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Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors |
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| Authors: | Federica Orvieto Danila Branca Claudia Giomini Philip Jones Uwe Koch Jesus M Ontoria Maria Cecilia Palumbi Michael Rowley Carlo Toniatti Ester Muraglia |
| Institution: | IRBM - Merck Research Laboratories Rome, Via Pontina km 30,600, Pomezia, 00040 Rome, Italy |
| Abstract: | A novel series of pyrazolo1,5-a]quinazolin-5(4H)-one derivatives proved to be a potent class of PARP-1 inhibitors. An extensive SAR around the 3-position of pyrazole in the scaffold led to the discovery of amides derivatives as low nanomolar PARP-1 inhibitors. |
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