Over expression of nucleotide pyrophosphatase (NPPs) activity is associated with chondrocalcinosis, osteoarthritis, type 2 diabetes, neurodegenerative diseases, allergies and cancer metastasis.
Benzothiazoloquinazolines are known to possess several interesting biological properties. Various arylated benzothiazoloquinazolines were synthesized from readily available 2‐bromo‐12H ‐benzothiazolo[2,3‐b]quinazolin‐12‐one by palladium catalysed Suzuki‐Miyaura reactions in 43 – 85% yield. Synthesized derivatives were analysed regarding their in vitro inhibition activity towards monoamine oxidases A and B and showed significant inhibitory values in the micromolar range. Molecular modelling as well as PAINS studies on the binding interaction of most potent inhibitors with both isoforms were studied to verify the experimental results.
In Kazakhstan, there is a problem of finding ways to clean local sites contaminated with pesticides. In particular, such sites are the deserted and destroyed storehouses where these pesticides were stored; existing storehouses do not fulfill sanitary standards. Phytoremediation is one potential method for reducing risk from these pesticides. Genetic heterogeneity of populations of wild and weedy species growing on pesticide-contaminated soil provides a source of plant species tolerant to these conditions. These plant species may be useful for phytoremediation applications. In 2008-2009 and 2011, we surveyed substances stored in 80 former pesticide storehouses in Kazakhstan (Almaty oblast) to demonstrate an inventory process needed to understand the obsolete pesticide problem throughout the country, and observed a total of 354.7 t of obsolete pesticides. At the sites, we have found organochlorine pesticides residues in soil including metabolites of dichlorodiphenyltrichloroethane and isomers of hexachlorocyclohexane. Twenty-four of the storehouse sites showed pesticides concentrations in soil higher than maximum allowable concentration which is equal to 100 μg kg(-1) in Kazakhstan. Seventeen pesticide-tolerant wild plant species were selected from colonizing plants that grew into/near the former storehouse's pesticides. The results have shown that colonizing plant annual and biannual species growing on soils polluted by pesticides possess ability to accumulate organochlorine pesticide residues and reduce pesticide concentrations in soil. Organochlorine pesticides taken up by the plants are distributed unevenly in different plant tissues. The main organ of organochlorine pesticide accumulation is the root system. The accumulation rate of organochlorine pesticides was found to be a specific characteristic of plant species and dependent on the degree of soil contamination. This information can be used for technology development of phytoremediation of pesticide-contaminated soils.
The combination of cyclocondensation with palladium catalysed cross‐coupling reactions, afforded a variety of 8‐functionalized benzothiazolo[3,2‐a]pyridimidin‐4‐ones in good to excellent yields. The anti‐proliferative potential of the synthetic compounds was evaluated in human cervical adenocarcinoma cells (HeLa) and hamster normal fibroblasts (BHK‐21). Three of the test derivatives exhibited the strongest cytotoxicity in HeLa cells with the median inhibitory concentration (IC50) of 0.93, 1.55 and 1.84 μM, respectively. Moreover, their anti‐proliferative effect was three times less strong in normal fibroblasts, asserting their possible anti‐cancer potential.
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