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81.
Shiou-Shiow Farn Yen-Buo Lai Kuo-Fong Hua Hsiang-Ping Chen Tzu-Yi Yu Sheng-Nan Lo Li-Hsin Shen Rong-Jiun Sheu Chung-Shan Yu 《Molecules (Basel, Switzerland)》2022,27(9)
A small fenbufen library comprising 18 compounds was prepared via Suzuki Miyara coupling. The five-step preparations deliver 9–17% biphenyl compounds in total yield. These fenbufen analogs exert insignificant activity against the IL-1 release as well as inhibiting cyclooxygenase 2 considerably. Both the para-amino and para-hydroxy mono substituents display the most substantial COX-2 inhibition, particularly the latter one showing a comparable activity as celecoxib. The most COX-2 selective and bioactive disubstituted compound encompasses one electron-withdrawing methyl and one electron-donating fluoro groups in one arene. COX-2 is selective but not COX-2 to bioactive compounds that contain both two electron-withdrawing groups; disubstituted analogs with both resonance-formable electron-donating dihydroxy groups display high COX-2 activity but inferior COX-2 selectivity. In silico simulation and modeling for three COX-2 active—p-fluoro, p-hydroxy and p-amino—fenbufens show a preferable docking to COX-2 than COX-1. The most stabilization by the p-hydroxy fenbufen with COX-2 predicted by theoretical simulation is consistent with its prominent COX-2 inhibition resulting from experiments. 相似文献
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Temperature dependent behavior of the responsivity of InAs/GaAs quantum dot infrared photodetectors was investigated with detailed measurement of the current gain. The current gain varied about two orders of magnitude with 100 K temperature change. Meanwhile, the change in quantum efficiency is within a factor of 10. The dramatic change of the current gain is explained by the repulsive coulomb potential of the extra carriers in the QDs. With the measured current gain, the extra carrier number in QDs was calculated. More than one electron per QD could be captured as the dark current increases at 150 K. The extra electrons in the QDs elevated the Fermi level and changed the quantum efficiency of the QDIPs. The temperature dependence of the responsivity was qualitatively explained with the extra electrons. 相似文献
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We present a numerical algorithm for pricing derivatives on electricity prices. The algorithm is based on approximating the generator of the underlying price process on a lattice of prices, resulting in an approximation of the stochastic process by a continuous time Markov chain. We numerically study the rate of convergence of the algorithm for the case of the Merton jump-diffusion model and apply the algorithm to calculate prices and sensitivities of both European and Bermudan electricity derivatives when the underlying price follows a stochastic process which exhibits both fast mean-reversion and jumps of large magnitude. 相似文献
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