Yazar "Gezegen, Hayreddin" seçeneğine göre listele
Listeleniyor 1 - 20 / 20
Sayfa Başına Sonuç
Sıralama seçenekleri
Öğe 2-Benzoil-1,3-diaril-2,3,3a,8a-tetrahidrosiklopenta[a]inden- 8(1H)-on Tu?revlerinin Sentezi, Tiyosemikarbazon ve Tiyazol Tu?revlerine Dönu?şu?mu?, Antikanser ve Antimikrobiyal Aktivitelerinin İncelenmesi(2019) Gezegen, Hayreddin; Tutar, Uğur; Hepokur, CeylanBu çalısmada öncelikle farklı su?bstitu?entlere sahip kalkon (1a-u) ve 2-benziliden indan-1-on tu?revi (2a-p) ilgili keton ve aldehitlerden aldol kondenzasyonu yolu ile sentezlendi. Elde edilen kalkon (1a-u) ve 2-benziliden indan-1-on (2a-p) tu?revleri DMSO içerisinde t-BuOK ile muamele edilerek tamamen yeni bisiklik 2-benzoil-1,3-diaril-2,3,3a,8a-tetrahidrosiklopenta[a]inden- 8(1H)-on tu?revleri (3a-z2) sentezlendi. Elde edilen bisiklik tu?revler (3a-z2) tiyosemikarbazit ile etanol içerisinde pTsOH varlıgında reflu?ks edilerek tiyosemikarbazon tu?revlerine (4a-z2) dönu?stu?ru?ldu?. Sonrasında ise sentezlenen tiyosemikarbazon (4a-z2) tu?revleri 2-brom asetofenon ile reaksiyona sokularak tiyazol (5a-z2) tu?revleri elde edildi. Elde edilen bilesiklerin spektroskopik yöntemler ile (1H-NMR, 13C-NMR, 2D-NMR, FT-IR ve Q-TOF LC/MS) yapı analizleri gerçeklestirildi. Son asamada ise sentezi gerçeklestirilen yeni bilesiklerin antimikrobiyal aktiviteleri on bes mikroorganizmaya karsı, antikanser aktiviteleri ise insan meme kanseri hu?cre hattı (MCF-7) ve insan meme kanseri adenokarsinoma (MDA-MB 231) hu?cre hattına karsı incelendi. Sitotoksik aktiviteleri ise insan saglıklı meme (MCF-10A) hu?cre hattına karsı incelendi. Sentezlenen bisiklik tu?revler (3a-z2) içerisinde en yu?ksek antimikrobiyal aktiviteyi 2-furan halkası içeren 3q bilesigi gösterirken tiyosemikarbazon tu?revleri (4a-z2) du?su?k du?zeyde antimikrobiyal aktivite göstermistir. Tiyazol tu?revlerinin (5a-z2) ise orta du?zeyde bir antimikrobiyal aktiviteye sahip oldugu göru?lmu?stu?r. Antikanser ve sitotoksik aktivite testlerinde sentezlenen bilesiklerin (3a-z2, 4a-z2 ve 5a-z2) iyi du?zeylerde antiproliferatif aktivite gösterdikleri gözlemlenmistir. Ancak sentezlenen bilesiklerin saglıklı hu?cre hattı (MCF-10A) ve kanser hu?cre hatlarındaki (MCF-7 ve MDA-MB-231) dozlarının birbirine yakın olması bir dezavantaj olarak degerlendirilmistir.Öğe A Potentiometric Sensor for the Determination of Pb(II) Ions in Different Environmental Samples(Wiley-V C H Verlag Gmbh, 2022) Ozbek, Oguz; Gezegen, Hayreddin; Cetin, Alper; Isildak, OmerIn this study, a novel PVC-based membrane containing (E)-2-(1-(4-(3-(4-chlorophenyl)ureido)phenyl)ethylidene)hydrazine carbothioamide (5) as an electroactive component (ionophore) along with potassium tetrakis (p-chlorophenyl) borate (KTpClPB) and bis(2-ethylhexyl)adipate (DEHA) in the ratio 4.0 : 32.0 : 1.0 : 63.0 (ionophore:PVC:KTpClPB:DEHA) (w/w) was used to develop a lead(II)-selective potentiometric sensor. The sensor exhibited a Nernstian response over a wide concentration range from 1.0x10(-5) to 1.0x10(-1) mol L-1 with a slope of 28.0 +/- 2.0 mV/decade, and a detection limit of 1.65x10(-6) mol L-1. It displayed very good selectivity towards Pb(II) ions over other cationic species. The lead(II)-selective sensor showed a fast response time of 5 s, good repeatability, and it worked in the broad pH range of 5.0-11.0. The sensor could be used as an indicator electrode in the quantification of Pb(II) by potentiometric titration against ethylenediaminetetraacetic acid (EDTA). In addition, this sensor was applied for the direct determination of Pb(II) in different water samples including spring water, purification water, commercial water, waste water and in a waste battery sample.Öğe A review of recent research on the antimicrobial activities of thiosemicarbazone-based compounds(2024) Korkmaz, Gürsel; Karaman, Isa; Gezegen, HayreddinThiosemicarbazones can be synthesized by condensation of thiosemicarbazides with ketones or aldehydes and play a role as precursors in the synthesis of many compounds such as thiazoles. They can exhibit many biological activities such as anti-inflammatory, antitumor, and antimicrobial properties. The discovery of antibiotics was an important milestone in the treatment of bacterial infections. However, antimicrobial resistance developed by microorganisms has created the need to discover new antimicrobial agents. Thiosemicarbazones and thiosemicarbazone-based compounds show significant antimicrobial potential. This review investigates the antimicrobial activity results of 244 Thiosemicarbazones and Thiosemicarbazone-based compounds over the last five years. We summarized some articles on thiosemicarbazones and their hybrids showing only antibacterial and antifungal activity in Web of Science (WOS) between 2019 and 2024.Öğe Alternate Method for the Synthesis of Six-Membered Carbocycles with Five Stereocenters: 1,2,3,4,6-Pentasubstituted-4-hydroxy-cyclohexanes(TAYLOR & FRANCIS INC, 2015) Gezegen, Hayreddin; Ceylan, MustafaA series of novel 1,2,3,4,6-pentasubstituted-4-hydroxy-cyclohexanes (3a-u) were synthesized from the reaction of aromatic ketones with aromatic aldehydes under mild reaction conditions in good yields. The stereochemistry of the synthesized compounds was established using 1D and 2D-NMR spectra.Öğe Crystal structure of racemic [(1R,2S,3R,4S,6S)-2,6-bis(furan-2-yl)-4-hydroxy-4-(thiophen-2-yl)cyclohexane-1,3-diyl]bis(thiophen-2-ylmethanone) (vol E72, pg 976, 2016)(INT UNION CRYSTALLOGRAPHY, 2016) Celik, Ismail; Ersanli, Cem Cuneyt; Akkurt, Mehmet; Gezegen, Hayreddin; Koseoglu, Rahmi…Öğe Design, synthesis, in vitro and computational analyses of anticancer nicotinamide derivatives(Natl Inst Science Communication & Policy Research-Niscpr, 2024) Gomec, Muhammed; Nasif, Vesim; Kafa, Ayse Huemeyra Taskin; Sayin, Koray; Gezegen, Hayreddin; Ataseven, HilmiThe search for ideal treatment continues for many health problems such as cancer and infection. In this context, new synthesis compounds have been promising and the nicotinamide derivative compounds, which is an important heterocyclic derivative, has attracted the attention of many researchers. Nowdays, anticancer, antifungal, antimicrobial, antibacterial and antibiofilm effects of some nicotinamide derivatives have been demonstrated. In this study, nine new nicotinamide derivative compounds have been designed and synthesized. The characterization of these synthesized compounds have been done by in silico methods. The anticancer effects of the compounds have been investigated in four different cancer types and compared with their effects on healthy fibroblast cells. N4 has been found to have a cytotoxic effect on MCF-7 human breast cancer, and the IC50 value has been calculated as 12.1 mu M. In addition, antibacterial, antifungal and antibiofilm activities were investigated by in vitro methods and they have been shown to be effective. As a result, it is observed that N4, one of the newly synthesized nicotinamide derivative compounds, has a serious cytotoxic effect in MCF-7 human breast cancer cells compared to healthy fibroblast cells. Pharmacophore map and ADME analyses of studied compound are performed in detail.Öğe Determining antifungal, anti-biofilm and anticancer activities of 1,3-di(thiophen-2-yl) prop-2- en-1-one chalcone derivative(2017) Tutar, Uğur; Çelik, Cem; Gezegen, Hayreddin; Hepokur, CeylanAmaç: Çalışmamızın amacı, literatürde rapor edilen beş kalkon bileşiğinin Candida albicans ve Candida tropicalis'e karşı potansiyel antifungal ve antibiyofilm aktivitelerinin belirlenmesidir. Ayrıca antimikrobiyal aktivitesi belirlenen \"1,3-di(thiophen-2-yl)prop-2-en-1-one\" kalkon bileşiğinin antioksidan ve insan meme kanseri (MCF-7) ve kemik kanseri (MG63) hücre hatları üzerindeki etkilerinin belirlenmesi amaçlanmıştır.Yöntem: Çalışmada kullanılan kalkonlar dimeti sülfoksit (DMSO) içinde iki kat seyreltilmiş ve 1000-15 ?g/mL konsantrasyonda hazırlanmıştır. Kalkonların antifungal ve anti-biyofilm aktiviteleri mikrodilüsyon yöntemi kullanılarak belirlenmiştir. Radikal süpürücü etkisi 2, 2-diphenyl-1-picrylhydrazyl (DPPH) ile test edilmiştir. Hücre canlılığı , kültür ortamına ilave edilen tetrazolium tuzları ile değerlendirilmiştir. Bulgular: Çalışmamızda antimikrobiyal aktivite gösteren \"1,3-di (tiyofen-2-il) prop-2-en-1-on\" C. albicans ve C. tropicalis üzerinde MIC değerleri 0.06 mg/mL bulunmuştur. MBC değerleri ise sırasıyla 0.12 mg/mL ve 0.5 mg/mL olarak saptanmıştır. MBIC aktiviteleri ise sırasıyla 0.06 ve 0.25 mg/mL olarak bulunmuştur. MBEC değerleri her iki mikroorganizma için 1 mg/mL bulunmuştur. C. albicans ve C. tropicalis' in 48 saatlik biyofilm yapılarına MIC değeri uygulandığında yapının sırasıyla 83% ve 81% oranında azaldığı saptanmıştır. \"1,3-di(thiophen-2-yl) prop-2-en-1-one\" IC50 değeri 13,52 µg/L olarak bulundu. MCF-7 ve MG63 hücre hatlarında 5 µg/mL konsantrasyonda 24 saat inkübasyon sonrasında sırasıyla hücrelerin % 30'u ve % 65' i canlı kalmıştır. Sonuç: Elde edilen sonuçlara göre tiyofen halkası içeren kalkon bileşiği C. albicans ve C. tropicalis suşları üzerinde hem üremelerini inhibe edici etki göstermiş hem de gerek biyofilm oluşumunda gerekse oluşan biofilm üzerinde etkili olduğu görülmüştür. Çalışmanın sonuçları tiyofen halkası içeren kalkon bileşiğinin potansiyel antimikrobiyal, antibiyofilm ve antikanser ajan olarak değerli olabileceğini ortaya koymuştur.Öğe Evaluation of acetylcholinesterase and carbonic anhydrase inhibition profiles of 1,2,3,4,6-pentasubstituted-4-hydroxy-cyclohexanes(WILEY, 2017) Kocyigit, Umit M.; Taslimi, Parham; Gezegen, Hayreddin; Gulcin, Ilhami; Ceylan, MustafaCarbonic anhydrase (CA; EC 4.2.1.1) is used for remedial purposes for several years, as there is significant focus on expanding more new activators (CAAs) and high affinity inhibitors. Alzheimers disease and other similar ailments such as dementia and vascular dementia with Lewy bodies reduce cholinergic activity in the important areas involved in cognition and memory. Prevalent drugs for the symptomatic therapy of dementia are significant in increasing the associated cholinergic deficiency by inhibiting acetylcholinesterase (AChE). These six-membered carbocycles showed nice inhibitory action against AChE and human carbonic anhydrase (hCA) II and I isoforms. The hCA I, II, and AChE were efficiently inhibited by these molecules, with K-i values in the range of 6.70-35.85nM for hCA I, 18.77-60.84nM for hCA II, and 0.74-4.60 for AChE, respectively.Öğe Evaluation of antimicrobial, antibiofilm and carbonic anhydrase inhibition profiles of 1,3-bis-chalcone derivatives(WILEY, 2019) Tutar, Ugur; Kocyigit, Umit M.; Gezegen, HayreddinA series of 1,3-bis-chalcone derivatives (3a-i, 6a-i and 8) were synthesized and evaluated antimicrobial, antibiofilm and carbonic anhydrase inhibition activities. In this evaluation, 6f was found to be the most active compound showing the same effect as the positive control against Bacillus subtilis and Streptococcus pyogenes in terms of antimicrobial activity. Biofilm structures formed by microorganisms were damaged by compounds at the minimum inhibitory concentration value between 0.5% and 97%.1,3-bis-chalcones ( 3a-i, 6a-i and 8) showed good inhibitory action against human (h) carbonic anhydrase (CA) isoforms I and II. hCA I and II were effectively inhibited by these compounds, with K-i values in the range of 94.33 +/- 13.26 to 787.38 +/- 82.64nM for hCA I, and of 100.37 +/- 11.41 to 801.76 +/- 91.11nM for hCA II, respectively. In contrast, acetazolamide clinically used as CA inhibitor showed K-i value of 1054.38 +/- 207.33nM against hCA I, and 983.78 +/- 251.08nM against hCA II, respectively.Öğe Fenilüre Birimi İçeren 2-Benzoilindan-1-on ve İndenopirazol Türevlerinin Sentezi ve Antikanser Aktivitelerinin İncelenmesi(2016) Gezegen, Hayreddin; Ceylan, MustafaHetero halkalı bileşikler arasında yer alan pirazol türevlerinin biyoaktif bileşikler olduğu bilinmektedir. Pirazol sınıfının bir üyesi olan indenopirazol türevleri de biyoaktif potansiyeli yüksek bileşiklerdir. Bu çalışmada fenilüre birimi içeren yeni 1,3-diketon bileşiklerinin sentezi ve bu bileşikler üzerinden de yeni indenopirazol türevlerinin sentezi amaçlanmıştır. Elde edilen bu yeni bileşiklerin antikanser aktivitelerinin incelenmesi de hedefler arasındadır. Çalışmada öncelikle, 4?-aminoasetofenonun farklı sübstitüentlere sahip fenilizosiyanatlar ile reaksiyonundan fenilüre birimi içeren asetofenon türevleri (1a-j) elde edildi. Elde edilen asetofenon türevlerinin (1a-j) ftaldialdehit ile reaksiyonundan ise 2-benzoilindan-1-on türevleri (2a-j) sentezlendi. Sonrasında ise 2-benzoilindan-1-on türevlerinin (2a-j) hidrazin veya fenil hidrazin ile muamele edilmesinden fenilüre birimi içeren indenopirazol türevlerinin sentezi (3a- j ve 4a-j) yüksek verimlerle gerçekleştirildi. Elde edilen bileşiklerin karakterizasyonu spektroskopik yöntemler (1H-NMR, 13C-NMR, 2D-NMR, IR ve HPLC-TOF/MS) ile yapıldı. Son aşamada sentezlenen bileşiklerin antikanser aktiviteleri incelendi. Bileşiklerin HeLa (insan servikal kanser hücre hattı) ve C6 (sıçan beyin tümörü) hücre hatlarına karşı % 50 inhibisyon konsantrasyonları (IC50) ve gösterdikleri antiproliferatif etkiler yapılan deneyler ile belirlendi. Yapılan testler sonucunda sentezlenen bileşikler içerisinde hidrazinden elde edilen indenopirazol türevlerinin (3a-j) daha yüksek antikanser aktivitelere sahip oldukları görüldü. Daha sonra antiproliferatif etkileri yüksek bileşiklerin hücre döngüsünde ve apoptosiste rol oynayan temel genlerin ekspresyonu üzerine etkisi belirlendi. Bu bileşikler içerisinden 3b ve 3d bileşiklerinin yüksek derecede apoptotik özelliğe sahip oldukları belirlenmiştir.Öğe Potassium carbonate mediated one-pot synthesis and antimicrobial activities of 2-alkoxy-4-(aryl)-5H-indeno[1,2b] pyridine-3-carbonitriles(ACG PUBLICATIONS, 2016) Ozturk, Sahin; Gurdere, Meliha Burcu; Gezegen, Hayreddin; Ceylan, Mustafa; Budak, Yakup2-Alkoxy-4-(aryl)-5H-indeno[ 1,2-b] pyridine-3-carbonitriles (3a-e and 4a-e) were synthesized via multicomponent reaction from 2-aryl-methylidineindan-1-ones (1a-e), malononitrile and K2CO3 in ethanol and/or methanol. The structures of obtained compounds (3a-e and 4a-e) were characterized using the spectroscopic methods (NMR, IR) and elemental analysis. Addition, the in vitro antimicrobial activities of compounds (3a-e) were tested against the five human pathogenic bacteria. Penicillin G and Ceftriaxone antibiotics were used as positive control. The results were given as MIC values (minimum inhibition concentration), and compounds 3b-d showed very high activity against Escherichia coli 111.Öğe Synthesis and Antimicrobial Activity of Racemic 1,5-Diols: 2-(1,3-Diaryl-3-hydroxypropyl)cyclohexan-1-ol Derivatives(WILEY-V C H VERLAG GMBH, 2016) Gezegen, Hayreddin; Tutar, Ugur; Ceylan, MustafaA series of novel racemic 2-(1,3-diaryl-3-hydroxypropyl)cyclohexan-1-ol derivatives were synthesized from 1,5-diketones. All the synthesized compounds were characterized by spectroscopic methods. The antibacterial activities of obtained chiral 1,5-diols were investigated against four Gram-positive and three Gram-negative bacteria by determining of minimum inhibitory concentrations (MICs) in vitro. Compounds 3b, 3c, and 3d were found to be active against Enterococcus faecalis and Escherichia coli. In addition, compound 3j were found to be moderately active against all tested bacterial strains.Öğe Synthesis and Biological Evaluation of Novel 1-(4-(Hydroxy(1-oxo-1,3-dihydro-2H-inden-2-ylidene)methyl)phenyl)-3-phenylurea Derivatives(WILEY-V C H VERLAG GMBH, 2017) Gezegen, Hayreddin; Hepokur, Ceylan; Tutar, Ugur; Ceylan, MustafaA series of novel phenylurea containing 2-benzoylindan-1-one derivatives 3a - 3j were synthesized from the reaction of phenylurea-substituted acetophenones 1a - 1j with phthalaldehyde 2 under mild reaction conditions in good yields. All synthesized compounds were characterized by spectroscopic methods. The obtained compounds (3a - 3j) were evaluated for anticancer activity against HeLa and C6 cell lines. Antiproliferative activity was determined by the BrdU proliferation ELISA assay, 3f and 3g were found to be most active compounds. The compounds were also screened for antimicrobial activity and all compounds showed remarkable activity against used microorganisms.Öğe Synthesis and biological evaluation of novel indenopyrazole derivatives(WILEY, 2019) Gezegen, Hayreddin; Tutar, Ugur; Hepokur, Ceylan; Ceylan, MustafaA series of novel indenopyrazole derivatives 2a-j and 3a-j were synthesized from the reaction of 1-(4-(hydroxy(1-oxo-1,3-dihydro-2H-inden-2-ylidene)methyl)phenyl)-3-phenylurea derivatives 1a-j with hydrazine and phenylhydrazine, respectively. The obtained novel indenopyrazoles (2a-j and 3a-j) were evaluated for anticancer activity against HeLa and C6 cell lines. Antiproliferative activity was determined by the BrdU proliferation ELISA assay; 2a, 2b, 2d, 2h, and 3h were found to be the most active compounds. The compounds were also screened for antimicrobial activity, and all compounds showed moderate activity against used microorganisms.Öğe Synthesis and Caracterizations of New Thiosemicarbazone and Thiazole Derivatives From Polycyclic Chiral 1,5-Diketones(Wiley-V C H Verlag Gmbh, 2023) Gezegen, HayreddinThiosemicarbazone derivatives have a wide spectrum of biological activity as well as various application areas such as forming complexes with metals, using as intermediates in the synthesis of heterocyclic bioactive compounds. Thiazole derivatives can be easily synthesized from thiosemicarbazones and are among the important compounds in demand in terms of biological activity. In this study, 14 new thiosemicarbazone derivatives were synthesized starting from polycyclic 1,5-diketone derivatives with five stereocenters, and 14 thiazole derivatives were synthesized from the reaction of the obtained thiosemicarbazones with 2-bromoacetophenone and their structure determinations were carried out using spectroscopic methods (1H-NMR, 13C-NMR, 2D-NMR, FT-IR and Q-TOF LC/MS). This synthesis route from polycyclic chiral 1,5-diketones may contribute to the design of new drug-like molecules, which are important in medicinal chemistry. Herein, 14 new thiosemicarbazone derivatives were synthesized starting from polycyclic 1,5-diketone derivatives with five stereocenters, and 14 thiazole derivatives were synthesized from the reaction of the obtained thiosemicarbazones with 2-bromoacetophenone and their structure determinations were carried out using spectroscopic methods.imageÖğe Synthesis and Characterization of Novel 2,4-Diaryloctahydro-2H-Chromene Derivatives with Four Stereocenters(2023) Gezegen, HayreddinChromene derivatives are among the natural compounds and they can also be easily obtained synthetically. They are one of the most commonly used skeletons in heterocyclic chemistry. Chromene derivatives are used in the cosmetic and pigment industries as well as having a wide spectrum of biological activity. Synthesis of chromene derivatives and their application areas is a current topic. In this study, it is aimed to synthesis and characterization of new chromene derivatives by catalysis of molecular iodine starting from 1,5-diol derivatives with chiral centers. In this context, 8 new 2,4-diaryloctahydro-2H-chromene derivatives were synthesized in high yields and their structure determinations were made by spectroscopic methods (1H-NMR, 13C-NMR, 2D-NMR, GCMS and FTIR) and their stereochemistry was determined.Öğe Synthesis of Bis-Nicotinonitrile Derivatives and Investigations of Antimicrobial and Antibiofilm Activities(Wiley-V C H Verlag Gmbh, 2023) Tutar, Ugur; Gezegen, HayreddinIn this study aimed to the synthesis of novel bis-nicotinonitrile derivatives starting from 1,3-bis-chalcones and investigate their antimicrobial activity potentials. Bis-nicotinonitrile derivatives were synthesized from 1,3-bis-chalcone derivatives reacted with malononitrile in ethanol in the presence of potassium carbonate. Characterization of the obtained compounds was carried out by spectroscopic methods. In total, 12 new 1,3-phenylene-bis-nicotinonitrile derivatives were synthesized. Finally, the antimicrobial and antibiofilm activities of synthesized 1,3-phenylene-bis-nicotinonitrile derivatives were tested against 5 microorganisms. As a result, it was observed that the synthesized new nicotinonitrile derivatives were quite active especially in terms of antibiofilm activity. In this study, the synthesis of new 1,3-phenylene-bis-nicotinonitrile derivatives starting from 1,3-bischalcones and their antimicrobial and antibiofilm activities are reported. In this context, 12 new 1,3-phenylene-bis-nicotinonitrile derivatives were synthesized and their structure analyzes were carried out using spectroscopic methods. As a result of antimicrobial and antibiofilm studies performed against 5 microorganisms, it was observed that the synthesized compounds had remarkable effects especially in terms of antibiofilm activity.imageÖğe Synthesis of Nanoparticles Loading Indenopyrazole Derivatives and Evaluation of Biological Features(Marmara Univ, Inst Health Sciences, 2022) Dogan, Murat; Kocyigit, Umit Muhammet; Gezegen, HayreddinObjective: In this study, it was aimed to prepare nanoparticle formulations using chitosan, a cationic natural polymer, and tripoly phosphate, and to perform mechanical characterization and in vitro cell culture studies. In addition, the cytotoxic effects of nanoparticles containing indenopyrazol derivatives against human glioma cells (C6) and human cervical cancer cells (HeLa) were investigated. Methods: Within the scope of the study, nanoparticles containing indenopyrazole derivative were prepared and characterization of particle size, zeta potential and morphological properties were performed. XTT cytotoxicity test was applied to evaluate the antiproliferative activities of nanoparticles containing these components. Results: Particle size, zeta potential and morphological properties of nanoparticles were observed to be suitable for application. In vitro cell culture studies showed that nanoparticles containing indenopyrazol derivatives showed better cytotoxic effects in both cell lines. Conclusion: The results showed that the mechanical properties of nanoparticles containing indenopyrazol derivatives are suitable and can be applied in anticancer activity studies.Öğe Synthesis, characterization, and biological studies of chalcone derivatives containing Schiff bases: Synthetic derivatives for the treatment of epilepsy and Alzheimer's disease(Wiley-V C H Verlag Gmbh, 2020) Kocyigit, Umit M.; Gezegen, Hayreddin; Taslimi, ParhamIn this study, first, Schiff base-containing chalcone derivatives were synthesized. The human carbonic anhydrase (hCA) isoenzymes I and II were then purified from human erythrocytes using Sepharose-4B-l-tyrosine-sulfanilamide affinity chromatography. In addition, the inhibitory effects of the newly synthesized compounds on the activities of hCA and acetylcholinesterase (AChE) were investigated in vitro, using the esterase and acetylcholine iodide method. The IC(50)values were determined and theK(i)values of AChE and hCA activities were calculated from the Lineweaver-Burk graphs determined in this study. The hCA I isoform was inhibited by these chalcone derivatives containing Schiff bases (3a-jand5a-f) in low nanomolar levels, whoseK(i)values ranged between 141.88 +/- 24.10 and 2,234.47 +/- 38.11 nM. Against the physiologically dominant isoform hCA II, the compounds demonstratedK(i)values varying from 199.31 +/- 40.45 to 602.79 +/- 263.22 nM. Also, these compounds effectively inhibited AChE, withK(i)values ranging from 20.41 +/- 6.04 to 125.94 +/- 23.88 nM. According to these results, the newly synthesized molecules were found to be potent inhibitors of these enzymes.Öğe Synthesis, spectral characterization, DFT calculations and investigation of anticancer properties of carbothioamide and metal (FeII and CrIII) complexes(Natl Inst Science Communication & Policy Research-Niscpr, 2025) Gueney, Elif; Sayin, Koray; Gezegen, HayreddinSchiff base and its metal complexes have a broad application in areas such as medicine, pharmacy, cosmetics, agriculture, plastic industry, dyestuff production, etc. Recently, the anticancer activities of these compounds have been investigated, and it is a matter of curiosity how the effectiveness changes with complexation. 2-(1-(2-Hydroxyphenyl) ethylidene) hydrazine-1carbotioamide (HL) and its metal (Fe-II and Cr-III) complexes have been synthesized and investigated computationally and experimentally. In the calculations, B3LYP-D3/6-31+G(d) for HL and B3LYP-D3/6-31+G(d)(LANL2DZ) for metal complexes have been used. Anticancer properties of these complexes have been investigated against three different cell lines which are breast cancer (MCF-7), colorectal cancer (HT-29) and gastric cancer (SNU-16). XTT test has been used in the cell viability assays. It is found that the studied compounds are active against breast cancer and Fe(II) complex has shown the best activity. Structural properties of compound have been examined computationally and experimentally. Electronic properties of the studied compounds (for HL) have been investigated by Hirshfeld surface analyses and MEP maps. Anticancer properties of studied compounds have been investigated by cell viability assays. It is found that synthesized compounds are only active against breast cell line, MCF-7. The best compound is found as [FeL2] due to the fact that its IC50 has been calculated as 1.62 mu M.
