New Pyrazolothiazole as Potential Wnt/β‐Catenin Inhibitors: Green Synthesis, Characterization, Antimicrobial, Antioxidant, Antineoplastic Evaluation, and Molecular Docking Study

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Abstract

In our attempt to develop potential new drug candidates with promising antimicrobial, antioxidant, and anticancer activities, a series of novel pyrazolothiazole derivatives (PTDs) were synthesized via conventional heating and microwave irradiation as a green technique. The synthesized compounds were characterized through different spectroscopic methods and elemental analyses. Moreover, these compounds were tested for their antimicrobial activity, antioxidant potency, and in‐ silico cancer prevention potential by inhibiting the wingless (Wnt)/β‐catenin signaling pathway, a potent method for cancer cell death. Our results showed that all compounds exhibited antimicrobial impact against E. coli, S. aureus, P. aeuroginosa, B. subtilis, A. flavus, and C. Albicans as well as antioxidant scavenging activity. In addition, the in‐ vitro cytotoxic evaluation of each compound was performed on a panel of cancer cell lines and they agreed with the molecular docking simulation results. Our findings showed that the newly synthesized pyrazolothiazole derivatives offer great potential as antimicrobial and anticancer agents.

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Rapid colorimetric assay for cellular growth and survival: Application to proliferation and cytotoxicity assays

Tim R. Mosmann (1983)

A tetrazolium salt has been used to develop a quantitative colorimetric assay for mammalian cell survival and proliferation. The assay detects living, but not dead cells and the signal generated is dependent on the degree of activation of the cells. This method can therefore be used to measure cytotoxicity, proliferation or activation. The results can be read on a multiwell scanning spectrophotometer (ELISA reader) and show a high degree of precision. No washing steps are used in the assay. The main advantages of the colorimetric assay are its rapidity and precision, and the lack of any radioisotope. We have used the assay to measure proliferative lymphokines, mitogen stimulations and complement-mediated lysis.

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Francesca Prestinaci, Patrizio Pezzotti, Annalisa Pantosti (2015)

Antimicrobial resistance (AMR) is one of the most serious global public health threats in this century. The first World Health Organization (WHO) Global report on surveillance of AMR, published in April 2014, collected for the first time data from national and international surveillance networks, showing the extent of this phenomenon in many parts of the world and also the presence of large gaps in the existing surveillance. In this review, we focus on antibacterial resistance (ABR), which represents at the moment the major problem, both for the high rates of resistance observed in bacteria that cause common infections and for the complexity of the consequences of ABR. We describe the health and economic impact of ABR, the principal risk factors for its emergence and, in particular, we illustrate the highlights of four antibiotic-resistant pathogens of global concern - Staphylococcus aureus, Klebsiella pneumoniae, non-typhoidal Salmonella and Mycobacterium tuberculosis - for whom we report resistance data worldwide. Measures to control the emergence and the spread of ABR are presented.

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Pyrazole containing natural products: synthetic preview and biological significance.

Ricky Sharma, K Kaur, G Gupta … (2013)

A large number of structurally diverse natural compounds containing azole nucleus constitute an important class of biologically active heterocycles that are gaining more attention in the field of medicinal chemistry. Among azoles, pyrazoles are rarely found in nature probably due to difficulty in the formation of N-N bond by living organisms. However, they exhibit numerous biological activities, including anti-diabetic, antiviral, anticancer, anti-inflammatory, antibacterial and antifungal activities. The present review is an attempt to understand the chemistry along with medicinal importance of pyrazole containing natural products reported till date which would certainly help the scientific community to bring further developments in the isolation and synthetic methodologies for pyrazole based novel bioactive compounds. Copyright © 2013 Elsevier Masson SAS. All rights reserved.