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HTS hit 7 was modified through hybrid design strategy to introduce a chiral side chain followed by introduction of Michael acceptor group to obtain potent EGFR kinase inhibitors 11 and 19. Both 11 and 19 showed over 3 orders of magnitude enhanced HCC827 antiproliferative activity compared to HTS hit 7 and also inhibited gefitinib-resistant double mutant (DM, T790M/L858R) EGFR kinase at nanomolar concentration. Moreover, treatment with 19 shrinked tumor in nude mice xenograft model.

Peptide-29 selected from biopanning may have clinical potential for HNSCC.

This article describes a theoretical model and computer program for calculating the pressure–volume ( PV ) diagram and the efficiency of an oil-injected screw compressor. The proposed model considers the mass and energy conservation laws, the heat transfer between air and oil, the leakages through various paths, and the discharges of air and oil. The proposed program, which uses seven empirical constants to account for the difference between the flow and the heat-transfer rates in the screw compressor and those estimated by available correlations, solves for the efficiency and the pressure curve of the compressed air. A systematic methodology for the determination of the seven empirical constants is presented in this article. Optimization is carried out to determine the seven empirical constants. With the empirical constants, which are determined with four sets of experiments, the maximum difference between the calculated and measured results in the training process, the verification process and the total process is 2.0 per cent for the volumetric and isentropic efficiencies and 5 per cent for the pressure curve. In the discharge process, the pressure in the compression chamber is noted to be affected by the area of the outlet port and the pressure in the neighbouring chambers.

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