Synthesis of isoquinolinone-based tetracycles as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors

  • Bioorg Med Chem. 2009 Nov 1;17(21):7537-41. doi: 10.1016/j.bmc.2009.09.014.
Hee-Kyung Rhee  1 ,  So Yun Lim ,  Mi-Ja Jung ,  Youngjoo Kwon ,  Myung-Hwa Kim ,  Hea-Young Park Choo
Affiliations
  • 1. Department of Biological Science, Sookmyung Women's University, Seoul, Republic of Korea.
PMID: 19800803 DOI: 10.1016/j.bmc.2009.09.014
Abstract

The isoquinolinone-based tetracyclic compounds were designed and synthesized and their PARP-1 inhibitory activity was evaluated. Most of synthesized compounds showed fairly good activity. Also the most active compound 6 showed its activity on potentiation of Anticancer agents, temozolamide and etoposide, by 1.7 times, respectively.