Synthesis and evaluation of thiopyrano[3,4-c]quinoline-9-carboxamide derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1)
- Title
- Synthesis and evaluation of thiopyrano[3,4-c]quinoline-9-carboxamide derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1)
- Author
- 김승현
- Keywords
- Poly(ADP-ribose)polymerase; PARP-1 inhibitor; Thiopyranoquinoline derivatives; CELL-DEATH; DNA-DAMAGE; CHEMOPOTENTIATION; TEMOZOLOMIDE; DISCOVERY; DEPLETION; NAD(+); CANCER; POTENT; SITE
- Issue Date
- 2012-08
- Publisher
- SPRINGER
- Citation
- MEDICINAL CHEMISTRY RESEARCH,Vol.21,No.8,p1533-1543
- 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.
- URI
- https://link.springer.com/article/10.1007%2Fs00044-011-9673-6http://hdl.handle.net/20.500.11754/41097
- ISSN
- 1054-2523
- DOI
- 10.1007/s00044-011-9673-6
- Appears in Collections:
- COLLEGE OF MEDICINE[S](의과대학) > MEDICINE(의학과) > Articles
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