A number of new compounds containing the 4-(aminomethyl)benzamide fragment as a linker were designed and synthesized, and their biological activities were evaluated as potential anticancer agents. The cytotoxicity activity of the designed compounds was studied in two hematological and five solid cell lines in comparison with the reference drugs. Targeted structures against eight receptor tyrosine kinases including EGFR, HER-2, HER-4, IGF1R, InsR, KDR, PDGFRa, and PDGFRb were investigated. The majority of the compounds showed a potent inhibitory activity against the tested kinases. The analogues 11 and 13 with the (trifluoromethyl)benzene ring in the amide or amine moiety of the molecule were proven to be highly potent against EGFR, with 91% and 92% inhibition at 10 nM, respectively. The docking of synthesized target compounds for nine protein kinases contained in the Protein Data Bank (PDB) database was carried out. The molecular modeling results for analogue 10 showed that the use of the 4-(aminomethyl)benzamide as a flexible linker leads to a favorable overall geometry of the molecule, which allows one to bypass the bulk isoleucine residue and provides the necessary binding to the active center of the T315I-mutant Abl (PDB: 3QRJ).
The problem of calculating the flexural deformation of the laminated core of the stator turbogenerator is examined. The evaluation of the effect of gluing the core sheets on its bending stiffness based on the compliance of the insulating cover sheet of active steel. An impact of pressing effort on the relative movement of the package of sheets is determined. An effect of wear of the insulating layer between sheets of laminated core on its reliability is determined. Conclusions are drawn on how to determine the possibility of extending the life of turbogenerators on the basis of the data obtained. References 8, Introduction. The economic condition of the country makes it impossible to perform the timely replacement of electrical equipment, which has worked on the technical specification operational time of the plant unit. Therefore, the period of its work can be extended only by means of modernization and/or partial replacement of major components. Modernization of turbogenerators (TG) is provided with the increase power in the installed overall dimensions, sometimes performed with replacement of refrigerant. Therefore, in the construction to be upgraded it is necessary to consider the accumulated experience of manufacturing and operation, to exclude all of the factors that lead to the destruction of the assembly machines and units, especially, a stator core, for reliability. Its destructions are the most frequent cause of crashes.TG reliability and durability are reduced due to a complex laminated core structure, vibration, electromagnetic continuous variables, thermal and mechanical loads. Due to the frequent destruction of the cores the researchers are looking for new design solutions for increasing operational reliability TG. The new design is based on the use of new materials and new techniques in the production of technology, on the knowledge of data exploitation and modern trends of development of the theory of the creation of turbogenerators [1][2][3].The aim of the article is to determine the effect of TG stator core assembly technology to its reliability and the definition of the possibility extending the service life (impact gluing the core sheets on its bending stiffness, impact of pressing forces on the relative movement of the package sheet and wear of the insulating layer between sheets of the laminated core).The main text of the article. The design quality of the laminated stator core determines its bending stiffness and consequently affects the value of the radial vibration and reliability. The works of many authors are devoted to these issues, [4][5][6][7][8], which also show the results of the research physical and mechanical properties of the insulating cover sheet steel. Also, the temperature coefficients of the materials that are used, static and dynamic loads; the presence, size, shape of ventilation ducts between packets impact on it.Consider the impact on the operational status of the core circuit stacking the stacked sheets and the quality of insulation coatings under the action of force...
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