том 17 издание 1 страницы 43-52

Structure-activity relationship between (E)-5-(2-bromovinyl)- and 5-vinyl-1-β-d-arabinofuranosyluracil (BV-araU, V-araU) in inhibition of Epstein-Barr virus replication

Тип публикацииJournal Article
Дата публикации1992-01-01
scimago Q1
wos Q1
БС1
SJR1.195
CiteScore7.3
Impact factor4.0
ISSN01663542, 18729096
Pharmacology
Virology
Краткое описание
The structure-activity relationship between ( E )-5-(2-bromovinyl)- and 5-vinyl-1-β- d -arabinofuranosyluracil (BV-araU and V-araU) in inhibition of Epstein-Barr virus (EBV) was evaluated. Both V-araU and BV-araU effectively inhibited EBV replication in virus-producer P3HR-1(LS) cells, as determined by DNA-DNA hybridization. The 50% effective doses (ED 50 ) for viral DNA replication were 0.005 and 0.3 μM for V-araU and BV-araU, respectively. The in vitro therapeutic index was 4000 for V-araU and 1300 for BV-araU. Synthesis of EBV-induced polypeptides with molecular weights of 145000 (145, 140, 130, and 110 kDa) was significantly inhibited by both drugs. Only V-araU inhibited the synthesis of 85-, 55-, and 32-kDa polypeptides by approx. 50%. Kinetic analysis of inhibition and reversibility of EBV DNA replication after removal of the drugs indicated that BV-araU has a more prolonged inhibitory effect than V-araU. These results indicate that the substitution of H by Br in the 5-vinyl group results in marked reduction in anti-EBV activity while prolonging the drug effect and diminishing cytotoxicity.
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Lin J. T. et al. Structure-activity relationship between (E)-5-(2-bromovinyl)- and 5-vinyl-1-β-d-arabinofuranosyluracil (BV-araU, V-araU) in inhibition of Epstein-Barr virus replication // Antiviral Research. 1992. Vol. 17. No. 1. pp. 43-52.
ГОСТ со всеми авторами (до 50) Скопировать
Lin J. T., Reefschläger J., Herrmann G., Pagano J. S. Structure-activity relationship between (E)-5-(2-bromovinyl)- and 5-vinyl-1-β-d-arabinofuranosyluracil (BV-araU, V-araU) in inhibition of Epstein-Barr virus replication // Antiviral Research. 1992. Vol. 17. No. 1. pp. 43-52.
RIS |
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TY - JOUR
DO - 10.1016/0166-3542(92)90089-n
UR - https://doi.org/10.1016/0166-3542(92)90089-n
TI - Structure-activity relationship between (E)-5-(2-bromovinyl)- and 5-vinyl-1-β-d-arabinofuranosyluracil (BV-araU, V-araU) in inhibition of Epstein-Barr virus replication
T2 - Antiviral Research
AU - Lin, James T.
AU - Reefschläger, Jürgen
AU - Herrmann, Gottfried
AU - Pagano, Joseph S.
PY - 1992
DA - 1992/01/01
PB - Elsevier
SP - 43-52
IS - 1
VL - 17
PMID - 1310582
SN - 0166-3542
SN - 1872-9096
ER -
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@article{1992_Lin,
author = {James T. Lin and Jürgen Reefschläger and Gottfried Herrmann and Joseph S. Pagano},
title = {Structure-activity relationship between (E)-5-(2-bromovinyl)- and 5-vinyl-1-β-d-arabinofuranosyluracil (BV-araU, V-araU) in inhibition of Epstein-Barr virus replication},
journal = {Antiviral Research},
year = {1992},
volume = {17},
publisher = {Elsevier},
month = {jan},
url = {https://doi.org/10.1016/0166-3542(92)90089-n},
number = {1},
pages = {43--52},
doi = {10.1016/0166-3542(92)90089-n}
}
MLA
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Lin, James T., et al. “Structure-activity relationship between (E)-5-(2-bromovinyl)- and 5-vinyl-1-β-d-arabinofuranosyluracil (BV-araU, V-araU) in inhibition of Epstein-Barr virus replication.” Antiviral Research, vol. 17, no. 1, Jan. 1992, pp. 43-52. https://doi.org/10.1016/0166-3542(92)90089-n.