Structural development studies of anti-hepatitis C virus agents with a phenanthridinone skeleton

Masahiko Nakamura; Atsushi Aoyama; Mohammed T.A. Salim; Mika Okamoto; Masanori Baba; Hiroyuki Miyachi; Yuichi Hashimoto; Hiroshi Aoyama

doi:10.1016/j.bmc.2010.02.057

Structural development studies of anti-hepatitis C virus agents with a phenanthridinone skeleton

Masahiko Nakamura, Atsushi Aoyama, Mohammed T.A. Salim, Mika Okamoto, Masanori Baba, Hiroyuki Miyachi, Yuichi Hashimoto, Hiroshi Aoyama

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

31 Citations (Scopus)

Abstract

A phenanthridinone skeleton was derived from our previous researches on thalidomide and retinoids as a multi-template for generation of anti-viral lead compounds. Structural development studies focusing on anti-hepatitis C virus activity afforded 5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenanthridin-6(5H)-one (10) and 5-butylbenzo[b]phenanthridin-6(5H)-one (39), which showed EC₅₀ values of approximately 3.7 and 3.2 μM, respectively.

Original language	English
Pages (from-to)	2402-2411
Number of pages	10
Journal	Bioorganic and Medicinal Chemistry
Volume	18
Issue number	7
DOIs	https://doi.org/10.1016/j.bmc.2010.02.057
Publication status	Published - Apr 1 2010
Externally published	Yes

Keywords

Am580
Am80
Anti-HCV agents
Phenanthridinone
Thalidomide

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.bmc.2010.02.057

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title = "Structural development studies of anti-hepatitis C virus agents with a phenanthridinone skeleton",

abstract = "A phenanthridinone skeleton was derived from our previous researches on thalidomide and retinoids as a multi-template for generation of anti-viral lead compounds. Structural development studies focusing on anti-hepatitis C virus activity afforded 5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenanthridin-6(5H)-one (10) and 5-butylbenzo[b]phenanthridin-6(5H)-one (39), which showed EC50 values of approximately 3.7 and 3.2 μM, respectively.",

keywords = "Am580, Am80, Anti-HCV agents, Phenanthridinone, Thalidomide",

author = "Masahiko Nakamura and Atsushi Aoyama and Salim, {Mohammed T.A.} and Mika Okamoto and Masanori Baba and Hiroyuki Miyachi and Yuichi Hashimoto and Hiroshi Aoyama",

note = "Funding Information: The work described in this paper was partially supported by Grants-in Aid for Scientific Research from the Science and Technology Incubation Program in Advanced Regions, Japan Science and Technology Agency (JST), Japan and The Ministry of Education, Culture, Sports, Science and Technology, Japan , and a Grant from the Japan Society for the Promotion of Science .",

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doi = "10.1016/j.bmc.2010.02.057",

language = "English",

volume = "18",

pages = "2402--2411",

journal = "Bioorganic and Medicinal Chemistry",

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T1 - Structural development studies of anti-hepatitis C virus agents with a phenanthridinone skeleton

AU - Nakamura, Masahiko

AU - Aoyama, Atsushi

AU - Salim, Mohammed T.A.

AU - Okamoto, Mika

AU - Baba, Masanori

AU - Miyachi, Hiroyuki

AU - Hashimoto, Yuichi

AU - Aoyama, Hiroshi

N1 - Funding Information: The work described in this paper was partially supported by Grants-in Aid for Scientific Research from the Science and Technology Incubation Program in Advanced Regions, Japan Science and Technology Agency (JST), Japan and The Ministry of Education, Culture, Sports, Science and Technology, Japan , and a Grant from the Japan Society for the Promotion of Science .

PY - 2010/4/1

Y1 - 2010/4/1

N2 - A phenanthridinone skeleton was derived from our previous researches on thalidomide and retinoids as a multi-template for generation of anti-viral lead compounds. Structural development studies focusing on anti-hepatitis C virus activity afforded 5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenanthridin-6(5H)-one (10) and 5-butylbenzo[b]phenanthridin-6(5H)-one (39), which showed EC50 values of approximately 3.7 and 3.2 μM, respectively.

AB - A phenanthridinone skeleton was derived from our previous researches on thalidomide and retinoids as a multi-template for generation of anti-viral lead compounds. Structural development studies focusing on anti-hepatitis C virus activity afforded 5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenanthridin-6(5H)-one (10) and 5-butylbenzo[b]phenanthridin-6(5H)-one (39), which showed EC50 values of approximately 3.7 and 3.2 μM, respectively.

KW - Am580

KW - Am80

KW - Anti-HCV agents

KW - Phenanthridinone

KW - Thalidomide

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DO - 10.1016/j.bmc.2010.02.057

M3 - Article

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SN - 0968-0896

VL - 18

SP - 2402

EP - 2411

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 7

ER -

Structural development studies of anti-hepatitis C virus agents with a phenanthridinone skeleton

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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