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

Xiaofeng Liu | Zendy; Hua Xie | Zendy; Cheng Luo | Zendy; Linjiang Tong | Zendy; Yi Wang | Zendy; Ting Peng | Zendy; Jian Ding | Zendy; Hualiang Jiang | Zendy; Honglin Li | Zendy

Open Access

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

Author(s) -

Xiaofeng Liu,

Hua Xie,

Cheng Luo,

Linjiang Tong,

Yi Wang,

Ting Peng,

Jian Ding,

Hualiang Jiang,

Honglin Li

Publication year - 2010

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm901798e

Subject(s) - chemistry , thiazolidine , tyrosine kinase , insulin like growth factor , growth factor receptor , receptor tyrosine kinase , structure–activity relationship , receptor , growth factor , pharmacology , stereochemistry , biochemistry , combinatorial chemistry , in vitro , biology

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.

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