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Novel phenothiazine-dithiocarbamate analogues were designed by molecular hybridization strategy and synthesized and evaluated for their anticancer activity in vitro against three selected cancer cell lines (EC-109, MGC-803, and PC-3). The preliminary structure-activity relationship (SAR) for this phenothiazine-dithiocarbamate hybrids is explored. Among all analogues, 2-oxo-2-(10H-phenothiazin-10-yl)ethyl 4-ethylpiperazine-1-carbodithioate (8a) showed the most potent inhibitory activity with an [Formula: see text] value of [Formula: see text] against PC-3 cells. In addition, compound 8a could arrest the cell cycle at the G1 phase and regulate the expression of G1 checkpoint-related proteins, suggesting that phenothiazine-dithiocarbamate hybrids might be useful as cell cycle blockers.

A series of 5,6-diaryl-1,2,4-triazines hybrids bearing a 1,2,3-triazole linker were synthesized by molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, EC-109 and PC-3). The first structure-activity relationship (SAR) for these 5,6-diaryl-1,2,4-triazines is explored in this report with evaluation of 15 variants of the structural class. Among these chemical derivatives, 3-(((1-(4-fluorobenzyl)-1H-1,2,3-triazol-4-yl)methyl)thio)-5,6-diphenyl-1,2,4-triazine (11E) showed the more potent inhibitory effect against three cell lines than 5-Fu. Cellular mechanism studies in MGC-803 cells elucidated 11E inhibited colony formation and arrested cell cycle at G2/M phase. Furthermore, compound 11E caused morphological changes, decreased mitochondrial membrane potential, and induced apoptosis through the apoptosis-related proteins in MGC-803 cells. It was the first time, to our knowledge, that 5,6-diaryl-1,2,4-triazines bearing a 1,2,3-triazole linker were used as potential apoptosis inducers.

A series of novel formononetin-dithiocarbamate derivatives were designed, synthesized and evaluated for antiproliferative activity against three selected cancer cell line (MGC-803, EC-109, PC-3). The first structure-activity relationship (SAR) for this formononetin-dithiocarbamate scaffold is explored in this report with evaluation of 14 variants of the structural class. Among these analogues, tert-butyl 4-(((3-((3-(4-methoxyphenyl)-4-oxo-4H-chromen-7-yl)oxy)propyl)thio)carbonothioyl)piperazine-1-carboxylate (8i) showed the best inhibitory activity against PC-3 cells (IC50 = 1.97 μM). Cellular mechanism studies elucidated 8i arrests cell cycle at G1 phase and regulates the expression of G1 checkpoint-related proteins in concentration-dependent manners. Furthermore, 8i could inhibit cell growth via MAPK signaling pathway and inhibit migration via Wnt pathway in PC-3 cells.

Guided by intergroup contact theory, this survey study investigates how White American adults' (N = 697 , Mage = 44.42, SD = 14.6, age range = 18 –67) social media intergroup expression frequency and valence, direct contact quality, and perceptions of institutional bias were associated with behavioral and affective attitudes toward ethnic Chinese during COVID-19. Structural Equation Modeling analyses indicate that social media intergroup expression valence and direct contact quality play a critical role in improving intergroup attitudes toward ethnic Chinese directly, and indirectly through building empathy and/or reducing anxiety. In addition, analyses demonstrate the negative role of social media intergroup expression frequency, which had: (1) a direct negative effect on behavioral attitudes and (2) an indirect negative effect on both attitudinal measures through increased anxiety and decreased empathy. Lastly, perceptions of institutional bias were negatively associated with affective attitudes through increased intergroup anxiety. Overall, findings reveal the dynamic interplay of the intergroup processes between social media intergroup expression, intergroup contact, and perceptions of institutional bias in shaping intergroup anxiety, empathy, and attitudes during COVID-19. [ABSTRACT FROM AUTHOR]

There is an emerging paradigm shift in oncology that seeks to emphasize molecularly targeted approaches for cancer prevention and therapy. Chalcones (1,3-diphenyl-2-propen-1-ones), naturally-occurring compounds with widespread distribution in spices, tea, beer, fruits and vegetables, consist of open-chain flavonoids in which the two aromatic rings are joined by a three-carbon α, β-unsaturated carbonyl system. Due to their structural diversity, relative ease of chemical manipulation and reaction of α, β-unsaturated carbonyl moiety with cysteine residues in proteins, some lead chalcones from both natural products and synthesis have been identified in a variety of screening assays for modulating important pathways or molecular targets in cancers. These pathways and targets that are affected by chalcones include MDM2/p53, tubulin, proteasome, NF-kappa B, TRIAL/death receptors and mitochondria mediated apoptotic pathways, cell cycle, STAT3, AP-1, NRF2, AR, ER, PPAR-γ and β-catenin/Wnt. Compared to current cancer targeted therapeutic drugs, chalcones have the advantages of being inexpensive, easily available and less toxic; the ease of synthesis of chalcones from substituted benzaldehydes and acetophenones also makes them an attractive drug scaffold. Therefore, this review is focused on molecular targets of chalcones and their potential implications in cancer prevention and therapy.

In order to enhance and toughen the polymer resin with hollow glass microspheres (HGM), polyurethane coating modification was carried out on HGM. The paper aims to explore the conditions and formulas of the physical coating and chemical coating. The physical method is to dissolve thermoplastic polyurethane elastomer in solvent and add HGM to prepare samples. In chemical method, HGM, alcohol component, and isocyanate component are added into solvent, and polymerization reaction is carried out under appropriate conditions to obtain samples. The coating effects and whether there was adhesion between the microspheres were observed through an optical microscope. The results showed that the polyurethane concentration of 4% was suitable for physical method. The reaction temperature of 80 °C is suitable for chemical method. The product synthesized by infrared spectroscopy was polyurethane, and the reaction time was 120 min according to the observation results of optical microscope. The effects of glycerol and toluene-2,4-diisocyanate (TDI) dosage on the thickness of the coating layer were explored through thermogravimetric analysis and optical microscope. This study provides a reference for the preparation of polyurethane-coated HGM 'soft-coated hard' core-shell structure, so that it can be used as a modifier to improve the comprehensive properties of resin. [ABSTRACT FROM AUTHOR]

Aberrant histone lysine methylation that is controlled by histone lysine methyltransferases (KMTs) and demethylases (KDMs) plays significant roles in carcinogenesis. Infections by tumor viruses or parasites and exposures to chemical carcinogens can modify the process of histone lysine methylation. Many KMTs and KDMs contribute to malignant transformation by regulating the expression of human telomerase reverse transcriptase (hTERT), forming a fused gene, interacting with proto-oncogenes or being up-regulated in cancer cells. In addition, histone lysine methylation participates in tumor suppressor gene inactivation during the early stages of carcinogenesis by regulating DNA methylation and/or by other DNA methylation independent mechanisms. Furthermore, recent genetic discoveries of many mutations in KMTs and KDMs in various types of cancers highlight their numerous roles in carcinogenesis and provide rare opportunities for selective and tumor-specific targeting of these enzymes. The study on global histone lysine methylation levels may also offer specific biomarkers for cancer detection, diagnosis and prognosis, as well as for genotoxic and non-genotoxic carcinogenic exposures and risk assessment. This review summarizes the role of histone lysine methylation in the process of cellular transformation and carcinogenesis, genetic alterations of KMTs and KDMs in different cancers and recent progress in discovery of small molecule inhibitors of these enzymes.

In this chapter, we focus on Communication Accommodation Theory (CAT)'s utility for analyzing one under-studied domain of intergroup communication, namely police-civilian encounters. By so doing, we focus on one aspect of institutional talk where a power imbalance is clearly evident. In addition to presenting recent self-report data relevant to this initiative, new intercultural data from China, Taiwan and the US, are also introduced. But first, we overview some important assumptions and concepts of the theory, interlaced with a selection of empirical research studies.

This experimental study, extending the communication accommodation theory and the Communication Predicament of Disability Model, examined people with disabilities' perceptions of four manipulated communication styles and tested the effects on their cognitive, emotional, and behavioral responses. Results revealed that participants in the integrative talk condition judged the coworker as the most competent and satisfying and had the least anxiety, followed by a relational talk, dismissive talk, and directive talk. Additionally, integrative talk resulted in the least internalized stigma and the highest likelihood of participants using accommodative response strategies, such as problem-solving and obliging. Furthermore, results revealed indirect effects of the communication styles on communication competence, satisfaction, stigma, and response strategies through communication anxiety. [ABSTRACT FROM AUTHOR]

From the perspectives of Saudi female journalists, the current study examined the predictive associations between gender discrimination, supervisor support, government support, and work-related outcomes (i.e., job stress and job satisfaction). Supporting our predictions, regression analyses results revealed that perceptions of gender discrimination were positively and perceptions of supervisor support were negatively associated with job stress. In addition, we found that perceptions of supervisor support and government support had positive associations with job satisfaction. Findings are discussed considering women's participation in the media industry in Saudi Arabia in relation to gender discrimination, supervisor and government support of women. [ABSTRACT FROM AUTHOR]