volume 23 issue 5 pages 1310-1314

Synthesis and biological evaluation of nucleoside analogues than contain silatrane on the basis of the structure of acyclovir (ACV) as novel inhibitors of hepatitis B virus (HBV)

Anyue Han 1
Lingna Li 1
Kuiyou Qing 1
Xiaolu Qi 1
Leping Hou 1
Xintong Luo 1
SHAOHUA SHI 1
Faqing Ye 1
Publication typeJournal Article
Publication date2013-03-01
scimago Q2
wos Q2
SJR0.472
CiteScore5.1
Impact factor2.2
ISSN0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
Hepatitis B virus (HBV) infection causes major public health problems worldwide. Acyclovir (ACV) is mainly used to inhibit herpes simplex virus (HSV) rather than HBV. In this study, we used the combination principle to design and synthesize nucleoside analogues that contain silatrane on the basis of the structure of ACV. We found that the compounds were effective inhibitors of HBV, both in vitro and in vivo. All of the compounds showed suppressive activity on the expression of HBV surface antigen (HBsAg) and HBV e antigen (HBeAg) in the HepG2.2.15 cell line with low cytotoxicity. One of compounds was studied in HBV transgenic mice model, and the test results showed its ability to reduce the levels of HBsAg, HBeAg and HBV DNA by ELASE and qPCR. Furthermore, significant improvement of T lymphocyte was observed after treatment, as evaluated by flow cytometry (FCM).
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GOST Copy
Han A. et al. Synthesis and biological evaluation of nucleoside analogues than contain silatrane on the basis of the structure of acyclovir (ACV) as novel inhibitors of hepatitis B virus (HBV) // Bioorganic and Medicinal Chemistry Letters. 2013. Vol. 23. No. 5. pp. 1310-1314.
GOST all authors (up to 50) Copy
Han A., Li L., Qing K., Qi X., Hou L., Luo X., SHI S., Ye F. Synthesis and biological evaluation of nucleoside analogues than contain silatrane on the basis of the structure of acyclovir (ACV) as novel inhibitors of hepatitis B virus (HBV) // Bioorganic and Medicinal Chemistry Letters. 2013. Vol. 23. No. 5. pp. 1310-1314.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/j.bmcl.2012.12.097
UR - https://doi.org/10.1016/j.bmcl.2012.12.097
TI - Synthesis and biological evaluation of nucleoside analogues than contain silatrane on the basis of the structure of acyclovir (ACV) as novel inhibitors of hepatitis B virus (HBV)
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Han, Anyue
AU - Li, Lingna
AU - Qing, Kuiyou
AU - Qi, Xiaolu
AU - Hou, Leping
AU - Luo, Xintong
AU - SHI, SHAOHUA
AU - Ye, Faqing
PY - 2013
DA - 2013/03/01
PB - Elsevier
SP - 1310-1314
IS - 5
VL - 23
PMID - 23369536
SN - 0960-894X
SN - 1464-3405
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2013_Han,
author = {Anyue Han and Lingna Li and Kuiyou Qing and Xiaolu Qi and Leping Hou and Xintong Luo and SHAOHUA SHI and Faqing Ye},
title = {Synthesis and biological evaluation of nucleoside analogues than contain silatrane on the basis of the structure of acyclovir (ACV) as novel inhibitors of hepatitis B virus (HBV)},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2013},
volume = {23},
publisher = {Elsevier},
month = {mar},
url = {https://doi.org/10.1016/j.bmcl.2012.12.097},
number = {5},
pages = {1310--1314},
doi = {10.1016/j.bmcl.2012.12.097}
}
MLA
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MLA Copy
Han, Anyue, et al. “Synthesis and biological evaluation of nucleoside analogues than contain silatrane on the basis of the structure of acyclovir (ACV) as novel inhibitors of hepatitis B virus (HBV).” Bioorganic and Medicinal Chemistry Letters, vol. 23, no. 5, Mar. 2013, pp. 1310-1314. https://doi.org/10.1016/j.bmcl.2012.12.097.