A series of benzohydrazide derivatives as novel ribosomal S6 kinase 2 （RSK2） inhibitors were designed and synthesized from a hit compound previously discovered by ligand-based virtual screening. Biological assays sh...A series of benzohydrazide derivatives as novel ribosomal S6 kinase 2 （RSK2） inhibitors were designed and synthesized from a hit compound previously discovered by ligand-based virtual screening. Biological assays showed that these compounds possessed moderate inhibitory activities towards RSK2. The structural activity relationships （SAR） were elucidated by molecular docking and further optimization was performed.展开更多
基金The Fundamental Research Funds for the Central Universitiesthe National Natural Science Foundation of China(Grants No.21173076,81102375and81102420)+3 种基金the Specialized Research Fund for the Doctoral Program of Higher Education of China(Grants No.20090074120012 and 20110074120009)the Shanghai Committee of Science and Technology(Grants No.11DZ2260600 and 10431902600)the Innovation Program of Shanghai Municipal Education Commission(Grant No.10ZZ41)the 863 Hi-Tech Program of China(Grant No.2012AA020308)
文摘A series of benzohydrazide derivatives as novel ribosomal S6 kinase 2 （RSK2） inhibitors were designed and synthesized from a hit compound previously discovered by ligand-based virtual screening. Biological assays showed that these compounds possessed moderate inhibitory activities towards RSK2. The structural activity relationships （SAR） were elucidated by molecular docking and further optimization was performed.
