Novel inhibitors for p90 ribosomal S6 protein kinase 2:design,synthesis and SAR

作     者：薛梦竹 袁俊 吴彬 赵雪 刘晓峰 黄瑾 赵振江 李洪林 徐玉芳 

作者机构：华东理工大学药学院上海市新药设计重点实验室上海200237 华东理工大学药学院上海市化学生物学重点实验室上海200237 

基　　金：The Fundamental Research Funds for the Central Universities the National Natural Science Foundation of China(Grants No.21173076,81102375and81102420) 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) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2012年第21卷第5期

页      码：401-408页

摘      要：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.

主 题 词：RSK2 inhibitors Benzohydrazide derivatives SAR Molecular docking 

学科分类：1007[医学-药学类] 100701[100701] 10[医学] 

D　O　I：10.5246/jcps.2012.05.053

馆 藏 号：203196181...