J. Appl. Cryst.の発刊に際して

The nitro group is considered to be a versatile and unique functional group in medicinal chemistry. Despite a long history of use in therapeutics, the nitro group has toxicity issues and is often categorized as a structural alert or a toxicophore, and evidence related to drugs containing nitro groups is rather contradictory. In general, drugs containing nitro groups have been extensively associated with mutagenicity and genotoxicity. In this context, efforts toward the structure–mutagenicity or structure–genotoxicity relationships have been undertaken. The current Perspective covers various aspects of agents that contain nitro groups, their bioreductive activation mechanisms, their toxicities, and approaches to combat their toxicity issues. In addition, recent advances in the field of anticancer, antitubercular and antiparasitic agents containing nitro groups, along with a patent survey on hypoxia-activated prodrugs containing nitro groups, are also covered.

Nitro-Group-Containing Drugs

Modern analytical techniques can determine a multitude of fungal metabolites contaminating food and feed. In addition to known mycotoxins, for which maximum levels in food are enforced, also currently unregulated, so-called “emerging mycotoxins” were shown to occur frequently in agricultural products. The aim of this review is to critically discuss the relevance of selected emerging mycotoxins to food and feed safety. Acute and chronic toxicity as well as occurrence data are presented for enniatins, beauvericin, moniliformin, fusaproliferin, fusaric acid, culmorin, butenolide, sterigmatocystin, emodin, mycophenolic acid, alternariol, alternariol monomethyl ether, and tenuazonic acid. By far not all of the detected compounds are toxicologically relevant at their naturally occurring levels and are therefore of little or no health concern to consumers. Still, gaps in knowledge have been identified for several compounds. These gaps should be closed by the scientific community in the coming years to allow a pr...

http://pubs.acs.org/doi/pdf/10.1021/acs.jafc.6b03413

Emerging Mycotoxins: Beyond Traditionally Determined Food Contaminants

Catalytic dehydrogenation of a wide variety of benzo fused N-heterocycles is achieved in the presence of a cyclometalated iridium complex as the catalyst in the absence of any oxidant or acceptor for hydrogen.

Acceptorless Dehydrogenation of Nitrogen Heterocycles with a Versatile Iridium Catalyst

We report formal [3 + 3] annulations of aromatic azides with aromatic imines and azobenzenes to give acridines and phenazines, respectively. These transformations proceed through a cascade process of Rh(III)-catalyzed amination followed by intramolecular electrophilic aromatic substitution and aromatization. Acridines can be directly prepared from aromatic aldehydes by in situ imine formation using catalytic benzylamine.

Facile synthesis of unsymmetrical acridines and phenazines by a Rh(III)-catalyzed amination/cyclization/aromatization cascade.

http://www.if-pan.krakow.pl/pjp/pdf/2011/2_305.pdf

Natural and synthetic acridines/acridones as antitumor agents: their biological activities and methods of synthesis.

Many people in the world struggle with cancer or bacterial, parasitic, viral, Alzheimer's and other diseases. Therefore, many scientists seek new, more effective, more selective and less toxic drugs. Acridine/acridone derivatives constitute a class of compounds with a broad spectrum of biological activity and are of great interest to scientists. To date, many acridine/acridone analogues have been obtained, which, inter alia, exhibit antitumour (e.g., (1–5)), antimicrobial (e.g., (59)), and antiviral (e.g., (61)) activities and are applicable in the treatment of Alzheimer's disease (e.g., (26)). However, in many cases, their clinical application is limited and excluded because of side effects. In this survey, we describe acridine and acridone derivatives reported since 2013, methods of their synthesis and their potential clinical applications.

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Recent developments in the synthesis and biological activity of acridine/acridone analogues

Opracowano synteze wysoce rozgalezionego poli(aryleno-oksyndolu) na drodze reakcji polimeryzacji pochodnej 5-bromoizatyny, a nastepnie modyfikacji terminalnych jednostek izatynowych. Tak przygotowany polimerowy rdzen, charakteryzujący sie stopniem rozgalezienia 100 %, byl substratem do rodnikowej polimeryzacji z przeniesieniem atomu (z ang. ATRP) w reakcji z akrylanem tert-butylu. Otrzymane kopolimery zawierające hydrofobowy rdzen i alkilowe lancuchy zakonczone wolnymi grupami karboksylowymi tworzą sferyczne nanocząstki. Przedstawiono wstepne wyniki badan dotyczących ich wlaściwości fizykochemicznych oraz potencjalnych zastosowan.

Core‐shell nanoparticles with hyperbranched poly(arylene‐oxindole) interiors

Synthesis and biological activity of mycophenolic acid-amino acid derivatives.

BACKGROUND Immunomodulation is one of the significant therapeutic strategies. It includes both stimulation and suppression of the immune system by a variety of substances called immunomodulators, designed to regulate the immune response of the organism against infections of varying etiology. An example of such a substance is tuftsin (TKPA) 3 (Fig. (1)). In this paper were included tuftsin derivatives, which were described over the years, their together with biological activity and clinical potential. METHODS We reviewed a bibliographic database to gather all the important information about the tuftsin peptide. We have delineated the significant information on the activity of the tetrapeptide itself and its derivatives. Analogs were divided because of their anti-tumor, anti-inflammatory, antimicrobial and anti-viral activity. RESULTS This paper describes eighty-six documents. Thirty-two of them concern on activity of tuftsin in the human organism. The remaining fifty-four describe peptide analogues and their properties, including eleven papers about the tuftsin-based peptides contained in the vaccines, nine papers representing anticancer activity of the tuftsin derivatives, twenty-six about antiinflammatory compounds, and five papers describing the antitumor activity of the tuftsin analogs. CONCLUSION The findings of this review confirm the importance of the tuftsin and their derivatives. Most of these substances showed anti-tumor, anti-inflammatory or antibacterial activities. A large amount of the compounds may find use in vaccines. Tuftsin can also be used to prepare fusion proteins in the treatment of cancer and as carriers of many biologically active substances.

Grzegorz Cholewinski

Papers

Natural and synthetic acridines/acridones as antitumor agents: their biological activities and methods of synthesis.

Recent developments in the synthesis and biological activity of acridine/acridone analogues

Core‐shell nanoparticles with hyperbranched poly(arylene‐oxindole) interiors

Synthesis and biological activity of mycophenolic acid-amino acid derivatives.

Tuftsin - Properties and Analogs.