Background: Pyrazole and its derivatives are known to exhibit significant biological and pharmacological activities such as anticancer, anti-inflammatory, antioxidant, antibacterial, analgesic, antiviral, antimicrobial, antifunga, anti-glycemic, antiamoebic, and antidepressive . Considering the immense biological properties, pyrazole is one of the most wide studied nitrogen-containing heterocyclic nuclei. Fused pyrazole derivatives are composed of the pyrazole nucleus attached to other heterocyclic moieties. Objective: The objective of this article is the synthesis of some new pyrazolo[1,5-a]pyrimidine and pyrazolo[5,1-c]1,2,4-triazine derivatives with potential anticancer and antimicrobial activities. Method: To evaluate The in vitro growth inhibitory rates (%) and inhibitory growth activity (as measured by IC50) of the newly synthesized compounds were determined against the MCF-7 human breast carcinoma cell line in comparison with the well-known anticancer drug doxorubicin as the standard, using the MTT viability assay. Data generated were used to plot a dose response curve from which the concentration (µM) of tested compounds required to kill 50% of cell population (IC50) was determined. Cytotoxic activity was expressed as the mean IC50 of three independent experiments. The difference between inhibitory activities of all compounds with different concentrations was statistically significant p < 0.001. All compounds were structurally characterized by different spectroscopic techniques EI-MS, 1H-NMR, 13C-NMR, and evaluated for their anticancer and antimicrobial activities (antibacterial and antifungal). Results: Several pyrazolo[1,5-a]pyrimidine derivatives were synthesized from the reaction of 2-(4-(5-amino-1H-pyrazol-3-yl)phenyl)-1H-indene-1,3(2H)-dione with the appropriate active methylene compounds in a boiling ethanol. Also, pyrazolo[5,1-c]triazines were obtained through the reaction of 2-(4-(5-(chlorodiazenyl)-1H-pyrazol-3-yl)phenyl)-1H-indene-1,3(2H)-dione with various active methylene compounds in ethanol containing sodium acetate at 0-5 0C. The structures of the newly synthesized compounds were elucidated on the basis of elemental analysis, spectral data, and alternative synthetic routes whenever possible. The newly synthesized compounds were evaluated for their antitumor activity against a breast cancer cell line (MCF-7) and a human colon cancer cell line (HCT-116). The results revealed that the tested compounds showed high variation in the inhibitory growth rates and activities against the tested tumor cell lines. All newly synthesized compounds screen towards microorganisms e.g. Gram-negative bacteria, Gram-positive bacteria and Fungi. Conclusions: 2-(4-(5-Amino-1H-pyrazol-3-yl)phenyl)isoindoline-1,3-dione proved to be a useful precursor for synthesis of various pyrazolo[1,5-a]pyrimidine and pyrazolo[5,1-c]-1,2,4-triazines. The structures of the newly synthesized compounds were confirmed by spectral data and elemental analyses. The newly synthesized compounds were tested in-vitro against the MCF-7, HCT-116 human cancer cell line and compared with doxorubicin as the standard, using the MTT viability assay. Most of the tested compounds were found to have moderate to high anticancer activity.
Mobile technology is a growing field with emerging new discoveries. The introduction of third generation mobile network services and the convergence of mobile and traditional internet services will make the mobile communication a key enabler for achieving competitive advantages in developing countries, including opportunities for mobile learning (M-learning). This study explores the possibility of applying M-learning in Egypt by looking at the factors that affect the students’ intentions to adopt M-learning. Data was collected by a survey of 239 business students of the English program in the faculty of commerce at Mansoura University. The technology adoption model is studied with two more independent variables, namely, pressure to act and resource availability. Results showed that there are four factors that can be used in modelling students’ intentions to adopt M-learning. These factors are attitude towards M-learning, perceived usefulness, availability of resources and perceived ease of use.
Background Thiazole is a core structural motif presents in a wide range of natural products. Thiazole derivatives also have a wide range of medicinal and biological properties. Results The reaction of hydrazonoyl halides with 2-(1-(4-(1,3-dioxoisoindolin-2-yl)phenyl)ethylidene)hydrazinecarbothioamidein ethanol and triethylamine yielded 2-(4-(1-(2-(4-(2-Arylhydrazono)-5-s-4,5-dihydrothiazol-2-yl)hydrazono)-ethyl)phenyl)isoindoline-1,3-dione and 2-(4-(1-(2-(5-(2-Arylhydrazono)-4-oxo-4,5-dihydrothiazol-2-yl)hydrazono)ethyl)-phenyl)isoindoline-1,3-dione.The reaction of 2-(4-(1-(2-(4-oxo-4,5-dihydrothiazol-2-yl)hydrazono)ethyl)phenyl)isoindoline-1,3-dione with arylidenemalononitrile also yielded 5-amino-2-(2-(1-(4-(1,3-dioxoisoindolin-2-yl)phenyl)ethylidene)hydrazinyl)-7-substituted-7 H -pyrano[2,3- d ]thiazole-6-carbonitrile. The structures of the newly synthesized compound were elucidated whenever possible on the basis of elemental analysis, spectral data, and alternative synthetic routes. Three of them were evaluated against a breast cancer cell line for their antitumor activity. Conclusions Compound (1) has been shown to be useful in the synthesis of a new series of 1,3-thiazole, pyrano[2,3- d ]thiazole and 4,5-dihydrothiazolo[4,5- b ]pyridine derivatives using hydrazonoyl halides as precursors. The anticancer efficacy of compounds (9b) , (9e) , and (9f) against MCF-7, a breast cancer cell line, was also compared to the standard anticancer drug doxorubicin. Electronic supplementary material The online version of this article (10.1186/s13065-019-0559-x) contains supplementary material, which is available to authorized users.
In view of the broad physiological activity of organometallic and organophosphorus compounds, the present paper deals with the synthesis of 2-(4-methoxybenzylidene amino) benzene-thiol, its metallation with mercury (II), nickel (II), palladium (II), and phosphorylation. The antimicrobial activities of all products were investigated. The palladated product displays a significant anticancer activity against human breast carcinoma cell. All the new products were investigated and their structures were elucidated using elemental analyses, thermal analysis, and spectroscopic data.
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