. © 2021 Marmara University Press ISSN: 2630-6344.Article Citation - WoS: 5Citation - Scopus: 5Synthesis, Antimicrobial Properties and in Silico Studies of Aryloxyacetic Acid Derivatives With Hydrazone or Thiazolidine-4 Scaffold(Taylor & Francis inc, 2023) Senkardes, Sevil; Kart, Didem; Bebek, Bilge; Gunduz, Miyase Gozde; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri BölümüIn this work, twenty hydrazide-hydrazone and 4-thiazolidinone derivatives were synthesized starting from m-cresol. Antimicrobial evaluation was carried out by microdilution method against Enterococcus faecalis and Staphylococcus aureus as Gram-positive bacteria and Escherichia coli and Pseudomonas aeruginosa as Gram-negative bacteria, and three pathogenic fungi Candida albicans, Candida parapsilosis and Candida krusei. Some compounds possessed considerable antimicrobial properties against the tested microorganisms, particularly against E. coli. 4-Thiazolidinones containing 3-methoxyphenyl and 3,5-dichlorophenyl moieties (4h and 4i) were found to be the most active derivatives with MICs of 2 mu g/mL against E. coli. N'-[(3,5-dichlorophenyl)methylidene]-2-(3-methylphenoxy)acetohydrazide (3i) also displayed antifungal activity against Candida krusei that was comparable to fluconazole. Calculated drug-likeness and ADMET parameters of the most active compounds confirmed their potential as antimicrobial drug candidates. Molecular docking investigations were carried out in the thiamine diphosphate-binding site of pyruvate dehydrogenase multienzyme complex E1 component (PDHc-E1) to clarify the potential antibacterial mechanism against E. coli. The results showed the potential and importance of developing new hydrazones and 4-thiazolidinones that would be effective against microbial strains. Communicated by Ramaswamy H. SarmaArticle Citation - WoS: 13Citation - Scopus: 15Design, Synthesis, and in Vitro and in Vivo Anticancer Activity Studies of New (s)-naproxen Thiosemicarbazide/1,2,4-triazole Derivatives(Royal Soc Chemistry, 2022) Han, M. Ihsan; Tunc, Cansu Umran; Atalay, Pinar; Erdogan, Omer; Unal, Gokhan; Bozkurt, Mehmet; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri BölümüIn this study, a series of novel (S)-Naproxen derivatives bearing a thiosemicarbazide/1,2,4-triazole 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 of the synthesized compounds (3a-m, 4a-j) were screened for anticancer activity against human breast cancer cell line MDA-MB-231. Among them, (S)-4-(2,4-dichlorophenyl)-5-[1-(6-methoxynaphthalen-2-yl)ethyl]-4H-1,2,4-triazole-3-thione (4b) showed the most potent anticancer activity with a good selectivity (IC50= 9.89 +/- 2.4 mu M). Inhibition of anti-apoptotic protein Bcl-2 was investigated in MDA-MB-231 cells treated with compound 4b using Western Blotting. Apoptosis was also detected by AO/EB and JC-1 staining. Furthermore, activation of caspase-3 enzyme activity demonstrated apoptosis. The flow cytometric analysis results showed that compound 4b decreases the number of cells in the G2/M phase and increases the cells in the S phase in a dose-dependent manner. The anticancer activity of compound 4b was also investigated. In the Ehrlich acid tumor model, a well-validated in vivo ectopic breast cancer model, compound 4b had anticancer activity and reduced the tumor volume at both low (60 mg kg(-1)) and high (120 mg kg(-1)) doses in mice, according to our in vivo results.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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