3-Cyanopyridine derivatives are known for exhibiting excellent anticancer activity due to their strong capability to inhibit various biological targets, including Pim-1 kinase, survivin, and tubulin polymerization. On the other hand, N-acylhydrazones (NAH) are known to be a very versatile motif in medicinal chemistry and drug design. Based on these data, we report in this paper, the synthesis of novel 3-cyanopyridines incorporating N-acyl hydrazine scaffold, the evaluation of their cytotoxicity on the breast (MCF-7) and ovarian (A-2780) cancer cell lines and their antioxidant properties.
View Article and Find Full Text PDFSeven novel pyrazole derivatives (4a-g) and four novel starting compounds incorporating substituted pyridine moieties were synthesized successfully. Cell viability assay for the tested compounds was performed, and the inhibitory concentrationlogarithmic 50 (LogIC ) values of the compounds were calculated after a 24-h treatment. Four of the examined compounds (3d, 3g, 4f, and 4g) showed comparable cytotoxic activity against CaCo-2 compared to the standard drug docetaxel at 0.
View Article and Find Full Text PDFSix new monopeptides, seven new dipeptides, and two deprotected monopeptide dihydroquinolinone conjugates were prepared by the benzothiazole-mediated method and their structures were confirmed by nuclear magnetic resonance, mass, infrared spectroscopy, and elemental analysis methods. The human carbonic anhydrase (hCA) I and hCA II enzyme inhibition activities of the compounds were determined using the stopped-flow instrument. The synthesized peptide-dihydroquinolinone conjugates 2, 3, 6, 10, 13, and 15 showed inhibition against the hCA II enzyme in the range of 15.
View Article and Find Full Text PDFNew dipeptide-dihydroquinolinone derivatives were successfully synthesised by benzotriazole mediated nucleophilic acyl substitution reaction and their structures were elucidated by spectroscopic and analytic techniques. The carbonic anhydrase (CA, EC 4.2.
View Article and Find Full Text PDFA series of amino acid-sulphonamide conjugates was prepared through benzotriazole mediated coupling reactions and characterised by H-NMR, C-NMR, MS, and FTIR spectroscopic techniques as well as elemental analysis. The carbonic anhydrase (CA, EC 4.2.
View Article and Find Full Text PDFThirteen novel benzothiazole derivatives incorporating glycine, methionine, alanine, and phenylalanine were synthesised by facile acylation reactions through benzotriazole or DCC mediated reactions and their structures were identified by H-NMR, 13C-NMR, and FT-IR spectroscopic techniques and elemental analysis. The carbonic anhydrase (CA, EC 4.2.
View Article and Find Full Text PDFThirty novel sulfonamide derivatives incorporating dipeptide were synthesized by facile acylation through benzotriazole mediated reactions and their structures were identified by H NMR, C NMR, MS and FT-IR spectroscopic techniques and elemental analysis. The carbonic anhydrase (CA, EC 4.2.
View Article and Find Full Text PDFTwenty-four novel sulfonamide derivatives incorporating dipeptide tails were synthesized by facile acylation reactions of homosulfanilamide through benzotriazole or dicyclohexyl carbodiimide (DCC) mediated coupling reactions. The carbonic anhydrase (CA, EC 4.2.
View Article and Find Full Text PDFN-protected amino acids (Gly, Ala and Phe protected with Boc and Z groups) were reacted with sulfonamide derivatives, leading to the corresponding N-protected amino acid-sulfonamide conjugates. The carbonic anhydrase (CA, EC 4.2.
View Article and Find Full Text PDFN-protected amino acids were reacted with substituted benzothiazoles to give the corresponding N-protected amino acid-benzothiazole conjugates (60-89%). Their structures were confirmed by proton nuclear magnetic resonance ((1)H NMR), carbon-13 nuclear magnetic resonance ((13)C NMR), IR and elemental analysis. Their carbonic anhydrase (CA, EC 4.
View Article and Find Full Text PDFN-Protected amino acids (Gly, Ala and Phe) were reacted with amino substituted coumarin and quinolinone derivatives, leading to the corresponding N-protected amino acid-coumarin/quinolinone conjugates. The carbonic anhydrase (CA, EC 4.2.
View Article and Find Full Text PDFNovel, cyclic peptidomimetics were synthesized by facile acylation reactions using benzotriazole chemistry. Microbiological testing of the synthesized compounds revealed an exceptionally high activity against Candida albicans with a minimum inhibitory concentration (MIC) two orders of magnitude lower than the MIC of the antifungal reference drug amphotericin B. A strikingly high activity was also observed against three Gram-negative bacterial strains (Pseudomonas aeruginosa, Klebsiella pneumoniae and Proteus vulgaris), two of which are known human pathogens.
View Article and Find Full Text PDFGuang Pu Xue Yu Guang Pu Fen Xi
September 2014
Eleven important medicinal plants generally used by the people of Turkey for the treatment of common cold have been studied for their mineral contents. Eleven minor and major elements (essential, non-essential and toxic) were identified in the Asplenium adiantum-nigrum L. , Althaea officinalis L.
View Article and Find Full Text PDFHydrodistilled volatile oil from the aerial parts of Achillea cretica L. (Asteraceae) was analysed by a combination of GC and GC/MS. Seventy-six components were identified, constituting 86.
View Article and Find Full Text PDFKarakaya Dam Lake (KDL) is one of the most important water sources, both for irrigation and fishery, located in eastern part of Turkey. This study is concerned with the pollution of the lake contributed by urban, industrial and agricultural activities. The parameters selected for this aim were the enzymes commonly used as biomarkers of environmental pollution.
View Article and Find Full Text PDFDeficiency of serum vitamin A is one of the widespread public health problem among pre-school children in developing countries. A limited number of studies have been done about this problem in Turkey and there is no similar work done in Malatya. Serum vitamin A and beta-carotene levels in 56 pre-school age children who had recurrent acute respiratory infections (ARI) or recurrent diarrhoea were determined by a UV/VIS spectrometer.
View Article and Find Full Text PDFSerum zinc, copper and magnesium levels were measured using atomic absorption spectrophotometry in 41 obese and 41 healthy (control) children (between 7 and 11 years of age) who were living in Malatya (Turkey). Serum zinc levels of obese children (mean value 102.40 +/- 2.
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