ChemInform Abstract: Synthesis and Evaluation of Tricyclic Derivatives Containing a Non‐Aromatic Amide as Poly(ADP‐ribose)polymerase‐1 (PARP‐1) Inhibitors.

Abstract

Amide as Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors. -The compounds (V) and (IX) are evaluated of their PARP-1 inhibitory activity. The compound (IXc) displays potent activity in a PARP-1 enzymatic assay and cell-based assay (IC50 = 0.142 μM, ED50 = 0.90 μM) with good water solubility. -(PARK, C.-H.; CHUN, K.; CHOI, J.-H.; JI, W.-K.; KIM, H. Y.; KIM, S. H.; HAN, G.; KIM*, M.-H.; Bull. Korean Chem.