2. Academic Validation
  3. Discovery and SAR of thiazolidine-2,4-dione analogues as insulin-like growth factor-1 receptor (IGF-1R) inhibitors via hierarchical virtual screening

Discovery and SAR of thiazolidine-2,4-dione analogues as insulin-like growth factor-1 receptor (IGF-1R) inhibitors via hierarchical virtual screening

  • J Med Chem. 2010 Mar 25;53(6):2661-5. doi: 10.1021/jm901798e.
Xiaofeng Liu 1,  Hua Xie,  Cheng Luo,  Linjiang Tong,  Yi Wang,  Ting Peng,  Jian Ding,  Hualiang Jiang,  Honglin Li
Affiliations

Affiliation

  • 1 Drug Discovery and Design Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
PMID: 20178321 DOI: 10.1021/jm901798e
Abstract

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.

Figures