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 journalArticle

22 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 languageEnglish
Pages (from-to)2402-2411
Number of pages10
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number7
DOIs
Publication statusPublished - Apr 1 2010

Fingerprint

Lead compounds
Thalidomide
Retinoids
Viruses
Skeleton
Hepacivirus
Research
Lead

Keywords

  • Am580
  • Am80
  • Anti-HCV agents
  • Phenanthridinone
  • Thalidomide

ASJC Scopus subject areas

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

Cite this

Nakamura, M., Aoyama, A., Salim, M. T. A., Okamoto, M., Baba, M., Miyachi, H., ... Aoyama, H. (2010). Structural development studies of anti-hepatitis C virus agents with a phenanthridinone skeleton. Bioorganic and Medicinal Chemistry, 18(7), 2402-2411. https://doi.org/10.1016/j.bmc.2010.02.057

Structural development studies of anti-hepatitis C virus agents with a phenanthridinone skeleton. / Nakamura, Masahiko; Aoyama, Atsushi; Salim, Mohammed T A; Okamoto, Mika; Baba, Masanori; Miyachi, Hiroyuki; Hashimoto, Yuichi; Aoyama, Hiroshi.

In: Bioorganic and Medicinal Chemistry, Vol. 18, No. 7, 01.04.2010, p. 2402-2411.

Research output: Contribution to journalArticle

Nakamura, M, Aoyama, A, Salim, MTA, Okamoto, M, Baba, M, Miyachi, H, Hashimoto, Y & Aoyama, H 2010, 'Structural development studies of anti-hepatitis C virus agents with a phenanthridinone skeleton', Bioorganic and Medicinal Chemistry, vol. 18, no. 7, pp. 2402-2411. https://doi.org/10.1016/j.bmc.2010.02.057
Nakamura, Masahiko ; Aoyama, Atsushi ; Salim, Mohammed T A ; Okamoto, Mika ; Baba, Masanori ; Miyachi, Hiroyuki ; Hashimoto, Yuichi ; Aoyama, Hiroshi. / Structural development studies of anti-hepatitis C virus agents with a phenanthridinone skeleton. In: Bioorganic and Medicinal Chemistry. 2010 ; Vol. 18, No. 7. pp. 2402-2411.
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