Issue 5, 2020
From the journal:

RSC Medicinal Chemistry

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

Ramakrishnamraju Samunuri,ab   Masaaki Toyama,c   Renuka Sivasankar Pallaka,b   Seshubabu Neeladri,b   Ashok Kumar Jha,b   Masanori Babac  and  Chandralata Bal ORCID logo *a  

* Corresponding authors

a Department of Chemistry, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India
E-mail: cbal@bitmesra.ac.in

b Chemistry Services, GVK Biosciences Pvt. Ltd, IDA Nacharam, Hyderabad, India

c Division of Antiviral Chemotherapy, Joint Research Center for Human Retrovirus Infection, Kagoshima University, 8-35-1, Sakuragaoka, Kagoshima, Japan

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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Article information

DOI
https://doi.org/10.1039/D0MD00059K
Article type
Research Article
Submitted
22 Feb 2020
Accepted
22 Apr 2020
First published
15 May 2020

RSC Med. Chem., 2020,11, 597-601

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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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