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Synthesis and evaluation of thiopyrano[3,4-c]quinoline-9-carboxamide derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1) |
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| Authors: | Chun-Ho Park Kwangwoo Chun Bo-Young Joe Jong-Hee Choi Han-Chang Lee Il-Whea Ku Hyun Young Kim Seong-Ho Koh Goang Won Cho Seung Hyun Kim Myung-Hwa Kim |
| Affiliation: | 1. Drug Discovery Laboratory, R&D Center, Jeil Pharmaceutical Co., Ltd, 117-1, Keungok-Ri, Baekam-Myun, Cheoin-Gu, Yongin-City, Kyunggi-Do, 449-861, Republic of Korea 3. Graduate Program in Biomaterials Science and Engineering, Yonsei University, Seodaemun-Gu, Seoul, 120-740, Republic of Korea 2. Department of Neurology, Hanyang University College of Medicine, Seoul, Republic of Korea |
| Abstract: | A series of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors, 5-oxo-2,4,5,6-tetrahydro-1H-thiopyrano[3,4-c]quinoline-9-carboxamide derivatives, were successfully synthesized and their PARP-1 inhibitory activity was evaluated. These compounds were prepared from carboxylic acid 7 and the appropriate amines, and a number of the synthesized compounds were found to have significant PARP-1 activity. Among them, 9m showed potent activity in a PARP-1 enzymatic assay and cell-based assay (IC50?=?0.045?μM, ED50?=?0.54?μM). Molecular modeling studies confirmed the obtained biological results. |
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