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Synthesis of isoquinolinone-based tetracycles as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors
- Authors
- Rhee, Hee-Kyung; Lim, So Yun; Jung, Mi-Ja; Kwon, Youngjoo; Kim, Myung-Hwa; Choo, Hea-Young Park
- Issue Date
- 1-Nov-2009
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- PARP-1; Isoquinolinone; Cytotoxic potentiation
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v.17, no.21, pp 7537 - 7541
- Pages
- 5
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- Volume
- 17
- Number
- 21
- Start Page
- 7537
- End Page
- 7541
- ISSN
- 0968-0896
1464-3391
- 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. (C) 2009 Elsevier Ltd. All rights reserved.
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