Dihydrofuro[3,4-c]pyridinones as Inhibitors of the Cytolytic Effects of the Pore-Forming Glycoprotein Perforin

作者：Lena Gersande; Trapani Joseph A; Sutton Vivien R; Ciccone Annette; Browne Kylie A; Smyth Mark J; Denny William A; Spicer Julie A^*

来源：Journal of Medicinal Chemistry, 2008, 51(23): 7614-7624.

DOI：10.1021/jm801063n

Dihydrofuro[3,4-c]pyridinones are the first class of small molecules reported to inhibit the cytolytic effects of the lymphocyte toxin perforin. A lead structure was identified from a high throughput screen, and a series of analogues were designed and prepared to explore structure-activity relationships around the core bicyclic thioxofuropyridinone and pendant furan ring. This resulted in the identification of a submicromolar inhibitor of the perforin-induced lysis of Jurkat T-lymphoma cells.

• 出版日期2008-12-11