Current Issue : January - March Volume : 2019 Issue Number : 1 Articles : 6 Articles
Anticancer screening of several novel thienopyrimidines has been performed. The thienopyrimidine\nderivatives were synthesized from available starting materials according to the convenient\nsynthetic procedures using a one-pot solvent-free reaction which gave a wide access to\nthienopyrimidine-derivative production. The synthesized compounds were preselected via molecular\ndocking to be tested for their anticancer activity in NCI 60 cell lines. It was observed that some\ncompounds showed remarkable anticancer activity. It was found that the most active compound\namongthieno[2,3-d]pyrimidine-4(3H)- ones is 2-(benzylamino)-5,6-dimethylthieno[2,3-d]pyrimidin-\n4(3H)-one, which possesses cytotoxic activity on almost all cancer cell lines with mean growth\n51.01%, where the most sensitive was the melanoma cell line MDA-MB-435 with GP (Growth Percent) ......... The patterns of structureâ??activity that are important for further optimization of the\nstructure and the creation of more selective and active anticancer agents were proposed....
In order to biomimetic synthesize hydroxyapatite similar to natural bone. Hydroxyapatite (HAP) is biomimetic synthesized in\nsimulated body fluid (SBF) by addition of imidazole-4,5-dicarboxylic acid grafted chitosan (IDACS). The effect of molar ratio of\nchitosan (CS) to imidazole-4,5-dicarboxylic acid (IDA) on preparation of HAP was investigated. The structure, size, and crystal\nphase of the obtained hydroxyapatite were observed by Fourier transform infrared spectroscopy, X-ray powder diffraction, and\nscanning electron microscopy. The results show that the molar ratio of CS to IDA is 1 : 3, the temperature is ... the aging time\nis 48 h, the synthesized nanorod-like hydroxyapatite with diameter 20â??30 nm, and length ranging from 75 to 120nm presents\nexcellent phase, which disperses well and is similar to the natural bone of HAP. The obtained HAP can be used to remove\nchromium(VI) by the orthogonal experiments, and the results indicated that the removal rate can reach 95.66% under the\noptimum conditions. These results suggest that the morphology of the obtained HAP is more affected by the material ratio of\nchitosan to imidazole-4,5-dicarboxylic acid than its structure, and the obtained HAP can effectively remove Cr(VI), which\nprovides a novel method for biomimetic synthesis of other biomaterials and application in the water purification....
A convenient total synthesis of (Z)-12-tetradecenyl acetate (1a) and (E)-12-tetradecenyl acetate (1b), which are the sex pheromones\nof Ostrinia furnacalis (Guen´ee), has been achieved. The target mixture molecules, of a cis-to-trans-isomer ratio of 27 to 73, were\nsynthesized in 40% overall yield and through [13C + 1C] synthetic strategy in five steps from commercially available and cheap\nindustrial brassylic acid as key starting material. The electroantennogram (EAG) responses of synthetic sex pheromone to ACB\nmale moths were conducted.The results showed that the target mixturemolecules were found to have a good activity and displayed\nsignificantly stronger EAG responses ranging from 10 to 1000 ... and the optimized stimulating dosage of the activity of synthetic\nsex pheromone to ACB males is 10... Compared with the existing routes, this synthetic approach is operationally simple, goodyielding,\nand cost-effective, which could serve as a basis for developing the techniques of sex pheromone mass trapping or mating\ndisruption and providing an environmentally benign method to control ACB pests....
Some species of the Baccharis genus have been shown to possess important biomedical properties, including cytotoxic activity.\nIn this study, we examined the cytotoxic effect of methanol extract from Baccharis obtusifolia (Asteraceae) in cancer cell lines of\nprostate (PC-3), colon (RKO), astrocytoma (D-384), and breast (MCF-7). The methanolic extract displayed the largest substantial\ncytotoxic effect in lines of colon cancer (RKO) and cerebral astrocytoma (D-384). Chromatographic purification of the B.\nobtusifolia methanolic extract led to the isolation and identification of ... dihydroxy ... methoxyflavone (1) and ... hydroxy ... dimethoxyflavone (2) compounds of the flavonoid type....
Bacterial resistance towards the existing class of antibacterial drugs continues to increase,\nposing a significant threat to the clinical usefulness of these drugs. These increasing and alarming\nrates of antibacterial resistance development and the decline in the number of new antibacterial\ndrugsâ?? approval continue to serve as a major impetus for research into the discovery and\ndevelopment of new antibacterial agents. We synthesized a series of D-/L-alaninyl substituted\ntriazolyl oxazolidinone derivatives and evaluated their antibacterial activity against selected standard\nGram-positive and Gram-negative bacterial strains. Overall, the compounds showed moderate\nto strong antibacterial activity. Compounds 9d and 10d (D- and L-alaninyl derivatives bearing\nthe 3,5-dinitrobenzoyl substituent), 10e (L-alaninyl derivative bearing the 5-nitrofurancarbonyl\ngroup) and 9f and 10f (D- and L-alaninyl derivatives bearing the 5-nitrothiophene carbonyl moiety)\ndemonstrated antibacterial activity ....... against Staphylococcus aureus, Staphylococcus\nepidermidis, Enterococcus faecalis and Moraxella catarrhalis standard bacterial strains. No significant\ndifferences were noticeable between the antibacterial activity of the D- and L-alaninyl derivatives as a\nresult of the stereochemistry of the compounds....
Many interesting applications have been found for nitroimidazoles as therapeutic agents.\nAmong others, some of these compounds can radiosensitize hypoxic tumor cells. The introduction\nof a second nitroimidazole ring to the molecule can improve the level of its pharmacological effect.\nThe aim of this article is to overview the literature concerning active compounds that contain two\nnitroimidazole moieties in their structures....
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