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

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

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-1Rinhibitors via hierarchical virtual screening. InitialSARand 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.