☆ 4.7 Article

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

JOURNAL OF MEDICINAL CHEMISTRY (2010)

期刊

JOURNAL OF MEDICINAL CHEMISTRY

卷 53, 期 6, 页码 2661-2665

出版社

AMER CHEMICAL SOC

DOI: 10.1021/jm901798e

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类别

Chemistry, Medicinal

资金

National Natural Science Foundation of China [20803022, 30672539, 20721003]
863 Hi-Tech Program of China [2007AA02Z304]
Special Fund for Major State Basic Research Project [2009CB918500]
Shanghai Committee of Science and Technology [09dZ1975700, 08JC1407800]
National S&T Major Project, China [009ZX09501-001, 2009ZX-09301-001, 2009ZX09103-102]
Shanghai Rising-Star Program [10QA1401800]

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Protocol

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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 SA R 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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