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971.
972.
973.
A novel and facile synthetic protocol for the construction of benzazepine and benzoxepine derivatives through a copper(I)‐catalyzed reaction of 2‐(2‐ethynylphenyl)‐1‐tosylaziridine or 2‐(2‐ethynylphenyl)oxirane with sulfonyl azides is disclosed. A ketenimine is the key intermediate during the reaction process. 相似文献
974.
Recently, thioredoxin reductase as a target for treatment of tumors has attracted the attention of scientists. 1,2‐[Bis(1,2‐benzisoselenazolone‐3(2 H)‐ketone)]ethane (ethaselen, BBSKE, PCT: CN02/00412), designed and synthesized previously, is an effective thioredoxin reductase inhibitor; presently it is in phase II clinical trials, targeting gastric cancer, lung cancer and colon cancer. To seek more novel and effective anticancer drugs, we have developed many selenazole‐based compounds. Evaluation of the thioredoxin reductase inhibitory effect and investigation of the mechanism of anticancer drugs require abundant thioredoxin reductase, but since commercial thioredoxin reductase is expensive its use is often limited. Therefore, the preparation of thioredoxin reductase is necessary. Base on the above investigation, in this work we have prepared thioredoxin reductase and evaluated selenazole‐based compounds, and found that 44 compounds have high inhibitory effect on thioredoxin reductase with IC50 < 10 µ m , of which 16 compounds have IC50 values below 1 µ m . This is helpful in investigating and elucidating the mechanism of this kind of compound. Copyright © 2012 John Wiley & Sons, Ltd. 相似文献
975.
Scanning deflectometric profilers based on an f–gθ system are typical optical tools used to measure mirror profiles at many synchrotron facilities. Unlike these profilers, which are based on a pencil beam, here a secondary light source and a pinhole are used to construct a system that automatically selects a beam that will always pass through the pinhole and propagate along the normal direction of the measured area on the surface under test. By measuring the angle variation of the selected beam, slope variations of the surface under test can be measured. Systematic errors introduced by manufacturing defects or aberrations of an optical element, which greatly degrade the performance of traditional profilers, could be minimized by using the developed method. Simulation values of the proposed method and a conventional method are compared. 相似文献
976.
977.
Graeme W. Carlile Robert A. Keyzers Katrina A. Teske Renaud Robert David E. Williams Roger G. Linington Christopher A. Gray Ryan M. Centko Luping Yan Suzana M. Anjos Heidi M. Sampson Donglei Zhang Jie Liao John W. Hanrahan Raymond J. Andersen David Y. Thomas 《Chemistry & biology》2012,19(10):1288-1299
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980.