Phytochemical investigation on the ethanol extract from the leaves of Aquitaria sinensis led to the isolation of five new benzophenone glycosides,aquilarinensides A-E（1-5）.Their structures were elucidated by a combi...Phytochemical investigation on the ethanol extract from the leaves of Aquitaria sinensis led to the isolation of five new benzophenone glycosides,aquilarinensides A-E（1-5）.Their structures were elucidated by a combination of 1D and 2D NMR,HRMS,and chemical analysis.展开更多
We report a functionalisation strategy which is able to generate Ricinus communis agglutinin 1 （RCA 120） modified PMMA microfluidic device for binding and culturing living cells. The functionalisation is achieved by...We report a functionalisation strategy which is able to generate Ricinus communis agglutinin 1 （RCA 120） modified PMMA microfluidic device for binding and culturing living cells. The functionalisation is achieved by standard aminealdehyde （Schiff base） reaction through the crosslinker, glutaraldehyde. To prove the ability of the RCA 120 modified PMMA surface, the PC 12 cell line （rat pheochromocytoma ceils） has been captured and cultured by the microfluidic device. In the presence of tunicamycin, the dose/timedependence on decreasing of binding affinity of RCA 120 modified device with PC 12 cell is also observed. The experimental results demonstrate that the lectin-functionalized microfluidic device can be employed as efficient cell culturing platform, and has a great promise of being used as a powerful tool for monitoring the interaction of drug with living cell.展开更多
The trend toward designing large hydrophobic molecules for lead optimization is often associated with poor drug-likeness and high attrition rates in drug discovery and development. Structural simplification is a power...The trend toward designing large hydrophobic molecules for lead optimization is often associated with poor drug-likeness and high attrition rates in drug discovery and development. Structural simplification is a powerful strategy for improving the efficiency and success rate of drug design by avoiding 'molecular obesity'. The structural simplification of large or complex lead compounds by truncating unnecessary groups can not only improve their synthetic accessibility but also improve their pharmacokinetic profiles, reduce side effects and so on. This review will summarize the application of structural simplification in lead optimization. Numerous case studies, particularly those involving successful examples leading to marketed drugs or drug-like candidates, will be introduced and analyzed to illustrate the design strategies and guidelines for structural simplification.展开更多
基金supported by the Special Program for New Drug Innovation of the Ministry of Science and Technology, China(Nos.2009ZX311-004,2009ZX0308-004)
文摘Phytochemical investigation on the ethanol extract from the leaves of Aquitaria sinensis led to the isolation of five new benzophenone glycosides,aquilarinensides A-E（1-5）.Their structures were elucidated by a combination of 1D and 2D NMR,HRMS,and chemical analysis.
基金supported by National Basic Research Program of China (2011CB935800)the Jilin Provincial Science and Technology Department (20100701)
文摘We report a functionalisation strategy which is able to generate Ricinus communis agglutinin 1 （RCA 120） modified PMMA microfluidic device for binding and culturing living cells. The functionalisation is achieved by standard aminealdehyde （Schiff base） reaction through the crosslinker, glutaraldehyde. To prove the ability of the RCA 120 modified PMMA surface, the PC 12 cell line （rat pheochromocytoma ceils） has been captured and cultured by the microfluidic device. In the presence of tunicamycin, the dose/timedependence on decreasing of binding affinity of RCA 120 modified device with PC 12 cell is also observed. The experimental results demonstrate that the lectin-functionalized microfluidic device can be employed as efficient cell culturing platform, and has a great promise of being used as a powerful tool for monitoring the interaction of drug with living cell.
基金supported by the National Natural Science Foundation of China (Grant No. 81725020 to Chunquan Sheng and No. 21602252 to Shengzheng Wang)the Innovation Program of Shanghai Municipal Education Commission (Grant No. 2019-0107-00-07-E00073 to Chunquan Sheng, China)the Hong Kong Scholars Program (Grant No. XJ201713 to Shengzheng Wang, China)
文摘The trend toward designing large hydrophobic molecules for lead optimization is often associated with poor drug-likeness and high attrition rates in drug discovery and development. Structural simplification is a powerful strategy for improving the efficiency and success rate of drug design by avoiding 'molecular obesity'. The structural simplification of large or complex lead compounds by truncating unnecessary groups can not only improve their synthetic accessibility but also improve their pharmacokinetic profiles, reduce side effects and so on. This review will summarize the application of structural simplification in lead optimization. Numerous case studies, particularly those involving successful examples leading to marketed drugs or drug-like candidates, will be introduced and analyzed to illustrate the design strategies and guidelines for structural simplification.
