TY - JOUR
T1 - Synthesis of substituted 5[H]phenanthridin-6-ones as potent poly(ADP-ribose)polymerase-1 (PARP1) inhibitors
AU - Li, Jia He
AU - Serdyuk, Larisa
AU - Ferraris, Dana V.
AU - Xiao, Ge
AU - Tays, Kevin L.
AU - Kletzly, Paul W.
AU - Li, Weixing
AU - Lautar, Susan
AU - Zhang, Jie
AU - Kalish, Vincent J.
PY - 2001/7/9
Y1 - 2001/7/9
N2 - 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.
AB - 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.
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U2 - 10.1016/S0960-894X(01)00281-5
DO - 10.1016/S0960-894X(01)00281-5
M3 - Article
C2 - 11425538
AN - SCOPUS:0035833028
SN - 0960-894X
VL - 11
SP - 1687
EP - 1690
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 13
ER -