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41.
Myriam Gonzlez María Ovejero-Snchez Alba Vicente-Blzquez Raquel lvarez Ana B. Herrero Manuel Medarde Rogelio Gonzlez-Sarmiento Rafael Pelez 《International journal of molecular sciences》2021,22(4)
Pan-Gyn cancers entail 1 in 5 cancer cases worldwide, breast cancer being the most commonly diagnosed and responsible for most cancer deaths in women. The high incidence and mortality of these malignancies, together with the handicaps of taxanes—first-line treatments—turn the development of alternative therapeutics into an urgency. Taxanes exhibit low water solubility that require formulations that involve side effects. These drugs are often associated with dose-limiting toxicities and with the appearance of multi-drug resistance (MDR). Here, we propose targeting tubulin with compounds directed to the colchicine site, as their smaller size offer pharmacokinetic advantages and make them less prone to MDR efflux. We have prepared 52 new Microtubule Destabilizing Sulfonamides (MDS) that mostly avoid MDR-mediated resistance and with improved aqueous solubility. The most potent compounds, N-methyl-N-(3,4,5-trimethoxyphenyl-4-methylaminobenzenesulfonamide 38, N-methyl-N-(3,4,5-trimethoxyphenyl-4-methoxy-3-aminobenzenesulfonamide 42, and N-benzyl-N-(3,4,5-trimethoxyphenyl-4-methoxy-3-aminobenzenesulfonamide 45 show nanomolar antiproliferative potencies against ovarian, breast, and cervix carcinoma cells, similar or even better than paclitaxel. Compounds behave as tubulin-binding agents, causing an evident disruption of the microtubule network, in vitro Tubulin Polymerization Inhibition (TPI), and mitotic catastrophe followed by apoptosis. Our results suggest that these novel MDS may be promising alternatives to taxane-based chemotherapy in chemoresistant Pan-Gyn cancers. 相似文献
42.
Bican Osman Bayça Salih Uğur Kuleyin Hamdi Gümrük Recep 《Metal Science and Heat Treatment》2021,63(3-4):156-162
Metal Science and Heat Treatment - The effect of solid boronizing at 950°C for 2 and 4 h on the phase composition, microstructure, hardness and abrasive wear of steel AISI 304L is studied... 相似文献
43.
Real‐time monitoring by proton relaxometry of radical polymerization reactions of acrylamide in aqueous solution 下载免费PDF全文
Elton Jorge da Rocha Rodrigues Roberto Pinto Cucinelli Neto Pedro José Oliveira Sebastião Maria Inês Bruno Tavares 《Polymer International》2018,67(6):675-683
The potential of time‐domain nuclear magnetic resonance (TD‐NMR) for the real‐time monitoring of solution radical polymerizations is demonstrated. A model system composed of a redox‐pair initiator system, acrylamide as monomer and water as solvent was investigated. A second‐generation continuous wave free precession technique was employed to measure the longitudinal relaxation time constant (T1) of the samples throughout the polymerization reactions. This parameter was shown to be sensitive to the reactant feed free‐radical enhancement of the water molecule relaxation time, making it a good probe to monitor monomer conversion in real time in an automated, non‐destructive fashion. It was found that the T1 value was better than the transverse relaxation time constant (T2) for describing the evolution of the polymerization reactions, due to its greater sensitivity to paramagnetic effects. The TD‐NMR signal variation observed was linked to the formation, propagation and termination steps of the radical polymerization kinetics scheme. These first results may contribute to the application of real‐time monitoring of radical polymerization reactions employing low‐cost and robust TD‐NMR spectrometers. © 2018 Society of Chemical Industry 相似文献
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Mauro D. Santos Ivonne Delgadillo Jorge A. Saraiva 《International Journal of Food Science & Technology》2020,55(3):1171-1179
Hyperbaric storage (HS) was evaluated as a new food preservation methodology at room temperature (RT) for beef and pork meat, both minced and in pieces, and compared to refrigeration (RF) storage. The meat samples were stored at 50, 75 and 100 MPa and variable RT up to 60 days. HS at 75 and 100 MPa could not only inhibit microbial growth but also inactivate microorganisms. Regarding physicochemical analyses, an overall equal to better pH maintenance in HS samples was achieved, and similar colour differences between HS and RF were observed. Generally, similarities in moisture content and drip loss between HS (mostly 75 and 100 MPa) and RF were detected (tendency for lower values in the former and higher values in the latter for the higher pressure level). Protein solubility revealed a decrease of sarcoplasmic protein values during storage with a pressure level dependency in some samples. 相似文献
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María Clara Verdi Constanza Melian Patricia Castellano Graciela Vignolo Mariana Blanco Massani 《International Journal of Food Science & Technology》2020,55(1):267-275
The effectiveness of antimicrobial mixtures against Listeria innocua 7, used as a L. monocytogenes surrogate, was investigated in broth and a food system. Synergistic effects were found for nisin (Nis), potassium sorbate (PS), calcium propionate (CP) and sodium lactate (SL), Nis + PS being the most effective binary mixture that exhibited listericidal activity in broth. To assess the effect of adding lactocin AL705 (AL705) to Nis + organic acid salt combinations, tridimensional isobolograms were generated. Sub-MIC combinations of the antimicrobials exerted bactericidal activity against L. innocua 7 after AL705 addition to the binary mixtures. However, when applied on Sardo cheese contaminated with L. innocua 7 (initial inoculum 4.45 ± 0.06 CFU g−1), only Nis + PS + AL705 produced count reductions respect to the control, reaching 3.04 ± 0.35 CFU g−1 counts after 15 days at 15 °C. Ternary combinations containing AL705 showed potential to reduce antimicrobial usages for L. innocua 7 inhibition. 相似文献
50.
Application of high‐temperature Fenton oxidation for the treatment of sulfonation plant wastewater 下载免费PDF全文