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Evaluation of Hydrazide-Hydrazone and 4-Thiazolidinone Derivatives of Etodolac as Potential Anticancer Agents in Leukemia Cells
(Bentham Science Publ Ltd, 2024) Küçükgüzel, Şükriye Güniz; Averbek, Sera; Sevinc, Sevgi Kocyigit; Kilinc, Olca; Suzgun, Pelin Cikla; Kucukguzel, S. Guniz; Orun, Oya; Eczacılık Meslek Bilimleri Bölümü
Background 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.
Citation Count: 0
Synthesis and Biological Evaluation of New 4-Thiazolidinone Derivatives of Flurbiprofen
(Acg Publications, 2023) Küçükgüzel, Şükriye Güniz; Senkardes, Sevil; Gurboga, Merve; Ozakpinar, Ozlem Bingol; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri Bölümü
In this study, the synthesis and characterization of 2-(2-fluorobiphenyl-4-yl)-N '-[(substituted methylene]propanehydrazides (3a-s) and 2-(2-fluoro-[1,1'-biphenyl]-4-yl)-N-(5-methyl-2-(substituted aryl)-4oxothiazolidin-3-yl)propanamides (4a-s) are described and also the antiproliferative effect of the compounds on HT 29, HeLa, A549 and MCF-7 cancer cell lines is investigated. Additionally, mouse embryonic fibroblast cells NIH3T3 were also evaluated to determine the selectivity. The results showed that the identified compounds did not cause any toxicity against NIH3T3 cell line. Moreover, N-(2-(3,5-Bis(trifluoromethyl)phenyl)-5-methyl-4-oxothiazolidin-3-yl)-2-(2-fluoro-[1,1'-biphenyl]-4-yl)propanamide (4h) had the most growth inhibitory effect (55.97% inhibition) on HT-29 colorectal adenocarcinoma cell line. The results obtained from the study show that the compound 4h, which has no cytotoxic effect on normal cells, may be an alternative in the treatment of colon cancer.
Citation Count: 2
Synthesis, Antimicrobial Properties and in Silico Studies of Aryloxyacetic Acid Derivatives With Hydrazone or Thiazolidine-4 Scaffold
(Taylor & Francis inc, 2023) Küçükgüzel, Şükriye Güniz; Kart, Didem; Bebek, Bilge; Gunduz, Miyase Gozde; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri Bölümü
In 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. Sarma

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