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Poly(ADP-ribose)polymerase (PARP) is a significant therapeutic target for the treatment of numerous human diseases. Olaparib has been approved as a PARP inhibitor. In this paper, a series of new compounds were designed and synthesized with Olaparib as the lead compound. In order to evaluate the inhibitory activities against PARP1 of the synthesized compounds, in vitro PARP1 inhibition assay and intracellular PARylation assay were conducted. The results showed that the inhibitory activities of the derivatives were related to the type of substituent and the length of alkyl chain connecting the aromatic ring. 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT)-based assay also proved that these compounds demonstrating strong inhibition to PARP1 also have high anti-proliferative activities against BRCA2-deficient cell line (Capan-1). Analysis of the entire results suggest that compound 23 with desirable inhibitory efficiency may hold promise for further in vivo exploration of PARP inhibition.

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As for the once-through unit using lignite, in order to meet the AGC requirements of load change, the coordinated control strategy of unit was optimized. The control strategy was optimized mainly from the aspects of steam temperature control and steam pressure control. In order to control the mid-temperature stability, strategy of using feed water and coal to correct the mid-temperature at the same time was adopted, and the feed water flow was revised by desuperheating water. Different measures including variable parameter control of turbine, rapid coal adding to improve the main steam pressure, and feed-forward adjustment of primary air pressure were taken to improve the delay of main steam pressure, and also shortens the starting time of pressure when changing load. When the unit was put into AGC control, according to the different load changing characteristics of the two modes of BLO and BLR, the variable parameters of the coordinated feedforward of each subsystem were modified. And it is necessary to dynamically adjust the correction factor according to the load fluctuation, in order to reduce disturbance of important parameters such as furnace pressure, main steam pressure, main steam temperature, etc. The application results of the control strategy in the power plant show that the optimized control logic can meet the load regulation requirements of different AGC modes for the lignite burning unit, and the steam temperature and steam pressure control effect is good in the process.

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