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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)
- Authors
- Park, Chun-Ho; Chun, Kwangwoo; Joe, Bo-Young; Choi, Jong-Hee; Lee, Han-Chang; Ku, Il-Whea; Kim, Hyun Young; Koh, Seong-Ho; Cho, Goang Won; Kim, Seung Hyun; Kim, Myung-Hwa
- Issue Date
- Aug-2012
- Publisher
- Birkhaeuser
- Keywords
- Poly(ADP-ribose)polymerase; PARP-1 inhibitor; Thiopyranoquinoline derivatives
- Citation
- Medicinal Chemistry Research, v.21, no.8, pp 1533 - 1543
- Pages
- 11
- Indexed
- SCIE
SCOPUS
- Journal Title
- Medicinal Chemistry Research
- Volume
- 21
- Number
- 8
- Start Page
- 1533
- End Page
- 1543
- ISSN
- 1054-2523
1554-8120
- 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 mu M, ED50 = 0.54 mu M). Molecular modeling studies confirmed the obtained biological results.
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Related Researcher
- Kim, Seung Hyun
- 서울 의과대학 (DEPARTMENT OF NEUROLOGY)