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

Hee Kyung Rhee, So Yun Lim, Mi Ja Jung, Youngjoo Kwon, Myung Hwa Kim, Hea Young Park Choo

Research output: Contribution to journalArticlepeer-review

20 Scopus citations


The isoquinolinone-based tetracyclic compounds were designed and synthesized and their PARP-I 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.

Original languageEnglish
Pages (from-to)7537-7541
Number of pages5
JournalBioorganic and Medicinal Chemistry
Issue number21
StatePublished - 1 Nov 2009

Bibliographical note

Funding Information:
This investigation was supported by Jeil Pharmaceutical Co.


  • Cytotoxic potentiation
  • Isoquinolinone
  • PARP-1


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