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Several studies have shown that expression of zinc‐finger protein 143 (ZNF143) is closely related to tumour progression including colon cancer. However, it remains unclear how ZNF143 expression is related to tumour progression within the tumour microenvironment. Here, we investigated whether ZNF143 expression affects the tumour microenvironment and tumour progression by screening molecules secreted by colon cancer cells stably expressing short‐hairpin RNAs against ZNF143 or control RNAs. We observed that secretion of interleukin (IL)‐8 was increased when ZNF143 expression was reduced in two colon cancer cell lines. The mRNA and protein levels of IL‐8 were increased in cells following ZNF143 knockdown, and this effect was reversed when ZNF143 expression was restored. The Janus tyrosine kinase/signal transducer and activator of transcription (JAK/STAT) and extracellular signal‐regulated kinase pathways were also shown to contribute to IL‐8 expression in ZNF143‐knockdown cells. The expression levels of ZNF143 and IL‐8 were inversely correlated with three‐dimensionally grown spheroids and colon cancer tissues. THP‐1 cells were differentiated when cells were incubated with condition media from colon cancer cell with less ZNF143, drastically. Loss of ZNF143 may contribute to the development of colon cancer by regulating intracellular and intercellular signalling for cell plasticity and the tumour microenvironment respectively.

The present investigation reports the stimulating effects of different substituted alkyl silatranes (3a-3e) on the early seedling growth of wheat (Triticum aestivum) and maize (Zea mays). Seeds of these plants were exposed to six different concentrations (0, 10, 50, 100, 200 and 500 µmol L-1 ). The results revealed that different substitutions (3a-3e) had different effects on root and shoot elongation. Silatranes (3a-3e) were synthesized employing microwave irradiation by a solvent-mediated transesterification reaction, thereby reducing reaction times from several hours under conventional reflux conditions to 15 min under microwave irradiation.; Results: It was of interest that the effect of these silatranes did not show a dose-dependent relationship but an optimum concentration, which was 100 µmol L-1 for maize and 200 µmol L-1 for wheat. γ-Aminopropyl silatranes (3b and 3e) gave the best results in maize, whereas γ-chloropropyl silatrane (3a) was most efficient for wheat at these optimum concentrations.; Conclusion: All the synthesized silatranes were effective in promoting root and shoot growth of wheat and maize. Furthermore, an efficient green microwave methodology was successful for the synthesis of silatranes. These observations pave the way for silatranes as efficient plant growth regulators for crops. © 2018 Society of Chemical Industry.; © 2018 Society of Chemical Industry.

Four compositions of TiCN-WC-Ni/Co cermets with or without TaC were prepared by pressureless sintering of respective powders, and unlubricated sliding wear behavior against bearing grade steel ball was studied at 5, 10, or 20 N load. Maximum hardness and fracture toughness were obtained for Ti(CN)-5WC-10Ni-10Co-5TaC (in wt%) cermet. With change in the cermet composition and sliding load, coefficient of friction varied from 0.3 to 1.0 and wear rate varied from 3 × 10−7 to 7 × 10−7 mm3/Nm. The increased material transfer and formation of iron oxide-rich tribochemical layer were responsible for the reduction in friction and wear for Ti(CN)-5WC-10Ni-10Co-5TaC cermet.

Some novel benzimidazole-tethered 1,2,3-triazole derivatives (4a-r) were synthesized by a click reaction between 2-substituted 1-(prop-2-yn-1-yl)-1H-benzo[d]imidazole and in situ azide. The structures of the synthesized compounds were confirmed by spectroscopic studies (one- and two-dimensional nuclear magnetic resonance, Fourier transform infrared, and high-resolution mass spectra). The synthesized compounds were evaluated for their antidiabetic activity. Compounds 4a-r exhibited a good-to-moderate α-amylase and α-glucosidase inhibitory activity, with IC50 values ranging from 0.0410 to 0.0916 µmol/ml and 0.0146 to 0.0732 µmol/ml, respectively. Compounds 4e, 4g, and 4n were found to be most active. Furthermore, the binding conformation of the most active compounds was ascertained by docking studies.

Estrogen Receptor-β (ER-β), a tumor-suppressor in prostate cancer, is epigenetically repressed by hypermethylation of its promoter. DNA-methyltransferases (DNMTs), which catalyze the transfer of methyl-groups to CpG islands of gene promoters, are overactive in cancers and can be inhibited by DNMT-inhibitors to re-express the tumor suppressors. The FDA-approved nucleoside DNMT-inhibitors like 5-Azacytidine and 5-Aza-deoxycytidine carry notable concerns due to their off-target toxicity, therefore non-nucleoside DNMT inhibitors are desirable for prolonged epigenetic therapy. Disulfiram (DSF), an antabuse drug, inhibits DNMT and prevents proliferation of cells in prostate and other cancers, plausibly through the re-expression of tumor suppressors like ER-β. To increase the DNMT-inhibitory activity of DSF, its chemical scaffold was optimized and compound-339 was discovered as a doubly potent DSF-derivative with similar off-target toxicity. It potently and selectively inhibited cell proliferation of prostate cancer (PC3/DU145) cells in comparison to normal (non-cancer) cells by promoting cell-cycle arrest and apoptosis, accompanied with inhibition of total DNMT activity, and re-expression of ER-β (mRNA/protein). Bisulfite-sequencing of ER-β promoter revealed that compound-339 demethylated CpG sites more efficaciously than DSF, restoring near-normal methylation status of ER-β promoter. Compound-339 docked on to the MTase domain of DNMT1 with half the energy of DSF. In xenograft mice-model, the tumor volume regressed by 24% and 50% after treatment with DSF and compound-339, respectively, with increase in ER-β expression. Apparently both compounds inhibit prostate cancer cell proliferation by re-expressing the epigenetically repressed tumor-suppressor ER-β through inhibition of DNMT activity. Compound-339 presents a new lead for further study as an anti-prostate cancer agent. © 2015 Wiley Periodicals, Inc.

Fruit extract of Cupressus sempervirens (CS), which is used traditionally to treat Benign Prostatic Hyperplasia (BPH)-like urinary symptoms in patients, was scientifically validated for anti-BPH activity. The ethanolic fruit extract of CS inhibited proliferation of human BPH-stromal cells and the activity was localized to its chloroform-soluble, diterpene-rich fraction. Eight major diterpenes isolated from this fraction exhibited moderate to potent activity and the most active diterpene (labda-8(17),12,14-trien-19-oic acid) exhibited an IC50 of 37.5 μM (antiproliferative activity against human BPH-stromal cells). It significantly inhibited activation (phosphorylation) of Stat-3 in BPH-stromal cells and prevented transactivation of androgen sensitive KLK3/PSA and TMPRSS2 genes in LNCaP cells. Labda-8(17),12,14-trien-19-oic acid-rich CS fraction prevented prostatic hyperplasia in rat model and caused TUNEL labeling of stromal cells with lower expressions of IGF-I, TGF-s and PCNA, and bcl-2/bax ratio. Human BPH tissues exhibited precise lowering of stromal component after incubation in labda-8(17),12,14-trien-19-oic acid, ex vivo. We conclude that labda-8(17),12,14-trien-19-oic acid contained in CS exhibits anti-BPH activity through inhibition of stromal proliferation and suppression of androgen action in the prostate, presenting a unique lead structure for further optimization of anti-BPH activity. Copyright © 2014 John Wiley & Sons, Ltd.

Readily accessible pyrazolylchalcones (III) suffer an iodine-mediated cyclization in DMSO leading to the title compounds (IV) in almost quantitative yield.

1-Azido-2-nitro-2-azapropane (1) was synthesized in high yield from 1-chloro-2-nitro-2-azapropane and sodium azide. 1-Nitrotetrazolato-2-nitro-2-azapropane (2) was synthesized in high yield from 1-chloro-2-nitro-2-azapropane and silver nitrotetrazolate. The highly energetic new compounds (1 and 2) were characterized using vibrational (IR and Raman) and multinuclear NMR spectroscopy (1H, 13C, 14N), elemental analysis and low-temperature single crystal X-ray diffraction. 1-Azido-2-nitro-2-azapropane (1) represents a covalently bound liquid energetic material which contains both a nitramine unit and an azide group in the molecule. 1-Nitrotetrazolato-2-nitro-2-azapropane (2) is a covalently bound room-temperature stable solid which contains a nitramine group and a nitrotetrazolate ring unit in the molecule. Compounds 1 and 2 are hydrolytically stable at ambient conditions. The impact sensitivity of compound 1 is very high (

The aim of this study was to describe the incidence of cardiac chamber collapse assessed by echocardiography and explore possible mechanisms in a clinical population of 116 patients with pleural effusion in the absence of pericardial effusion. We found that the frequency of chamber collapse was 18% in patients with pleural effusion in the absence of pericardial effusion, thus cardiac chamber collapse occurs in patients with pleural effusion. (ECHOCARDIOGRAPHY, Volume 20, April 2003)

A series of novel symmetrically (II) as well as unsymmetrically (VI) diaryl-substituted 1H-naphtho[1,2-e][1,3]oxazines are synthesized and screened for their antimicrobial and cytotoxic activities.