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We investigated the anticancer potential of 5-amino-2-[p-bromophenyl]-benzoxazole [BB] which is a new benzoxazole derivative in different breast cancer cell lines. BB was applied to estrogen receptor positive [ER+] MCF-7 and receptor negative [ER-] MDA-MB cell lines and its effects were determined by histopathological examinations, viability test [MTT], immunocytochemistry assays [Tunnel, VEGF and eNOS]. Moreover, its effects on apoptozis-related proteins such as Apaf-1, cytochrome C, caspase-3, bcl-2 and NF-κB were examined by western blot. Histopathological examinations showed that BB killed many cells for both cancer cell line while the cells lost their adhesion in MCF-7 and lost their adhesion and epiteloid morphology in MDA-MB. MTT analyses demonstrated that BB caused a clear dose depended toxic effect for both cell types. BB application resulted in an increase labeled apoptotic cells after Tunnel staining which was more obvious for MDA-MB compared to that of MCF-7. VEGF staining was decreased after BB application in both cell lines. The decrease of VEGF staining was clearer for MDA-MB compared to that of MCF-7. The status of oxidative stress was shown by eNOS immunocytochemistry which was increase after BB application in both cell lines. The levels of Apaf-1 and bcl-2 were found to be similar while caspase 9 and NF-κB levels were decreased compared to the control group after BB application for both cell lines. On the other hand, cytochrome C levels were slightly increased in MCF-7 cells while this increase was found very obvious in MDA-MB cell lines in BB groups. In conclusion, BB which is a new benzoxazole derivative have shown significant anticancer effects by increasing apoptosis and decreasing angiogenesis in MCF-7 or MDA-MB breast cancer cell lines. These effects of BB seem to be more prominent for [ER-] MDA-MB cell lines which mimic more aggressive type of breast cancer. These results suggest that BB may be useful to treat [ER-] breast cancers and may be added to treatment protocols. [ABSTRACT FROM AUTHOR]

The 2-amino-4′-flouro-benzophenone ( 1) that was reacted with chloroacetylchloride to afford 2-chloro- N-(2-(4′-fluorobenzoyl) phenyl)acetamide ( 2) was subsequently converted to 1,4-benzodiazepines ( 3) by the modification of the known hexamethylenetetramine based reaction developed by Blazevic and Kajfez. Thus, obtained product ( 3) was reacted with a variety of alkyl halide using KOH in DMF to give 1-substituted-5-(4-fluorophenyl)-1 H-benzo[e][1,4]diazepin-2(3 H)-one ( 4a, 4b). To achieve 1, 3-disubstituted 1, 4-benzodiazepines ( 5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i, 5j, 5k, 5l, 5m, 5n, 5o, 5p, 5q, 5r, 5s, 5t), 1-substituted-5-(4-fluorophenyl)-1 H-benzo[e][1,4]diazepin-2(3 H)-one ( 4a, 4b) was treated with various aromatic aldehydes in the presence of KOH in toluene. [ABSTRACT FROM AUTHOR]

A systematic analysis of all naturally-occurring glycosylated bacterial secondary metabolites reported in the scientific literature up through early 2013 is presented. This comprehensive analysis of 15 940 bacterial natural products revealed 3426 glycosides containing 344 distinct appended carbohydrates and highlights a range of unique opportunities for future biosynthetic study and glycodiversification efforts. [ABSTRACT FROM AUTHOR]

Ambazone is a pharmaceutical compound that possesses antiseptic activity and tested as well for anti-tumor properties. Metal complexes of Zn(II), Fe(III), and Cu(II) containing ambazone as ligand were synthesized using a molar ratio salt:ligand of 1:1, heating the mixture up to 50 °C for 6 h. Coordination compounds were characterized by thin-layer chromatography, FT-IR spectroscopy, elemental analysis, and thermal behavior. The non-isothermal experiments were carried out in order to investigate the thermal degradation process of these complexes and were performed in a dynamic air atmosphere at a heating rate β = 10 °C min from ambient temperature, up to 500 °C. It was revealed that decomposition process is a multistadial one. [ABSTRACT FROM AUTHOR]

At the Delft University of Technology (DUT), the data of six stations participating in the first international GLONASS (Global Navigation Satellite System, the Russian counterpart of GPS) tracking campaign, IGEX-98, were analyzed with integrity monitoring software. The software was developed at the Department of Mathematical Geodesy and Positioning of DUT. The main function of this software is to detect slips and outliers in phase and code observations in real time. In addition, the software also allowe the validation of the information contained in the broadcast navigation messages. The results of the IGEX-98 data analyses will be presented in a three-part series. In this second part of the series, GLONASS outlier and slip statistics will be discussed in detail. The first part was concerned with the availability of GLONASS observations, while in the third one the broadcast navigation message validation results will be considered. © 2000 John Wiley & Sons, Inc. [ABSTRACT FROM AUTHOR]

ZIMET 3164 inhibited the growth of sarcoma 180 P, sarcoma 180 G, and Walker 256 carcinosarcoma, but was unable to prolong the survival time of mice bearing Ehrlich ascites carcinoma or the leukaemias L 1210 and LAJ I to a worthwhile extent. The primary and secondary haemagglutinin formation to xenogenic red blood cells and immunological memory were significantly suppressed in mice. The drug exerted maximum effect when given on days −2 to +2 relative to antigenic stimulus. Administration exclusively prior to immunization induced only moderate immunosuppression while injection afterwards failed to affect the primary response at all, suggesting that the drug interferes with the afferent limb of immune response. In general, ZIMET 3164 proved to be half as effective as cyclophosphamide, but more effective than chlorambucil. [ABSTRACT FROM AUTHOR]

Because of the spread of drug resistance, it is necessary to look for new antibiotics that are effective against pathogenic microorganisms. The purpose of this study was to analyse the species composition of actinobacteria isolated from the digestive tract of the millipedes Nedyopus dawydoffiae and to determine their antimicrobial properties. Species identification was carried out on the basis of the morphological and culture properties and the sequence of the 16S rRNA gene. Actinobacteria were grown in different liquid media. Antibiotic properties were determined against some Gram-positive and Gram-negative bacteria as well as fungi. Of the 15 isolated strains, 13 have antibiotic activity against Gram-positive bacteria (including methicillin-resistant Staphylococcus aureus—MRSA) and fungi, but there was no antibiotic activity against Gram-negative test strains Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853. It was established that antibiotic-producing actinobacteria belong to eight species of the genus Streptomyces. Depending on the nutrient medium, actinobacteria demonstrate different antimicrobial activities. As an example, S. hydrogenans shows that even strains selected in one population differ by the range of antimicrobial activity and the level of biosynthesis. Since the antibiotic production is considered as a feature for species competition in the microbiota community, the variability of antibiotic production among different strains of the same species is an adaptive characteristic for the competition in millipedes' digestive tract community. [ABSTRACT FROM AUTHOR]