Based on our previous work,a series of hydrazone moiety-bearing aminopyrimidines were synthesized.The compounds were evaluated for inhibitory activities against EGFRT790M/L858 R and antiproliferative activities agains...Based on our previous work,a series of hydrazone moiety-bearing aminopyrimidines were synthesized.The compounds were evaluated for inhibitory activities against EGFRT790M/L858 R and antiproliferative activities against H1975 and A549 NSCLC cell lines harboring different forms of EGFR.Compounds 7f and7 k exhibited potent and selective activity in inhibition of gefitinib-resistant H1975 cancer cells(IC50;0.45,0.2μmol/L) while were much less active on A549 cancer cells(IC50;52.83,〉100μmol/L).Both compounds could be served as promising lead compounds for further investigation.展开更多
Purpose This study aimed to compare the effects of ground and treadmill running on energy metabolism and muscle con-tractile properties,providing a basis for the general public to choose running venues.Methods Ten mal...Purpose This study aimed to compare the effects of ground and treadmill running on energy metabolism and muscle con-tractile properties,providing a basis for the general public to choose running venues.Methods Ten male college students(age,20.10±1.53 years;height,176.20±5.49 cm;weight,72.14±8.25 kg;body fat percent,12.41%±4.65%)were recruited in this study.Energy expenditure(EE)was measured using the accelerometer(GT9X)combined with specific estimation equations.Average heart rate(HR)was measured using a heart rate band(Polar).Muscle contractile properties were assessed by measuring muscle displacement(Dm)and contraction velocity(Vc)using tensiomyography(TMG-S1).Blood glucose(Glu)and lactate(Lac)were measured by portable devices(eB-G and Lactate Scout).The running speed was 9 km/h and the duration was 25 min.Two-way ANOVA(protocol×time)was used to analyze the effect of running protocols on energy metabolism and muscle contractile properties.Results EE of treadmill running was significantly higher than EE of ground running(protocol main effect,P<0.001),and HR of treadmill running was significantly higher than that of ground running in the first testing time(protocol simple effect,P=0.026;protocol×time interaction P=0.043).The decrease in Dm of the rectus femoris after treadmill running was significantly higher than that of ground running(protocol main effect,P=0.009).The interaction of different running protocols and testing times on Lac was significant(P=0.025),but all results of the simple effects analysis were not statisti-cally significant(P>0.05).Conclusion Our study found a difference in energy expenditure between treadmill and ground running at 9 km/h with duration of 25 min.In addition,treadmills are more likely to cause a decrease in muscle displacement distance of the rectus femoris measured after exercise than ground running.Future studies are needed to further investigate whether the differences are induced by internal metabolism or the environmental conditions of running.展开更多
基金supported by grants from Science Foundation of Shenyang Pharmaceutical University(No.QNJJ2014502)
文摘Based on our previous work,a series of hydrazone moiety-bearing aminopyrimidines were synthesized.The compounds were evaluated for inhibitory activities against EGFRT790M/L858 R and antiproliferative activities against H1975 and A549 NSCLC cell lines harboring different forms of EGFR.Compounds 7f and7 k exhibited potent and selective activity in inhibition of gefitinib-resistant H1975 cancer cells(IC50;0.45,0.2μmol/L) while were much less active on A549 cancer cells(IC50;52.83,〉100μmol/L).Both compounds could be served as promising lead compounds for further investigation.
文摘Purpose This study aimed to compare the effects of ground and treadmill running on energy metabolism and muscle con-tractile properties,providing a basis for the general public to choose running venues.Methods Ten male college students(age,20.10±1.53 years;height,176.20±5.49 cm;weight,72.14±8.25 kg;body fat percent,12.41%±4.65%)were recruited in this study.Energy expenditure(EE)was measured using the accelerometer(GT9X)combined with specific estimation equations.Average heart rate(HR)was measured using a heart rate band(Polar).Muscle contractile properties were assessed by measuring muscle displacement(Dm)and contraction velocity(Vc)using tensiomyography(TMG-S1).Blood glucose(Glu)and lactate(Lac)were measured by portable devices(eB-G and Lactate Scout).The running speed was 9 km/h and the duration was 25 min.Two-way ANOVA(protocol×time)was used to analyze the effect of running protocols on energy metabolism and muscle contractile properties.Results EE of treadmill running was significantly higher than EE of ground running(protocol main effect,P<0.001),and HR of treadmill running was significantly higher than that of ground running in the first testing time(protocol simple effect,P=0.026;protocol×time interaction P=0.043).The decrease in Dm of the rectus femoris after treadmill running was significantly higher than that of ground running(protocol main effect,P=0.009).The interaction of different running protocols and testing times on Lac was significant(P=0.025),but all results of the simple effects analysis were not statisti-cally significant(P>0.05).Conclusion Our study found a difference in energy expenditure between treadmill and ground running at 9 km/h with duration of 25 min.In addition,treadmills are more likely to cause a decrease in muscle displacement distance of the rectus femoris measured after exercise than ground running.Future studies are needed to further investigate whether the differences are induced by internal metabolism or the environmental conditions of running.