283173-02-4

Upstream product

• 74-89-5 methylamine 
• 283172-78-1 2-(4-(N,N-dimethylamino)methylphenyl)-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-one 
• 160320-11-6 3-(1-pivaloyl-1H-indol-3-yl)propanoic acid 
• 1028267-60-8 3-[1-(2,2-Dimethyl-propionyl)-1H-indol-3-yl]-propionyl chloride 
• 160320-10-5 1-(2,2-Dimethyl-propionyl)-3,4-dihydro-1H-benzo[cd]indol-5-one 
• 38073-22-2 3,4,5,6-tetrahydro-1H-azepino<5,4,3-cd>indol-6-one 
• 283173-72-8 2-bromo-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-one 
• 283173-74-0 4-(1-oxo-2,3,4,6-tetrahydro-1H-azepino[5,4,3-cd]indol-5-yl)benzaldehyde 
• 830-96-6 Indole-3-propionic acid 
• 98-80-6 phenylboronic acid 
• 283172-68-9 2-phenyl-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-one 

Relevant academic research and scientific papers

Poly(ADP-ribose) Polymerase in Neurodegeneration: Radiosynthesis and Radioligand Binding in ARC-SWE tg Mice

We report the synthesis, radiosynthesis, and characterization of a radioligand for poly(ADP-ribose) polymerase (PARP). PARP is of central importance in cell homeostasis, neuroplasticity, and neurodegeneration in the brain. A radiolabeled PARP inhibitor was developed and used for autoradiographic quantification of PARP protein concentration in wild-type and transgenic rodent brains ex vivo in high resolution. The binding of [3H]rucaparib was found to be confined to PARP-expressing domains, for example, cerebellar cortex or hippocampal regions in both models. Saturation binding experiments confirmed selective and reversible binding to a single site (Kd = 1.1 ± 0.2 nM).

Tricyclic inhibitors of poly(ADP-ribose) polymerases

Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapuetics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and nuerodegenerative disease. STR1As cancer therapuetics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.