Key result
Janus type nucleoside analogue 1a demonstrated potential for antiviral drug development with an in vitro HBV DNA replication inhibition IC50 of 10 μM and a selectivity index of 78.9.
Novel Janus type nucleoside analogue 1a demonstrates in vitro inhibition of HBV DNA replication, suggesting potential for antiviral drug development.
Supports preclinical development of Janus nucleosides for HBV; leaves open in vivo efficacy and clinical translation.
Novel Janus type nucleoside analogues 1a and 1b were synthesized in seven steps from 2-amino-4,6-dihydroxypyrimidine and 4,6-dihydroxypyrimidine. The base moiety of 1a has one face with a Watson-Crick donor-donor-acceptor (DDA) H-bond array of guanine and the other face with an acceptor-acceptor-donor (AAD) array of cytosine, which might lead to its base pairing with either cytosine or guanine due to the rotating of the glycosyl bond. This property may enable Janus type nucleoside analogues to act as an antiviral compound in a similar way to ribavirin. Both 1a and 1b were screened by a vitro HBV DNA replication inhibition test and indeed 1a showed a great potential with IC(50) = 10 μM and SI = 78.9 for antiviral drug development.
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Yang et al. (2010) studied HBV infection (in vitro). Janus type nucleoside analogues 1a and 1b was evaluated on in vitro HBV DNA replication inhibition (IC50 = 10 μM). Janus type nucleoside analogue 1a demonstrated potential for antiviral drug development with an in vitro HBV DNA replication inhibition IC50 of 10 μM and a selectivity index of 78.9.
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