The discovery of new compounds with antitumoral activity has become one of the most important goals in medicinal chemistry. One interesting group of chemotherapeutic agents used in cancer therapy comprises molecules that interact with DNA. Research in this area has revealed a range of DNA recognizing molecules that act as antitumoral agents, including groove binders, alkylating and intercalator compounds. DNA intercalators (molecules that intercalate between DNA base pairs) have attracted particular attention due to their antitumoral activity. For example, a number of acridine and anthracycline derivatives are excellent DNA intercalators that are now on the market as chemotherapeutic agents. Commercially available acridine and anthracycline derivatives have been widely studied from a variety of viewpoints, such as physicochemical properties, structural requirements, synthesis and biological activity. However, the clinical application of these and other compounds of the same class has encountered problems such as multidrug resistance (MRD), and secondary and/or collateral effects. These shortcomings have motivated the search for new compounds to be used either in place of, or in conjunction with, the existing compounds. Unfortunately, the results of this search have not met expectations. The vast majority of candidate intercalator compounds tested for use as anticancer agents have shown little or no biological activity. Research in this area has not been without benefits, however, for it has produced much information on the synthesis and antitumoral properties of hundreds of compounds, which have been tested on diverse tumoral cell lines. This review considers the structural and biological considerations relevant to the use of DNA intercalators and bis-intercalators as antitumoral agents, with an emphasis on the relationship between structure and activity, produced in last decade.
The aim of this work was to characterize the mucilage extracted from six species of Opuntia. The species studied were as follows: O. atropes, O. tomentosa, O. hyptiacantha, O. streptacantha y O. joconostle and O. ficus‐indica. The first step was to find the best extraction conditions to obtain an unaltered chemical structure of mucilage. The mucilages were characterized using high‐performance liquid chromatography and Fourier transform infrared spectroscopy techniques. The optimal conditions employed to obtain the mucilage were: ratio of cladodes : ethanol solution at 50% of 1:1 (w/v), temperature of 22C and precipitation of mucilage with a solution of ethanol 96%, at a ratio of 1:4 (v/v). Mucilage from all species studied had a high content of soluble dietary fiber, ranging from 51.79 to 67.51%. In decreasing order, sugars found in the mucilages were: L‐arabinose (26.83–35.36%), D‐galactose (21.59–45.48%), D‐xylose (12.23–17.05%), uronic acids (5.59–13.91%), D‐glucose (5.18–16.21%) and L‐rhamnose (1.41–5.40%).
Practical Applications
This research presents an optimization method for the extraction of mucilage five wild species of cactus based on temperature and time of extraction and solvent ratio: sample used. Mucilages were characterized chemically and by chromatographic and Fourier transform infrared spectroscopy techniques and were compared with the species mucilage Opuntia ficus‐indica, the species most commercially studied. The mucilage obtained can be used for commercial purposes as additives in the food industry.
In regard to the actual public health global emergency and, based on the state of the art about the ways to inhibit the SARS-CoV-2 treating the COVID19, a family of 1,5-disubstituted tetrazole-1,2,3-triazoles, previously synthesized, have been evaluated through in silico assays against the main protease of the mentioned virus (CoV-2-MPro). The results show that three of these compounds present a more favorable interaction with the selected target than the co-crystallized molecule, which is a peptide-like derivative. It was also found that also hydrophobic interactions play a key role in the ligand-target molecular couplings, due to the higher hydrophobic surfaces into the active site. Finally, a pharmacophore model has been proposed based on the results below, and a family of 1,5-DT derivatives has been designed and tested with the same methods employed in this work. It was concluded that the compound with the isatin as a substituent (P8) present the higher ligand-target interaction, which makes this a strong drug candidate against COVID19, due can inhibit the CoV-2-MPro protein.
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