You Li, Nicky Hwang, Andrew Snedeker, Stanley Lemon, Daisy Noe, Liren Sun, Jason A Clement, Tianlun Zhou, Liudi Tang, Timothy Block, Yanming Du
Dihydroquinolizinones (DHQs) that inhibit cellular polyadenylating polymerases 5 and 7 (PAPD5 & 7), such as RG7834, have been shown to inhibit hepatitis A and B virus (HAV, HBV) in vitro and in vivo. In this report, we describe RG7834-based Proteolysis Targeting Chimeras (PROTACs), such as compound 12b, (6S)-9-((1-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-21-oxo-3,6,9,12,15,18-hexaoxa-22-azapentacosan-25-yl)oxy)-6-isopropyl-10-methoxy-2-oxo-6,7-dihydro-2H-pyrido[2,1-a]isoquinoline-3-carboxylic acid...
February 28, 2024: Bioorganic & Medicinal Chemistry Letters