Synthesis of substituted 5[H]phenanthridin-6-ones as potent poly(ADP-ribose)polymerase-1 (PARP1) inhibitors

Jia He Li, Larisa Serdyuk, Dana V. Ferraris, Ge Xiao, Kevin L. Tays, Paul W. Kletzly, Weixing Li, Susan Lautar, Jie Zhang, Vincent J. Kalish

Research output: Contribution to journalArticlepeer-review

51 Scopus citations


1-, 2-, 3-, 4-, 8-, or 10-Substituted 5(H)phenanthridin-6-ones were synthesized and found to be potent PARP1 inhibitors. Among the 28 compounds prepared, some showed not only low IC 50 values (compound 1b, 10 nM) but also desirable water solubility characteristics. These properties, which are superior to the common PARP1 inhibitors such as benzamides and isoquinolin-1-ones, are essential for potential therapeutic usage. The variety of compounds allows SAR analysis of favored substituents and substituted positions on 5(H)phenanthridin-6-one ring.

Original languageEnglish (US)
Pages (from-to)1687-1690
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number13
StatePublished - Jul 9 2001
Externally publishedYes

ASJC Scopus subject areas

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


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