Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modeling.

@article{Ishida2006DiscoveryOP,
  title={Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modeling.},
  author={Junya Ishida and Hirofumi Yamamoto and Yoshiyuki Kido and Kazunori Kamijo and Kenji Murano and Hiroshi Miyake and Mitsuru Ohkubo and Takayoshi Kinoshita and Masaichi Warizaya and Akinori Iwashita and Kayoko Mihara and Nobuya Matsuoka and Kouji Hattori},
  journal={Bioorganic & medicinal chemistry},
  year={2006},
  volume={14 5},
  pages={1378-90}
}
We disclose herein our efforts aimed at discovery of selective PARP-1 and PARP-2 inhibitors. We have recently discovered several novel classes of quinazolinones, quinazolidinones, and quinoxalines as potent PARP-1 inhibitors, which may represent attractive therapeutic candidates. In PARP enzyme assays using recombinant PARP-1 and PARP-2, the quinazolinone derivatives displayed relatively high selectivity for PARP-1 and quinoxaline derivatives showed superior selectivity for PARP-2, and the… CONTINUE READING

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