Novel fullerene derivatives as dual inhibitors of Hepatitis C virus NS5B polymerase and NS3/4A protease

Hiroki Kataoka; Tomoyuki Ohe; Kyoko Takahashi; Shigeo Nakamura; Tadahiko Mashino

doi:10.1016/j.bmcl.2016.08.086

Novel fullerene derivatives as dual inhibitors of Hepatitis C virus NS5B polymerase and NS3/4A protease

Hiroki Kataoka, Tomoyuki Ohe, Kyoko Takahashi, Shigeo Nakamura, Tadahiko Mashino

School of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

25 Citations (Scopus)

Abstract

We evaluated the Hepatitis C virus (HCV) NS5B polymerase and HCV NS3/4A protease inhibition activities of a new set of proline-type fullerene derivatives. All of the compounds had the potential to inhibit both the enzymes, indicating that the fullerene derivatives may be dual inhibitors against NS5B and NS3/4A and could be novel lead compounds for the treatment of HCV infections.

Original language	English
Pages (from-to)	4565-4567
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	26
Issue number	19
DOIs	https://doi.org/10.1016/j.bmcl.2016.08.086
Publication status	Published - 2016

Keywords

Fullerene
Hepatitis C virus (HCV)
NS3/4A protease
NS5B polymerase

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2016.08.086

Cite this

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title = "Novel fullerene derivatives as dual inhibitors of Hepatitis C virus NS5B polymerase and NS3/4A protease",

abstract = "We evaluated the Hepatitis C virus (HCV) NS5B polymerase and HCV NS3/4A protease inhibition activities of a new set of proline-type fullerene derivatives. All of the compounds had the potential to inhibit both the enzymes, indicating that the fullerene derivatives may be dual inhibitors against NS5B and NS3/4A and could be novel lead compounds for the treatment of HCV infections.",

keywords = "Fullerene, Hepatitis C virus (HCV), NS3/4A protease, NS5B polymerase",

author = "Hiroki Kataoka and Tomoyuki Ohe and Kyoko Takahashi and Shigeo Nakamura and Tadahiko Mashino",

note = "Funding Information: This work was supported by a Health Labor Sciences Research Grant from the Ministry of Health, Labor, and Welfare of Japan ( MHLW ) and by the Platform for Drug Discovery, Informatics, and Structural Life Science from the Ministry of Education, Culture, Sports, Science and Technology of Japan ( MEXT ). We thank Dr. Kumiko Shimotohno and Dr. Kunitada Shimotohno for their assistance and support in the preparation of NS5B polymerase. Publisher Copyright: {\textcopyright} 2016 Elsevier Ltd",

year = "2016",

doi = "10.1016/j.bmcl.2016.08.086",

language = "English",

volume = "26",

pages = "4565--4567",

journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Novel fullerene derivatives as dual inhibitors of Hepatitis C virus NS5B polymerase and NS3/4A protease

AU - Kataoka, Hiroki

AU - Ohe, Tomoyuki

AU - Takahashi, Kyoko

AU - Nakamura, Shigeo

AU - Mashino, Tadahiko

N1 - Funding Information: This work was supported by a Health Labor Sciences Research Grant from the Ministry of Health, Labor, and Welfare of Japan ( MHLW ) and by the Platform for Drug Discovery, Informatics, and Structural Life Science from the Ministry of Education, Culture, Sports, Science and Technology of Japan ( MEXT ). We thank Dr. Kumiko Shimotohno and Dr. Kunitada Shimotohno for their assistance and support in the preparation of NS5B polymerase. Publisher Copyright: © 2016 Elsevier Ltd

PY - 2016

Y1 - 2016

N2 - We evaluated the Hepatitis C virus (HCV) NS5B polymerase and HCV NS3/4A protease inhibition activities of a new set of proline-type fullerene derivatives. All of the compounds had the potential to inhibit both the enzymes, indicating that the fullerene derivatives may be dual inhibitors against NS5B and NS3/4A and could be novel lead compounds for the treatment of HCV infections.

AB - We evaluated the Hepatitis C virus (HCV) NS5B polymerase and HCV NS3/4A protease inhibition activities of a new set of proline-type fullerene derivatives. All of the compounds had the potential to inhibit both the enzymes, indicating that the fullerene derivatives may be dual inhibitors against NS5B and NS3/4A and could be novel lead compounds for the treatment of HCV infections.

KW - Fullerene

KW - Hepatitis C virus (HCV)

KW - NS3/4A protease

KW - NS5B polymerase

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AN - SCOPUS:84985998151

SN - 0960-894X

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EP - 4567

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 19

ER -

Novel fullerene derivatives as dual inhibitors of Hepatitis C virus NS5B polymerase and NS3/4A protease

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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