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81.
Journal of Communications Technology and Electronics - Approximate formulas for calculating the coefficient of reflection from an artificial magnetic conductor (AMC) based on a capacitive lattice...  相似文献   
82.
Power Technology and Engineering - The monitoring of hydraulic structures as high-risk facilities is discussed. Monitoring should ensure the reliability and functioning of a hydraulic structure...  相似文献   
83.
Atomic Energy - The results of calculations and experimental determination of the neutronics characteristics of the IRT-T research reactor are presented. The IRT-T reactor is a pool reactor with...  相似文献   
84.
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   
85.
We deal with the mathematical model of the incremental degradation of the internal coating (e.g. a polymeric material) of a metallic pipe in which a fluid flows relatively fast. The fluid drags solid impurities so that longitudinal scratches, inaccessible to any direct inspection procedure, are produced on the coating. Time evolution of this kind of defects can be reconstructed from the knowledge of a sequence of temperature maps of the external surface. The time-varying orthogonal section of this damaged interface is determined as a function of time and polar angle through the identification of a suitable effective heat transfer coefficient by means of Thin Plate Approximation.  相似文献   
86.
Strength of Materials - The paper addresses the investigation of high-strain rate compressive behavior of Al foams subjected to impact at the intermediate striking velocity ranged from 40 to...  相似文献   
87.
88.
The failure of frontline antibiotics in the clinic is one of the most serious threats to human health and requires a multitude of novel therapeutics and innovative approaches to treatment so as to curtail the growing crisis. In addition to traditional resistance mechanisms resulting in the lack of efficacy of many antibiotics, most chronic and recurring infections are further made tolerant to antibiotic action by the presence of biofilms. Herein, we report an expanded set of 5-benzylidene-4-oxazolidinones that are able to inhibit the formation of Staphylococcus aureus biofilms, disperse preformed biofilms, and, in combination with common antibiotics, are able to significantly reduce the bacterial load in a robust collagen-matrix model of biofilm infection.  相似文献   
89.
90.
Potentiometric sensors with plasticized poly(vinyl chloride) membranes based on β-lactam–tetraalkylammonium ion associates sensitive to penicillin antibiotics are proposed. The physicochemical characteristics (solubility product constants and dissociation constants) of active membrane components and the electrode, transport, and selective properties of the membranes of liquidand solid-contact sensors have been studied. The quantitative characteristics of membrane transport (penetrability, ion flux, and transport rate) have been evaluated. The main charge carriers in the membranes and at the membrane/solution interface have been determined from the membrane transport characteristics. The potentiometric sensors are shown to be applicable to the determination of penicillin antibiotics in biological fluids (blood serum and oral fluid) from patients with urinary tract infection.  相似文献   
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