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Issue 5, 2020
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Synthesis and anti-HBV activity of carbocyclic nucleoside hybrids with salient features of entecavir and aristeromycin

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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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Supplementary files

Article information


Submitted
22 Feb 2020
Accepted
22 Apr 2020
First published
15 May 2020

RSC Med. Chem., 2020,11, 597-601
Article type
Research Article

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

R. Samunuri, M. Toyama, R. S. Pallaka, S. Neeladri, A. K. Jha, M. Baba and C. Bal, RSC Med. Chem., 2020, 11, 597 DOI: 10.1039/D0MD00059K

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