5′-Nor carbocyclic nucleosides: unusual nonnucleoside inhibitors of HIV-1 reverse transcriptase
Elena Matyugina
1
,
A. A. Kushch
1
,
Denis A Babkov
2
,
Mikhail S. Novikov
2
,
А. В. Иванов
1
,
С. Н. Кочетков
1
,
Jan Balzarini
3
,
Publication type: Journal Article
Publication date: 2013-03-06
SJR: —
CiteScore: —
Impact factor: —
ISSN: 20402503, 20402511
Organic Chemistry
Drug Discovery
Biochemistry
Pharmacology
Pharmaceutical Science
Molecular Medicine
Abstract
A new series of potential nonnucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs) based on the carbocyclic 5′-nor-uracil scaffold were designed and synthesized. Binding modes in the active site of the enzyme were studied computationally to provide insight on potential interactions. Several of the 2′,3′-dideoxy-2′,3′-didehydro-5′-nor-uridine analogues showed inhibitory activity against wild-type and mutant (L100I) HIV-RT with Ki 13–18 μM and 1–11 μM, respectively.
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11
Total citations:
11
Citations from 2024:
1
(9%)
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MLA
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GOST
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Matyugina E. et al. 5′-Nor carbocyclic nucleosides: unusual nonnucleoside inhibitors of HIV-1 reverse transcriptase // MedChemComm. 2013. Vol. 4. No. 4. p. 741.
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Matyugina E., Kushch A. A., Babkov D. A., Novikov M. S., Иванов А. В., Кочетков С. Н., Balzarini J., Seley-Radtke K. L., Khandazhinskaya A. 5′-Nor carbocyclic nucleosides: unusual nonnucleoside inhibitors of HIV-1 reverse transcriptase // MedChemComm. 2013. Vol. 4. No. 4. p. 741.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1039/c3md00036b
UR - https://doi.org/10.1039/c3md00036b
TI - 5′-Nor carbocyclic nucleosides: unusual nonnucleoside inhibitors of HIV-1 reverse transcriptase
T2 - MedChemComm
AU - Matyugina, Elena
AU - Kushch, A. A.
AU - Babkov, Denis A
AU - Novikov, Mikhail S.
AU - Иванов, А. В.
AU - Кочетков, С. Н.
AU - Balzarini, Jan
AU - Seley-Radtke, Katherine L.
AU - Khandazhinskaya, Anastasia
PY - 2013
DA - 2013/03/06
PB - Royal Society of Chemistry (RSC)
SP - 741
IS - 4
VL - 4
SN - 2040-2503
SN - 2040-2511
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2013_Matyugina,
author = {Elena Matyugina and A. A. Kushch and Denis A Babkov and Mikhail S. Novikov and А. В. Иванов and С. Н. Кочетков and Jan Balzarini and Katherine L. Seley-Radtke and Anastasia Khandazhinskaya},
title = {5′-Nor carbocyclic nucleosides: unusual nonnucleoside inhibitors of HIV-1 reverse transcriptase},
journal = {MedChemComm},
year = {2013},
volume = {4},
publisher = {Royal Society of Chemistry (RSC)},
month = {mar},
url = {https://doi.org/10.1039/c3md00036b},
number = {4},
pages = {741},
doi = {10.1039/c3md00036b}
}
Cite this
MLA
Copy
Matyugina, Elena, et al. “5′-Nor carbocyclic nucleosides: unusual nonnucleoside inhibitors of HIV-1 reverse transcriptase.” MedChemComm, vol. 4, no. 4, Mar. 2013, p. 741. https://doi.org/10.1039/c3md00036b.