Synthesis, antimicrobial and antioxidant activities of pyridyl substituted thiazolyl triazole derivatives

In this present study, 63 different 5-[4-methyl-2-(pyridin-3/4-yl)thiazole-5-yl]-4-substituted-3-substituted benzylthio-4H-1,2,4-triazole derivatives were synthesized, and evaluated for their in vitro antimicrobial activity against various human pathogenic microorganisms and antioxidant activity. The derivatives were synthesized in a multi-step synthesis procedure including triazole and thiazole ring closure reactions, respectively. The synthesized derivatives (A1-24; B1-39) were screened for their antibacterial, antifungal, and antioxidant activities compared to standard agents. The derivatives possessing 3-pyridyl moiety particularly exhibited relatively high antibacterial activity (MIC= < 3.09-500 µg/mL) against Gram-positive bacteria, and compounds possessing 4-pyridyl moiety showed remarkable antioxidant activity.Eskisehir Osmangazi Universit

Microwave supported synthesis of some novel 1,3-Diarylpyrazino[1,2-a] benzimidazole derivatives and investigation of their anticancer activities

WOS: 000286905400048PubMed ID: 21122952The syntheses of 1,3-diarylpyrazino[1,2-a]benzimidazole derivatives and the investigation of their anticancer activities were studied. For this, 2-aryloylbenzimidazole derivatives were reacted with 2-bromoacetophenones in acetone to give 1-(2-aryl-2-oxoethyl)-2-aryloylbenzimidazoles. The resulting materials were reacted with ammonium acetate in acetic acid to obtain the aimed compound. In this reaction, microwave irradiation method was applied as the reaction conditions. Anticancer activities of the compounds obtained were investigated. It was observed that some of the compounds showed remarkable anticancer activities

Synthesis of some 2,3,6,8-tetraarylimidazo[1,2-a]pyrazine derivatives by using either reflux or microwave irradiation method, and investigation their anticancer activities

WOS: 000286528300002In this study, some 2,3,6,8-tetraarylimidazo[1,2-a]pyrazine derivatives were synthesized by reacting 1-(2-aryl-2-oxoethyl)-2-aryloyl-4,5-diarylimidazoles from 2-aryloyl-4,5-diarylimidazole and 2-bromoacetophenone derivatives with ammonium acetate in acetic acid by using the method that was previously developed and repeatedly tested in our studies. Structural elucidation of the compounds was performed by IR, (1)H-NMR, and MASS spectroscopic data and elemental analysis results. Anticancer activities of selected compounds were evaluated and the noticeable activity values were reported

Microwave supported synthesis of some novel 1,3-Diarylpyrazino[1,2-a]benzimidazole derivatives and investigation of their anticancer activities

a b s t r a c t The syntheses of 1,3-diarylpyrazino[1,2-a]benzimidazole derivatives and the investigation of their anticancer activities were studied. For this, 2-aryloylbenzimidazole derivatives were reacted with 2-bromoacetophenones in acetone to give 1-(2-aryl-2-oxoethyl)-2-aryloylbenzimidazoles. The resulting materials were reacted with ammonium acetate in acetic acid to obtain the aimed compound. In this reaction, microwave irradiation method was applied as the reaction conditions. Anticancer activities of the compounds obtained were investigated. It was observed that some of the compounds showed remarkable anticancer activities

Synthesis and characterizations of novel thiazolyl-thiadiazole derivatives as telomerase activators

WOS: 000433980300014Pyridine-3/4-thiocarboxamide derivatives were used as starting materials for the synthesis of the target compounds. The pyridine-3/4-thiocarboxamide derivatives were reacted with ethyl 2-chloroacetoacetate in ethanol to give the thiazole derivatives (1, 2). The two ethyl thiazole-carboxylate derivatives (1, 2) thus obtained were treated with sodium hydroxide solution and ethanol and converted to carboxylic acids (3, 4). The carboxylic acid derivatives (3, 4) were reacted with thiosemicarbazide in phosphoroxy trichloride and aminothiadiazole rings (5, 6) were formed. Thus, two thiazolyl-thiadiazole amine derivatives (5, 6) were obtained. These two derivatives (5, 6) were converted into two chloroacetamidothiadiazole derivatives (7, 8) by reaction with chloroacetylchloride over the amino group in the presence of triethylamine in acetone. After all these steps, the starting materials (7, 8) needed to reach the target compounds were obtained. With the two derivatives (7, 8) obtained in this last step, phenol and thiophenol derivatives were reacted in acetone in the presence of potassium carbonate. The target compounds, thiazolyl-thiadiazole derivatives (TDA (1-16)) , are completely unique and their structure has been elucidated by elemental analysis, IR, NMR, and MS spectral data. After all these synthesis steps, telomerase activity studies were performed on the target compounds obtained. For this purpose, a PCR ELISA-based TRAP method was used on the heart of zebrafish. According to the enzyme assay results, derivative TDA (8) has shown an increase of telomerase enzyme activity.Scientific and Technological Research Council of Turkey (TUBITAK) [212T181]The synthesis and characterization of this study were supported by the Scientific and Technological Research Council of Turkey (TUBITAK, Grant Number 212T181)

New chroman-4-one/thiochroman-4-one derivatives as potential anticancer agents

WOS: 000414346300017PubMed ID: 29158716The synthesis of 3-[3/4-(2-aryl-2-oxoethoxy) arylidene] chroman/thiochroman-4-one derivatives (1-34) and evaluation of their anticancer activities were aimed in this work. Final compounds were obtained in multistep synthesis reactions using phenol/thiophenol derivatives as starting materials. For anticancer activity evaluation, all compounds were offered to National Cancer Institute (NCI), USA and selected ones were tested against sixty human tumor cell lines derived from nine neoplastic diseases. The activity results were evaluated according to the drug screening protocol of the institute. Compounds containing thiochromanone skeleton exhibited higher anticancer activity.Anadolu University, Turkey (BAP) [050301]This work was supported by Anadolu University, Turkey (BAP Project No: 050301). The authors present their thanks to NCI (USA) and Anadolu University BIBAM (Turkey) for anticancer test results and NMR spectra, respectively

Synthesis and antifungal activity evaluation of New 1,2,4-triazole derivatives bearing salicylidene hydrazide moiety

WOS: 000364521600009A series of new N'-(arylidene)-2-[(1-(4-nitrophenyl)-1H-1,2,4-triazol-3-yl)oxy]acetohydrazide derivatives (116) were prepared and tested for theira ntifungal activity against six plant pathogens, three human pathogens and two non-pathogen microorganisms. The target compounds were obtained with a multi-step reaction starting from 4-substitutedarylhydrazine derivatives and the structures of final compounds have been elucidated with IR, NMR, Mass spectroscopy data and elemental analysis results. The antifungal activity of the compounds was determined against eleven different Fusarium, Trichoderma, Aspergillus and Penicilliumspeciesby using microdilution method. Most of the target compounds showed excellent antifungal activity against a variety of fungal pathogens

Synthesis and anti-cancer activity evaluation of new aurone derivatives

WOS: 000361328700014PubMed ID: 25716125In this study, we have synthesized 2-[3-or 4-(2-aryl-2-oxoethoxy) arylidene] benzofuran-3-one derivatives (D1-D38) and evaluated their anti-cancer activities. The final compounds were obtained in multistep synthesis reactions using benzofuranon-3-one derivatives (A1-A4, B) as starting materials which were gained in various synthetic ways. Aurone derivatives (C1-C10) were acquired with the condensation reaction of these starting materials and 3-/4-hydroxybenzaldehyde which were then reacted with a-bromoacetophenones to get final compounds. The anti-cancer activity of the selected compounds was performed by National Cancer Institute (NCI), USA against 60 human tumor cell lines derived from nine neoplastic diseases. Compounds exhibited anti-cancer activity in varying ratios.Anadolu University, Turkey (BAP) [050301]This work was supported by Anadolu University, Turkey (BAP Project No: 050301). The authors report no conflicts of interest

Synthesis and antiproliferative activity of 2-arylidene 6-(2-aryl-2-oxoethoxy) benzofuran-3-one derivatives

WOS: 000389460600011The synthesis of 2-arylidene 6-(2-aryl-2-oxoethoxy) benzofuran-3-one derivatives was reported and selected compounds were determined for their anticancer activity evaluation in National Cancer Institute NCI, USA according to the drug screening protocol of the institute against approximately 60 tumor cell lines derived from nine cancer diseases. Compound 3r, namely 2-(4-chlorobenzylidene)- 6-[2-(4-methoxyphenyl)-2-oxoethoxy] benzofuran-3-one exhibited the highest antitumor activity against non-small lung cancer cell lines.Anadolu University, Turkey (BAP Project) [050301]The study was financially supported by Anadolu University, Turkey (BAP Project No: 050301). The authors present their thanks to NCI (USA) and Anadolu University BIBAM (Turkiye) for anticancer test results and NMR spectra, respectively

Synthesis and anticancer activity of some 2-[3/4-(2-substituted phenyl-2-oxoethoxy)benzylidene]-6-substituted-2,3-dihydro-1H-inden-1-one derivatives

WOS: 000335394500005The synthesis of 2-[3/ 4-(2-substituted phenyl-2-oxoethoxy) benzylidene]-6-substituted-2,3-dihydro-1H-inden-1one derivatives and the investigation of their anticancer activity were studied. 2-(3- or 4-Hydroxybenzylidene)-6substituted- 2,3-dihydro-1H-inden-1-ones were reacted with suitable 2-bromoacetophenones to give 2-[3/ 4-(2-substituted phenyl-2-oxoethoxy) benzylidene]-6-substituted-2,3-dihydro-1H-inden-1-one derivatives. The structure elucidation of the synthesised compounds was performed by IR, 1H-NMR, mass spectroscopic data and elemental analyses. The anticancer screening was carried out in National Cancer Institute (NCI), USA. Notable activity was obtained for some compounds.Anadolu University, Turkey [050301]This work was supported by Anadolu University, Turkey (BAP Project No: 050301). NCI, USA is gratefully acknowledged for investigating anticancer activity