46794-07-4Relevant academic research and scientific papers
Synthesis of substituted 5[H]phenanthridin-6-ones as potent poly(ADP-ribose)polymerase-1 (PARP1) inhibitors
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.
, p. 1687 - 1690 (2007/10/03)
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 IC50 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.
INVESTIGATION OF PHENANTHRIDONE AND DIOXOTETRAHYDRODIAZAPYRENE. 4. SYNTHESIS OF AMINO-SUBSTITUTED PHENANTHRIDONES and DIOXOTETRAHYDRODIAZAPYRENES
Migachev, G. I.,Terent'ev, A. M.
, p. 295 - 298 (2007/10/02)
The corresponding mono-, di-, and triamino derivatives substituted in the 2, 4, and 8 positions of the phenanthridone ring were obtained by reduction of mono-, di-, and trinitro-substituted phenanthridone (I), phenanthridone-10-carboxylic acid (II), phenanthridone-1-carboxylic acid (III), 4H-cyclopentaphenanthridine-5,9-dione (IV), 4H-cyclopentaphenanthridin-5-one (V), 5,10-dioxo-4,5,9,10-tetrahydro-4,9-diazapyrene(VI), and 5,9-dioxo-4,5,9,10-tetrahydro-4,10-diazapyrene (VII) with powdered iron in an electrolyte medium, with hydrogen in the presence of a nickel catalyst, or with stannous chloride.The 2,4,7,9-tetraamino derivative of VI was similarly obtained. 1-Amino, 7-amino-, and 10-aminophenanthridones were obtained by the Schmidt reaction from the corresponding carboxylic acids. 1,10-Diamino- and 3,8-diaminophenanthridones were similarly obtained from the corresponding aminofluorenones.
