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Synthesis and anti-HBV activity of carbocyclic nucleoside hybrids with salient features of entecavir and aristeromycin†
Masaaki Toyama,Renuka Sivasankar Pallaka,Seshubabu Neeladri,Ashok Kumar Jha,Masanori Baba,Chandralata Bal
RSC Medicinal Chemistry Pub Date : 05/15/2020 00:00:00 , DOI:10.1039/D0MD00059K
Abstract

Modified carbocyclic nucleosides (4a–g) constituting 7-deazapurine, 4′-methyl, exocyclic double bond and 2′,3′-hydroxy were synthesized. NOE and X-ray studies of 4c confirmed the α-configuration of 4′-methyl. The anti-HBV assay demonstrated 4e (IC50 = 3.4 μM) without notable cytotoxicity (CC50 = 87.5 μM) as a promising lead for future exploration.

Graphical abstract: Synthesis and anti-HBV activity of carbocyclic nucleoside hybrids with salient features of entecavir and aristeromycin
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