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Dihydrofuro[3,4-c]pyridinones as inhibitors of the cytolytic effects of the pore-forming glycoprotein perforin.

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Lena G,Trapani JA,Sutton VR,Ciccone A,Browne KA,Smyth MJ,Denny WA,Spicer JA

doi

10.1021/jm801063n

subject

Has Abstract

pub_date

2008-12-11 00:00:00

pages

7614-24

issue

23

eissn

0022-2623

issn

1520-4804

journal_volume

51

pub_type

杂志文章

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