Synthesis of isoquinolinone-based tetracycles as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors |
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| Authors: | Hee-Kyung Rhee So Yun Lim Mi-Ja Jung Youngjoo Kwon Myung-Hwa Kim Hea-Young Park Choo |
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| Affiliation: | aDepartment of Biological Science, Sookmyung Women’s University, Seoul 140-742, Republic of Korea;bCollege of Pharmacy and Division of Life and Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea;cR&D Center, Jeil Pharmaceutical Co. Ltd, Kyunggi-do 449-861, Republic of Korea |
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| 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. |
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| Keywords: | PARP-1 Isoquinolinone Cytotoxic potentiation |
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