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1.
Synthesis and Biopharmaceutical Evaluation of Imatinib Analogues Featuring Unusual Structural Motifs 下载免费PDF全文
Prof. Kyriacos C. Nicolaou Dr. Dionisios Vourloumis Dr. Sotirios Totokotsopoulos Dr. Athanasios Papakyriakou Dr. Holger Karsunky Hanan Fernando Dr. Julia Gavrilyuk Dr. Damien Webb Dr. Antonia F. Stepan 《ChemMedChem》2016,11(1):31-37
A convenient synthesis of imatinib, a potent inhibitor of ABL1 kinase and widely prescribed drug for the treatment of a variety of leukemias, was devised and applied to the construction of a series of novel imatinib analogues featuring a number of non‐aromatic structural motifs in place of the parent molecule's phenyl moiety. These analogues were subsequently evaluated for their biopharmaceutical properties (e.g., ABL1 kinase inhibitory activity, cytotoxicity). The bicyclo[1.1.1]pentane‐ and cubane‐containing analogues were found to possess higher themodynamic solubility, whereas cubane‐ and cyclohexyl‐containing analogues exhibited the highest inhibitory activity against ABL1 kinase and the most potent cytotoxicity values against cancer cell lines K562 and SUP‐B15. Molecular modeling was employed to rationalize the weak activity of the compounds against ABL1 kinase, and it is likely that the observed cytotoxicity of these agents arises through off‐target effects. 相似文献
2.
Rao Y.J. Kalli K. Brady G. Webb D.J. Jackson D.A. Zhang L. Bennion I. 《Electronics letters》1995,31(12):1009-1010
A prototype fibre-optic system using interferometric wavelength-shift detection, capable of multiplexing up to 32 fibre-optic Bragg grating strain and temperature sensors with identical characteristics, has been demonstrated. This system is based on a spatially multiplexed scheme for use with fibre-based low-coherence interferometric sensors, reported previously. Four fibre-optic Bragg grating channels using the same fibre grating have been demonstrated for measuring quasi-static strain and temperature 相似文献
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Jinhong Shin Wyatt A. Winkenwerder Kyriacos Agapiou Gyeong S. Hwang 《Thin solid films》2007,515(13):5298-5307
Chemical vapor deposition growth of amorphous ruthenium-phosphorus films on SiO2 containing ∼ 15% phosphorus is reported. cis-Ruthenium(II)dihydridotetrakis-(trimethylphosphine), cis-RuH2(PMe3)4 (Me = CH3) was used at growth temperatures ranging from 525 to 575 K. Both Ru and P are zero-valent. The films are metastable, becoming increasingly more polycrystalline upon annealing to 775 and 975 K. Surface studies illustrate that demethylation is quite efficient near 560 K. Precursor adsorption at 135 K or 210 K and heating reveal the precursor undergoes a complex decomposition process in which the hydride and trimethylphosphine ligands are lost at temperatures as low at 280 K. Phosphorus and its manner of incorporation appear responsible for the amorphous-like character. Molecular dynamics simulations are presented to suggest the local structure in the films and the causes for phosphorus stabilizing the amorphous phase. 相似文献
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Kalli Sai Bhavani Tummala Anusha Pradeep Kumar Brahman 《International Journal of Hydrogen Energy》2021,46(13):9199-9214
In the present study, we report an eco-friendly and simple route to design and synthesize novel nanocomposite catalyst based on platinum nanoparticles anchored on binary support of graphitic carbon nitride (g-C3N4) and cobalt-metal-organic framework (ZIF-67). For this purpose, ZIF-67 was prepared by precipitation method and g-C3N4 was prepared through thermal polymerization method. Later, ZIF-67 and g-C3N4 were hybridized through sonication to get homogeneous g–C3N4–ZIF-67 nanocomposite support material. Platinum nanoparticles (PtNPs) were uniformly deposited on g–C3N4–ZIF-67 by an electrochemical method. The as-developed nanocatalyst was characterized by morphological, structural and electrochemical techniques. The electrocatalytic activity of PtNPs@g–C3N4–ZIF-67 nanocatalyst towards butanol oxidation was evaluated via CV, CA, LSV and EIS in an alkaline medium. Results revealed that the proposed catalyst showed greatly enhanced electrooxidation of butanol in terms of high magnificent current density, lower oxidation potential, excellent long-term stability, large surface area, low charge transfer resistance and less toxic ability. Enhanced catalytic performance of the proposed catalyst could be ascribed to the synergistic effect of g–C3N4–ZIF-67 nanocomposite and PtNPs. The PtNPs@g–C3N4–ZIF-67 catalyst holds promising potential applications to be used as an anodic electrocatalyst for the development of high-performance alkaline fuel cells. 相似文献
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The development of a coal pyrolysis reactor and a novel gas chromatography method for fast on-line composition analysis of pyrolysis products are presented. The annular fluidized bed reactor system minimizes particle agglomeration during the pyrolysis of plastic coals and the new column switching technique significantly reduces the time required for measuring the composition of low-volatile pyrolysis gases on a conventional gas chromatograph. Data from representative pyrolysis runs are presented and discussed. 相似文献
9.
The sequence distribution of the styrene crosslinks in a cured polyester formed from propylene glycol, terephthalic acid and maleic anhydride has been studied by 13C nuclear magnetic resonance and infrared spectroscopy. The n.m.r. method involved the degradation of the crosslinked polyester into a copolymer of styrene and fumaric acid and the interpretation of the peaks in the 13C spectrum, which arise from the quaternary phenyl carbon atoms in sequences of styrene units, by considering the 13C spectra of copolymer standards of styrene and diethyl fumarate. The crosslinking process was monitored directly by infra-red spectroscopy, and the distribution of sequence lengths of styrene units was then estimated by considering that crosslinking may be interpreted by a statistical treatment of copolymerization. Values of mol fractions of styrene units in sequences of monads, diads and triads determined by 13C n.m.r. and infra-red spectroscopy were in fair agreement. 相似文献
10.
S Kalli J Gr?nlund H Ihalainen A Siimes I V?lim?ki K Antila 《Computers and biomedical research》1988,21(6):512-530
The neonatal cardiovascular control system is a complicated interactive system which is under vigorous development at birth. From the measurement point of view the cardiovascular control is a closed-loop system. However, it can be examined on a beat-by-beat basis by analyzing circulatory-controlled variables with advanced signal analysis techniques. This paper proposes to use a multivariate autoregressive modeling technique in the analysis of several simultaneous physiological signals in order to examine interactions and inherent properties in the system. With the proposed multivariate autoregressive modeling technique, a signal is modeled as a linear combination of its own past and the past values of the other simultaneous signals plus a predictive error term of the model. The interactions in the system after the model identification are analyzed in frequency domain utilizing power spectrum estimates of the signals and signal contributions. The applicability of the proposed method was examined by a three-variable model between heart rate, blood pressure and respiration in the study of autonomic cardiovascular control in a chronic neonatal lamb model, in which the cardiovascular status was changed by using a beta-adrenergic autonomic nervous blockade. The study showed that the multivariate autoregressive modeling technique is a feasible technique in studying complicated interactions within the cardiovascular control system. 相似文献