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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)
- Park, Chun-Ho;
- Chun, Kwangwoo;
- Joe, Bo-Young;
- Choi, Jong-Hee;
- Lee, Han-Chang;
- ... Kim, Hyun Young;
- ... Koh, Seong-Ho;
- ... Kim, Seung Hyun;
- 외 3명
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4Citations
SCOPUS
4초록
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.
키워드
Poly(ADP-ribose)polymerase; PARP-1 inhibitor; Thiopyranoquinoline derivatives; CELL-DEATH; DNA-DAMAGE; CHEMOPOTENTIATION; TEMOZOLOMIDE; DISCOVERY; DEPLETION; NAD(+); CANCER; POTENT; SITE
- 제목
- Synthesis and evaluation of thiopyrano[3,4-c]quinoline-9-carboxamide derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1)
- 저자
- 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
- 발행일
- 2012-08
- 유형
- Article
- 권
- 21
- 호
- 8
- 페이지
- 1533 ~ 1543
- 언어
- ENG
- 출판사
- SPRINGER
- 발행국가
- 미국
- 분량
- 11 페이지
- ISSN
- P 1054-2523