Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1)

Tricyclic PARP-1 inhibitor 12a (IC 50 = 42 nM) is reported. Highly potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors, including 9-hydroxy-1,2-dihydro-4 H-thiopyrano[3,4- c]quinolin-5(6 H)-one derivatives with a non-aromatic A-ring, were synthesized. Among the derivatives, 12a showed low nanomo...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2250-2253
Hauptverfasser:	Park, Chun-Ho, Chun, Kwangwoo, Joe, Bo-Young, Park, Ji-Seon, Kim, Young-Chul, Choi, Ji-Soo, Ryu, Dong-Kyu, Koh, Seong-Ho, Cho, Goang Won, Kim, Seung Hyun, Kim, Myung-Hwa
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemistry Amides - pharmacokinetics Amides - pharmacology Analytical, structural and metabolic biochemistry Animals Biological and medical sciences Brain - metabolism CHO Cells Cricetinae Cricetulus Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology Humans Medical sciences Microsomes, Liver - metabolism Miscellaneous Models, Molecular Pharmacology. Drug treatments Poly (ADP-Ribose) Polymerase-1 Poly(ADP-ribose) Polymerase Inhibitors Poly(ADP-ribose) Polymerases - chemistry Poly(ADP-ribose) Polymerases - metabolism Poly(ADP-ribose)polymerase PARP-1 Polycyclic Compounds - chemistry Polycyclic Compounds - pharmacokinetics Polycyclic Compounds - pharmacology Rats Structure-Activity Relationship Transferases Tricyclic derivatives
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