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Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1)
- Authors
- Park, Chun-Ho; Chun, Kwangwoo; Joe, Bo-Young; Park, Ji-Seon; Kim, Young-Chul; Choi, Ji-Soo; Ryu, Dong-Kyu; Koh, Seong-Ho; Cho, Goang Won; Kim, Seung Hyun; Kim, Myung-Hwa
- Issue Date
- Apr-2010
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Poly(ADP-ribose)polymerase PARP-1; Tricyclic derivatives
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.20, no.7, pp.2250 - 2253
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 20
- Number
- 7
- Start Page
- 2250
- End Page
- 2253
- ISSN
- 0960-894X
- Abstract
- Highly potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors, including 9-hydroxy-1,2-dihydro-4H-thiopyrano[ 3,4-c]quinolin-5(6H)-one derivatives with a non-aromatic A-ring, were synthesized. Among the derivatives, 12a showed low nanomolar enzyme and cellular activity (IC50 = 42 nM, ED50 = 220 nM) with good water solubility. Further, 12a exhibited microsomal stability in vitro and brain permeability in vivo.
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Related Researcher
- Koh, Seong-Ho
- COLLEGE OF MEDICINE (DEPARTMENT OF NEUROLOGY)