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 journalArticlepeer-review

30 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
Externally publishedYes

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

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