SAR by MS: discovery of a new class of RNA-binding small molecules for the hepatitis C virus: internal ribosome entry site IIA subdomain

…, EA Jefferson, KA Sannes-Lowery…

文献索引：Seth, Punit P.; Miyaji, Alycia; Jefferson, Elizabeth A.; Sannes-Lowery, Kristin A.; Osgood, Stephen A.; Propp, Stephanie S.; Ranken, Ray; Massire, Christian; Sampath, Rangarajan; Ecker, David J.; Swayze, Eric E.; Griffey, Richard H. Journal of Medicinal Chemistry, 2005 , vol. 48, # 23 p. 7099 - 7102

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被引用次数: 105

摘要

A new class of small molecules that bind the HCV RNA IRES IIA subdomain with sub- micromolar affinity is reported. The benzimidazole'hit'1 with a KD~ 100 μM to a 29-mer RNA model of Domain IIA was identified from a 180000-member library using mass spectrometry- based screening methods. Further MS-assisted SAR (structure-activity relationships) studies afforded benzimidazole derivatives with sub-micromolar binding affinity for the IIA RNA ...