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Ruthenium (II) komplekslerinin DNA bağlanması He ilgili olan yüksek antitumor aktiviteleri nedeni He bu bileşikler son yıllarda araştırmacıların yoğun ilgisini çekmektedir. Bu çalismada imidazo[4,5-f][ 1,10]fenantrolin (ip) and 2-fenilimidazo[4,5-f][ 1,10]fenantrolin (pip) ligand olarak kullanılarak, iki rutenyum (II) kompleksi sentezlenmiş olup, bu bileşikler spektroskobik ve elemental analiz yöntemleri He karakterize edilmiştir. İlk olarak, bu komplekslerin insan akciğer karsinoma, A549 hücreleri üzerine olan ölümcül etkileri araştırHmıştır. MTT deneyi He elde edilen sitotoksik sonuçlar göstermiştir ki, A 549 hücrelerinin 24 saat imidazo[4,5-f][1,10]fenantrolin Ru(II) kompleksi [Ru(ip)3](PF6)2 ve 2-fenilimidazo[4,5-f][ 1,10]fenantrolin Ru(II) kompleksi [Ru(pip)3](PF6)2 ile inkübasyonu sonucunda IC50 değerlerinin sırasıyla yaklasik olarak 32 ve 46 jug/ml'dır.ilginçtir ki, bu komplekler normal insan akciğer hücrelerine karsi dusuk sitotoksik etkiye sahiptirler (IC50 > 80 ug/ml).BrdU bağlanma deneyi sonucunda, [Ru(pip)3](PF6)2 kompleksinin diğer hücrelere kıyasla A549 hücreleri üzerinde güçlü baskılayıcı etkiye sahip olduğu gdrülmustiir. [Ru(pip)3](PF6)2 kompleksinin dana timus DNA 'sı He etkileşimi sonrasında DNA baglanma aktivitesinin arttigi viskozite deneyi He tespit edilmiştir.Özet olarak, [Ru(pip)3](PF6)2 kompleksi anlamh sitoksik etki ve A549 hiicre çoğalması üzerine inhibitor bir etki göstermiştir. Bu kompleksin güçlü tedavi edici bir etkiye sahip olabileceği ve bu nedenle tedavi edici ajanların geliştirilmesi için farklı in vitro biyoassaylar kullanarak araştırılması gerekliliği varsayılmaktadır., In recent years, ruthenium (II) complexes have increasingly attracted the interest of researchers because of their high antitumor activities that are usually related to DNA binding. Here, we synthesized two ruthenium (II) complexes, using imidazo[4,5-f][1,10]phenanthroline (ip) and 2-phenylimidazo[4,5-f][1,10]phenanthroline (pip) that were characterized by spectroscopic and elemental analyses. First of all, we investigated the ability of these complexes to produce lethal effects in human lung carcinoma, A 549 cells. The cytotoxicity results evaluated by the MTT assay, revealed that the IC50for Ru(II) complexes of imidazo[4,5-f][1,10]phenanthroline [Ru(ip)3](PF6)2 and 2-phenylimidazo[4,5-f][1,10]phenanthroline [Ru(pip)3](PF6)2 after 24 h of incubation with A549 cells was approximately 32 and 46 jilg/ml, respectively. Interestingly, it was observed that these complexes showed weak cytotoxic effects in normal human lung cells (IC50 > 80 ug/ml). [Ru(pip)3](PF6)2 has a potent inhibitory effects on A549 compared to other cells as measured by BrdU labeling assay. Treatment of DNA with [Ru(pip)3](PF6)2induced DNA binding activity, which was demonstrated by a viscosity assay. In summary, Ru(II) complexes of [Ru(pip)3](PF6)2 showed significant cytotoxic and anti-proliferative effects on A549 cells, suggesting that this complex may have potential therapeutic agent, and therefore, this must be further investigated by other in vitro bioassays for the development of therapeutic agents.

8th International Conference on Thrombosis and Hemostasis Issues in Cancer -- APR 08-10, 2016 -- Bergamo, ITALY, WOS: 000373731900081, PubMed ID: 27161724, …

In recent years, ruthenium (II) complexes have increasingly attracted the interest of researchers because of their high antitumor activities that are usually related to DNA binding. Here, we synthesized two ruthenium (II) complexes, using imidazo[4,5-f][1,10]phenanthroline (ip) and 2-phenylimidazo[4,5-f][1,10]phenanthroline (pip) that were characterized by spectroscopic and elemental analyses. First of all, we investigated the ability of these complexes to produce lethal effects in human lung carcinoma, A549 cells. The cytotoxicity results evaluated by the MTT assay, revealed that the IC50for Ru(II) complexes ofimidazo[4,5-f][1,10]phenanthroline [Ru(ip)3](PF6)2 and 2-phenylimidazo[4,5-f][1,10]phenanthroline [Ru(pip) 3](PF6) 2 after 24 h of incubation with A549 cells was approximately 32 and 46 Mg/ml, especttvely. Interestingly,i was observed that these complexes showed weak cytotoxic effects in normal human lung cells (IC50 > 80 ug/ml). [Ru(pip)3](PF6)2 has a potent inhibitory effects on A549 compared to other cells as measured by BrdU labeling assay Treatment of DNA with [Ru(pip)3]PF6)2inducedDNA binding activity, which was demonstrated by a viscosity assay. In summary, Ru(II) complexes of [Ru(pip)3](PF6)2 showed significant cytotoxic and antiproliferative effects on A549 cells, suggesting that this complex may have potential therapeutic agent, and therefore this must be further investigated by other in vitro bioassaysfor the development of therapeutic agents.

WOS: 000285267300053, The increasing clinical importance of drug-resistant mycobacterial pathogens has lent additional urgency to microbiological research and I new antimycobacterial compound development. For this purpose, in this study, Zn(II), Cd(II) and Hg(II) complexes of a heptadentate, N(5)S(2) donor Schiff base ligands including 2,6-bis(2-aminothiophenoxymethyl) pyridine and 2,2'-bipyridine-6,6'-dicarboxaldehyde were I obtained by using the literature methods and evaluated for antituberculosis activity. Antituberculosis activities of the compounds were I determined by broth microdilution assay, the microplate alamar blue assay, in BACTEC12B medium and results were screened in vitro, I using BACTEC 460 radiometric system against Mycobacterium tuberculosis H(37)R(v) (ATCC 27294) at 6.25 mu g/mL and tested compounds I showed important inhibition ranging from 84 to 58 %. Antimicrobial activities of these complexes have also been searched. All complexes I showed the same activity against Pseudomonas aeruginosa and moderate activities against Proteus vulgaris, but they didn't give significant antibacterial activity against other bacterial strains. On the other hand they showed moderate activities when compared with antifungal agent Ketoconazole against Candida albicans and Candida globrata., Anadolu University, The authors are grateful to Anadolu University, Commission of Scientific Research Projects for support of this study and to the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) in USA for the in vitro evaluation of antimycobacterial activity.

36th FEBS Congress of the Biochemistry for Tomorrows Medicine -- JUN 25-30, 2011 -- Torino, ITALY, WOS: 000292333102310, …, Federat Soc Biochem & Mol Biol

36th FEBS Congress of the Biochemistry for Tomorrows Medicine -- JUN 25-30, 2011 -- Torino, ITALY, WOS: 000292333102299, …, Federat Soc Biochem & Mol Biol

WOS: 000188542400010, The compounds 1-substituted 2-(imidazol-1-yl)-3-(4,5-diarylimidazol-2-yl) indoles 2, I-substituted 2-(imidazol-1-yl)3-(phenanthro[9,10-d]imidazol-2-yl)indoles 3 and 1-substituted 2-(imidazol-1-yl)-3-(benzimidazol-2-yl)indoles 4 have been synthesized from 1-substituted 2-(imidazol-1-yl)-3-formylindole 1. The structural elucidation of the synthesised compounds has been performed by IR, H-1 NMR and mass spectroscopic data and elemental analyses. Antimicrobial activities of the compounds are examined and notable antifungal activity is obtained from some of the compounds as expected in comparison with the control agent ketoconazole.

Terpineol is a monoterpene alcohol used as a fragrance material in perfumery industry and for the production of some volatile compounds. Several techniques have been described in the literature for its synthesis. These techniques recommend the conversion of olefinic terpenes to their hydrochlorides or esters with acids, followed by hydrolysis into the desired alcohol. This paper describes a method which involves hydration of ?-pinene to terpinhydrate which is then dehydrated to give ?-terpineol. Cation exchange resin was also used in an oxygen-free medium to obtain ?-terpineol in higher (73%) yield.

Bu çalışmada, 6-kloro- ve 6,7-dikloro-2,3-disübstitüe-kinoksalin türevleri sentezlenerek, sitotoksisiteleri ve antitümör etkileri araştırıldı. 6-Kloro- ve 6,7-dikloro-2,3-disübstitüe-kinoksalin bileşikleri, uygun 1,2-dikarbonil bileşiği ve sübstitüe o-fenilendiamin ile, derişik asetik asit içerisinde, 4-5 saat geri çeviren soğutucu altında kaynatılarak elde edildi. Sentezlenen bileşiklerin yapıları IR, 1H-NMR ve Mass spektroskopik verileri ve elementel analiz sonuçları ile aydınlatıldı. Bileşiklerin antitümör aktiviteleri ve sitotoksisiteleri araştırıldı., In this study, 6-chloro- and 6,7-dichloro-2,3-disubstituted-quinoxaline derivatives were synthesized and their cytotoxicity and antitumor activities were tested. 6-Chloro- and 6,7-dichloro-2,3-disubstituted-quinoxaline compounds were obtained by reacting 1,2-dicarbonyl compound and substituted o-phenylenediamine under reflux for 4-5 hours in glacial acetic acid. The structure elucidation of the compounds was performed by IR, 1H-NMR and Mass spectroscopic data and elemental analysis results. Antitumor activities and cytotoxicities of the compounds were examined.

In this study, some thiosemicarbazide derivatives were synthesized by reaction of hydrazides with the appropriate arylisothiocyanate and the platinum complexes of these compounds were prepared. The structure elucidation of the compounds were performed by IR, ¹H-NMR spectral data and elemental analyses results. Antimicrobial activities of the ligands and complexes were examined without the reactions being interrrupted by using a bioauto graphic agar overlay method. Toxicities and antimycotic activities of some of these compounds were also investigated., Bu çalışmada, uygun arilisotiyosiyanatlar ve hidrazidlerin reaksiyonu ile bazı tiyosemikarbazid türevleri sen-tezlenerek platin kompleksleri hazırlandı. Bileşiklerin yapıları IR, 1,H NMR spektral verileri ve elemental analiz sonuçları ile aydınlatıldı. Ligandlarm ve komplekslerin antimikrobiyal aktiviteleri, reaksiyonlar kesilmeden "bioautographic ağar overlay" metodu ile test edildi. Aynı zamanda bileşiklerin toksisiteleri ve antimitotik aktiviteleri araştırıldı.

Tez (doktora) - Anadolu Üniversitesi, Anadolu Üniversitesi, Sağlık Bilimleri Enstitüsü, Farmasötik Kimya Anabilim Dalı, Kayıt no: 115481, Bu çalışmada, otuzdört yeni 3-arilamino-5-ariloksimetil [1,2,4] triazol türevi bileşik, S-Metilarilizotiyoüronyum iyodür türevlerinin piridin içerisinde uygun fenoksiasetilhidrazidleriyle ısıtılması sonucunda sentezlenmiştir. Elde edilen bileşiklerin yapıları, UV, IR, H-NMR ve MASS spektroskopik verileri ve elementel analiz sonuçları yardımıyla aydınlatılmıştır. Bileşiklerin antibakteriyel ve antifungal etkileri tüp dilüsyon tekniği ile incelenmiş, sonuçlar MİK (ug/ml) olarak elde edilmiştir. Bileşiklerimizin gösterdikleri etkilerin sübstitüentlere göre sınıflandırılabilir olmadıkları görülmüştür.