Discovery and SAR of Thiazolidine-2,4-dione Analogues as Insulin-like Growth Factor-1 Receptor (IGF-1R) Inhibitors via Hierarchical Virtual Screening

摘要：

Insulin-like growth factor-1 receptor (IGF-1R) is a growth factor receptor tyrosine kinase acting as a critical mediator of cell proliferation and survival. Novel 5-benzylidenethiazolidine-2,4-dione (5) and 5(furan-2-ylmethylene)thiazolidine-2,4-dione (6) compounds were identified as potent and selective IGF-1R inhibitors via hierarchical virtual screening. Initial SAR and biological activity of the analogues of 5 and 6 with thiazolidine-2,4-dione template are presented, and several inhibitors with low nanomolar potency are reported.

作者: Xiaofeng Liu Hua Xie Cheng Luo Linjiang Tong Yi Wang Ting Peng Jian Ding Hualiang Jiang Honglin Li

作者单位: Drug Discovery and Design Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Division of Anti-Tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Ma Drug Discovery and Design Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science an

会议类型: 国际会议

会议名称: The 5th International Conference of Molecular Simulations and Applied Informatics Technologies(第五届国际分子模拟与信息技术应用学术会议 ICMS&I)

会议地点: 武汉

会议语种:英文

页码: 642-646

在线出版日期: 2010-09-01（万方平台首次上网日期，不代表论文的发表时间）