Ionic liquids are viewed as green media for many engineering applications and exhibit exceptional properties, including negligible vapor pressure, null flammability, wide liquid range, and high thermal and chemical stabilities. We present new thermophysical properties of 1-alkyl-1-methylpyrrolidinium bis(trifluoromethylsulfonyl)imides ([C n C 1 pyr][NTf 2 ] with n = 3, 4) for future application them as heat-transfer media. The speed of sound was measured at pressures up to 100 MPa and at temperatures from 293 K to 318 K. The pρT, pC p T data, and derived thermophysical properties were determined using the acoustic method. TGA of [C n C 1 pyr][NTf 2 ] and cytotoxicity of [C n C 1 pyr][NTf 2 ] and their imidazolium counterparts ([C n C 1 im][NTf 2 ]) are investigated. The physicochemical properties of [C n C 1 pyr][NTf 2 ] are compared with those of [C n C 1 im][NTf 2 ] and commercial heat-transfer fluids (Therminol VP-1, Therminol 66, Marlotherm SH). [C 3 C 1 pyr][NTf 2 ] and [C 4 C 1 pyr][NTf 2 ] have a wide liquid range of ∼480 K and high decomposition onset temperatures of 771 and 776 K, respectively. [C n C 1 pyr][NTf 2 ] exhibit high energy storage density of ∼1.98 MJ m −3 K −1 , which is slightly dependent on temperature and pressure. The thermal conductivity of [C n C 1 pyr][NTf 2 ] is comparable to that of commercial heat-transfer fluids. [C n C 1 pyr][NTf 2 ] have lower toxicity for normal human dermal fibroblast cells than [C n C 1 im][NTf 2 ]. Thus, [C n C 1 pyr][NTf 2 ] are promising heat-transfer fluid candidates.
Thiosemicarbazones (TSCs) are an interesting class of ligands that show a diverse range of biological activity, including anti-fungal, anti-viral and anti-cancer effects. Our previous studies have demonstrated the potent in vivo anti-tumor activity of novel TSCs and their ability to overcome resistance to clinically used chemotherapeutics. In the current study, 35 novel TSCs of 6 different classes were designed using a combination of retro-fragments that appear in other TSCs. Additionally, di-substitution at the terminal N4 atom, which was previously identified to be critical for potent anti-cancer activity, was preserved through the incorporation of an N4-based piperazine or morpholine ring. The anti-proliferative activity of the novel TSCs were examined in a variety of cancer and normal cell-types. In particular, compounds 1d and 3c demonstrated the greatest promise as anti-cancer agents with potent and selective anti-proliferative activity. Structure-activity relationship studies revealed that the chelators that utilized “soft” donor atoms, such as nitrogen and sulfur, resulted in potent anti-cancer activity. Indeed, the N,N,S donor atom set was crucial for the formation of redox active iron complexes that were able to mediate the oxidation of ascorbate. This further highlights the important role of reactive oxygen species generation in mediating potent anti-cancer activity. Significantly, this study identified the potent and selective anti-cancer activity of 1d and 3c that warrants further examination.
The paper reports a new route for the fabrication and determination of physicochemical properties and biological activity, of metallic silica-based nanostructure (Ag/SiO2, Cu/SiO2).
Glioblastomas (GBMs) are high‐grade brain tumors, differentially driven by alterations (amplification, deletion or missense mutations) in the epidermal growth factor receptor (EGFR), that carry a poor prognosis of just 12–15 months following standard therapy. A combination of interventions targeting tumor‐specific cell surface regulators along with convergent downstream signaling pathways may enhance treatment efficacy. Against this background, we investigated a novel photoimmunotherapy approach combining the cytotoxicity of photodynamic therapy with the specificity of immunotherapy. An EGFR‐specific affibody (ZEGFR:03115) was conjugated to the phthalocyanine dye, IR700DX, which when excited with near‐infrared light produces a cytotoxic response. ZEGFR:03115–IR700DX EGFR‐specific binding was confirmed by flow cytometry and confocal microscopy. The conjugate showed effective targeting of EGFR positive GBM cells in the brain. The therapeutic potential of the conjugate was assessed both in vitro, in GBM cell lines and spheroids by the CellTiter‐Glo® assay, and in vivo using subcutaneous U87‐MGvIII xenografts. In addition, mice were imaged pre‐ and post‐PIT using the IVIS/Spectrum/CT to monitor treatment response. Binding of the conjugate correlated to the level of EGFR expression in GBM cell lines. The cell proliferation assay revealed a receptor‐dependent response between the tested cell lines. Inhibition of EGFRvIII+ve tumor growth was observed following administration of the immunoconjugate and irradiation. Importantly, this response was not seen in control tumors. In conclusion, the ZEGFR:03115–IR700DX showed specific uptake in vitro and enabled imaging of EGFR expression in the orthotopic brain tumor model. Moreover, the proof‐of‐concept in vivo PIT study demonstrated therapeutic efficacy of the conjugate in subcutaneous glioma xenografts.
One of the possible research directions for developing the modern energy sector is searching for innovative working fluids with exceptional properties, which leads to reducing energy consumption and the costs of the operation of the system. As a continuation of our investigations of ionic liquids (ILs) for their use as heat transfer fluids (HTFs), we present new thermophysical properties of 1). Speeds of sound were conducted in the temperature range 298−323 K and in the pressure range 0.1−76 MPa. The temperature and pressure dependence of densities, isobaric heat capacities, and related quantities were obtained by acoustic method. The viscosities, the TGA, and the cytotoxicities were also conducted. The thermal conductivities, energy storage densities, Prandtl numbers, isobaric heat capacities, viscosities, densities, isobaric thermal expansibilities, and isothermal and isentropic compressibilities of [C n MMIm][TFSI] are compared with those of 1-alkyl-3-methyl-1H-imidazol-3-ium bis[(trifluoromethyl)sulfonyl]azanides [C n MIm][TFSI], n = 2, 4) and 1-alkyl-1-methylpyrrolidinium bis[(trifluoromethyl)sulfonyl]azanides ([C n MPyr][TFSI], n = 3, 4), considered as good candidates as HTFs and commercial HTFs. The wide liquidity range (∼450 K), high decomposition onset temperature (∼763 K), significant energy storage density (∼1.95 × 10 6 J m −3 K −1 ) of [C 2 MMIm][TFSI] and [C 4 MMIm][TFSI] predestine them as heat transfer media in sustainable energy systems.
A group of styrylquinolines were synthesized and tested for their anti-proliferative activity. Anti-proliferative activity was evaluated against the human colon carcinoma cell lines that had a normal expression of the p53 protein (HCT116 p53+/+) and mutants with a disabled TP53 gene (HCT116 p53-/-) and against the GM 07492 normal human fibroblast cell line. A SAR study revealed the importance of Cl and OH as substituents in the styryl moiety. Several of the compounds that were tested were found to have a marked anti-proliferative activity that was similar to or better than doxorubicin and were more active against the p53 null than the wild type cells. The cellular localization tests and caspase activity assays suggest a mechanism of action through the mitochondrial pathway of apoptosis in a p53-independent manner. The activity of the styrylquinoline compounds may be associated with their DNA intercalating ability.
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