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

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 super...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-07, Vol.11 (13), p.1687-1690
Hauptverfasser:	Li, Jia-He, Serdyuk, Larisa, Ferraris, Dana V., Xiao, Ge, Tays, Kevin L., Kletzly, Paul W., Li, Weixing, Lautar, Susan, Zhang, Jie, Kalish, Vincent J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Cardiovascular system Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Medical sciences Miscellaneous Pharmacology. Drug treatments Phenanthridines - chemical synthesis Phenanthridines - chemistry Phenanthridines - pharmacology Poly(ADP-ribose) Polymerase Inhibitors Structure-Activity Relationship
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