A new synthetic approach for pyrazolo[1,5-a]pyrazine-4(5H)-one derivatives and their antiproliferative effects on lung adenocarcinoma cell line

Starting from the 3,5-dimethyl pyrazole ring and acetophenone derivatives, five different N-propargylated C-3 substitutedpyrazoles were obtained. These derivatives were reacted with different amine derivatives using Cs2CO3in methanol and11 different pyrazolo [1,5-a] pyrazine-4(5H)-one derivatives were obtained, which are not found in the literature. The cytotoxiceffects of these derivatives in the A549 cell line were investigated. The 160 µM concentration of two derivatives wasfound to increase cell death rate to 50%, and two derivatives increased cell death rate by up to 40%. The structure–activityrelationship (SAR) study revealed an amide group with a long alkyl chain and benzene ring with a p-CF3 group could beimportant for efficiency. With theoretical ADMET studies of pyrazolopyrazine derivatives, pharmacokinetic phases werepredicted to be suitable

THE KNOWLEDGE AND ATTITUDE OF UNIVERSITY STUDENTS ABOUT HEALTH HABITUDE AND CANCER

Amaç: Bu çalışmanın amacı Tıp Fakültesi dönem bir öğrencilerinin yaşam biçimi ve alışkanlıkların kanser hastalığı üzerine etkilerine yönelik bilgi ve tutumlarını saptamaktır. Gereç ve yöntem: Araştırma grubu Dokuz Eylül Üniversitesi Tıp Fakültesi birinci sınıfta eğitim gören öğrencilerden oluşmaktadır. Tanımlayıcı tipte bir çalışmadır. Veriler anketle toplanmıştır. Öğrencilerin sosyodemografik özellikleri, sigara, alkol, spor ve beslenme ile ilgili alışkanlıkları değerlendirilmiş; alışkanlıklar ve kanser arasındaki ilişki konusundaki bilgileri belirlenmiştir. Bulgular: Araştırmaya %52,7'si erkek, %47,3'ü kadın toplam 184 öğrenci katılmıştır. Araştırma grubunun %41,8'inin yakınında kanser hastalığı öyküsü bulunmaktadır. Öğrencilerin %15,2'si halen sigara içmektedir. Araştırma grubunun %48,4'ü haftada iki kez ya da daha seyrek olarak alkol kullanmaktadır. Araştırma grubunun %24,6'sı düzenli olarak spor yapmaktadır; tüm öğrenciler arasında sedanter olmayanların oranı yalnızca %11,8'dir. Yaşam biçimi ve bazı alışkanlıkların kansere etkisi olduğunu bilenlerin oranı %86,8'dir. Sonuç: Sigara kullanma oranı ülkemizde yapılmış çalışmalara benzer, alkol kullanma oranının ise yüksek olduğu bulunmuştur. Spor yapan öğrenciler azınlıkta olup çoğunluğun sedanter olduğu, sağlıklı beslenme alışkanlığı olanların oldukça düşük oranda olduğu saptanmıştır. Araştırma grubunun şişmanlığın kanser hastalığı oluşumunda etkisi konusundaki bilgi düzeyi düşüktür. Sağlık algısı yüksek ve orta olan öğrenciler daha fazla yağlı ve kalorili gıdalarla beslenmektedir. Öğrencilerin bireysel sağlıklı yaşam biçimini benimsemeleri önemlidir. SUMMARY Objecive: The aim of this study is to determine the knowledge and attitude of first year medical school students about lifestyle related factors and their association with cancers. Material and method: The study group was consisted of Dokuz Eylül University Faculty of Medicine first grade students. Data is collected with a questionnaire. The questionnaire included questions about demographic characteristics, knowledge and attitudes about cigarette, alcohol, sport and nutrition. Results: Total 184 students respond questionnaire which was 52.7% male and 47.3% female. Forty-two percent of students have at least one relative with a cancer. 15.2% were smokers. Fifty-two of study group were taking alcohol which was more than two times in a week. Twenty-four of study group were doing sport regularly and rate of non-sedentary life was only 11.8% among all students. The effects of lifestyle and some habituation risk factors on cancer diseases were known by 86.8%. Conclusions: Cigarette smoking rates were similarly but alcohol using were higher than our country results. A small part of our population was making sport while more have a sedentary lifestyle and poor healthy nutrition habituation. Knowledge level of obesity on cancer disease development was low. The students with medium and high score of health awareness, have more faty and high calori diet. Acceptance and application of healty lifestyle by students have great importance

Problematic meaning of art in different places

Text in Turkish; Abstract: Turkish and EnglishIncludes bibliographical references (leaves: 105-107)xii, 108 leavesTarih boyunca, sanat ve mekan arasındaki ilişki sürekli değişim gösterir. Nadire kabineleri, değerli nesnelerin biriktirilip gösterildiği mekansal düzenlemelerin ilk örnekleridir. Tarihsel aşamalar boyunca gelişen ve büyüyen kabineler, müzelere dönüşmeye başlar. Kabinelerdeki akıldışı ve hayal gücüyle oluşturulan düzen, müzelerde yerini akılcı, bilimsel ve tarihsel disiplinlere bırakır.Nesnelerin teşhir edildikleri mekanlarla olan bağları, tarihsel süreci kapsayan gelişmelere paralel olarak,değişim göstermiştir. Sosyo-ekonomik ve kültürel politikaların kuşattığı sistemin etkisi sonucu dönüşen sanat, daima özgürlük arayışı içinde olmuştur. Sanatçıysa, yeni anlatım biçimleri ve deneyimlerle, sistemin yönlendiriciliği ve tahakkümleri karşısında yer almaktadır.Art and venue has always had an evolving relationship in the course of history.Cabinet of curiosities,where valuable objects were stored and displayed, are the first examples of spatial arrangements. In time, Kunstkabinetts turned into museums as they thrived and grew in size. Curated by imagination, the extraordinary layouts of Kunstkabinetts transformed into rational, scientific and historical disciplines. Objects' ties to the place of exhibition underwent changes in parallel to the changes in historical processes. Surrounded by socio-economic and cultural policies, art is in constant search of liberty. Artists on the other hand, stand up to the dominance and inducement of the system through new ways of expression and experiences

Efficient synthesis of some oxalacetic acid and pyruvic acid derivatives from the reactions of 2,3-furandiones with 2-phenylindole

Oxalacetic acid and pyruvic acid derivatives have been synthesized efficiently in high yields by the treatment of 4-ethoxycarbonyl-5phenyl-2,3-furandione and 4-benzoyl-5-phenyl-2,3-furandione with 2-phenylindole at room temperature and converted to simple derivatives such as an ester or a hydrazone. (C) 2008 Elsevier Ltd. All rights reserved

Synthesis of Indolizines by Dimerization of N-Propargylated Pyrroles via Allene Intermediates

Ten different N-propargyl pyrrole derivatives having various substituents at the C-2 position were synthesized. These derivatives were converted into indolizine derivatives by the [2+2] cycloaddition reaction of pyrrole N-allene, forming in situ, by heating in PrOH in basic medium. The structures were characterized by NMR and X-ray crystallography. The N-propargylated derivatives smoothly underwent intermolecular cyclizations to produce indolizine derivatives in good yields. We proposed a radical mechanism for the dimerization. Reaction of an allene product with butylated hydroxytoluene (BHT), a radical scavenger, did not give any dimerization product. This result supports the radical reaction

Synthesis of pyrrole-fused C,N-Cyclic Azomethine Imines and Pyrazolopyrrolopyrazines: Analysis of their aromaticity using nucleus-independent chemical shifts values

Menges, Nurettin/0000-0002-5990-6275WOS: 000369771800017PubMed: 26752224The AgOTf-catalyzed reaction of C-2 substituted pyrrole hydrazones having an N-propargyl group was studied. The selective 6-endo-dig mode of cyclization was observed, giving rise to the formation of pyrrole-fused C,N-cyclic azomethine imine derivatives. The reaction of one azomethine imine derivative with various dipolarophiles resulted in the formation of cycloadducts having a pyrazolopyrrolopyrazine skeleton. The aromaticity of C,N-cyclic azomethine imines as well as that of pyrazolopyrrolopyrazines was determined by calculating of nucleus-independent chemical shifts values.Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [TBAG-112 T360]; Yuzuncu Yil UniversityYuzuncu Yil University [2014-ECZ-B170]; Turkish Academy of Sciences (TUBA)Turkish Academy of Sciences; Middle East Technical University (METU)Financial support from the Scientific and Technological Research Council of Turkey (TUBITAK, Grant No. TBAG-112 T360), Yuzuncu Yil University (Grant No. 2014-ECZ-B170), the Turkish Academy of Sciences (TUBA), and the Middle East Technical University (METU) is gratefully acknowledged

Single-step approach for synthesis of a novel tetracyclic skeleton: Investigation of X-ray analysis, fluorescence spectra, TD-DFT calculations and biological activities

MakaleWOS:000904967000006Tetracyclic molecules show important properties such as biological activities and fluorescence sensors. Hence, in this study, we have reported unknown tetracyclic skeleton. N -propargylated C-2 and C-4 disubstituted imidazole derivatives were reacted by 2-aminomethyl piperidine without using any transition metal. The reaction unveiled 16 different imidazo[1,2-a]pyrido[1 ' ,2 ' :3,4]imidazo[2,1-c]pyrazine skeletons. Cyclization reaction tolerated phenyl, naphthyl, bi-phenyl, 2-thienyl, and many substituents on the benzene ring such as OMe, CF 3 , and halogens. We have uncovered the exact structure of the tetracyclic skeleton using single-crystal X-ray analysis. Significant fluorescence emission of tetracyclic molecules was investigated, and derivatives bearing electron-withdrawing groups, CF 3 , and the 2-thienyl group possessed a bathochromic effect (shift to longer wavelength) which was confirmed by not only steady-state experiments but HOMOs and LUMOs calculations. The antimicrobial effects of the synthesized molecules on six different or ganisms were tested. Considerable activities of molecules 5p and 5n on many organisms were determined. Docking modeling and Lipinski, Ghose, and Veber compatibility studies of two different molecules were performed.Scientific and Technological Research Council of Türkiye (TUBITAK