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Your search keyword '"Elena S. Matyugina"' showing total 2 results
Start Over Author "Elena S. Matyugina" Publisher royal society of chemistry (rsc)
2 results on '"Elena S. Matyugina"'

1. 5′-Nor carbocyclic nucleosides: unusual nonnucleoside inhibitors of HIV-1 reverse transcriptase

Author

Vladimir T. Valuev-Elliston, Mikhail S. Novikov, Alexander V. Ivanov, Denis A. Babkov, Katherine L. Seley-Radtke, Jan Balzarini, Elena S. Matyugina, Sergey N. Kochetkov, and Anastasia L. Khandazhinskaya

Subjects
Pharmacology, chemistry.chemical_classification, biology, Chemistry, Stereochemistry, Organic Chemistry, Mutant, Human immunodeficiency virus (HIV), Pharmaceutical Science, Active site, medicine.disease_cause, Inhibitory postsynaptic potential, Biochemistry, Reverse transcriptase, Enzyme, Drug Discovery, biology.protein, medicine, 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.

Published
2013

2. Structure-activity evaluation of new uracil-based non-nucleoside inhibitors of HIV reverse transcriptase

Author

Elena S. Matyugina, Sergey N. Kochetkov, Vladimir T. Valuev-Elliston, Anastasia L. Khandazhinskaya, Alexander O. Chizhov, Alexander N. Geisman, Mikhail S. Novikov, and Katherine L. Seley-Radtke

Subjects
Pharmacology, Stereochemistry, Organic Chemistry, Mutant, Pharmaceutical Science, Uracil, Biochemistry, Reverse transcriptase, chemistry.chemical_compound, Residue (chemistry), chemistry, Drug Discovery, Benzyl group, Molecular Medicine, Linker, IC50, Nucleoside
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. Three different aspects of the scaffold were investigated: the effects of adding a linker between the carbocyclic and phenyl fragments, introduction of different substituents on the benzoyl residue and replacing the central carbocyclic ring with a benzyl group. Analogues of 2′,3′-dideoxy-2′,3′-didehydro-5′-nor-uridine, bearing 3,5-dichloro- or 3,5-dimethylbenzoyl groups, showed inhibitory activity against HIV-RT wild-type (IC50 5–10 μM) and mutants L100I (IC50 1.2–2.1 μM) and K103N (IC50 8–17 μM).

Published
2013

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