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Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1) |
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| Authors: | Giovanna Pescatore Danila Branca Fabrizio Fiore Olaf Kinzel Laura Llauger Bufi Ester Muraglia Federica Orvieto Michael Rowley Carlo Toniatti Caterina Torrisi Philip Jones |
| Affiliation: | IRBM/Merck Research Laboratories, Via Pontina km 30,600, 00040 Pomezia, Italy |
| Abstract: | Herein we describe the discovery of a novel series of pyrrolo[1,2-a]pyrazin-1(2H)-one PARP inhibitors. Optimization led to compounds that display excellent PARP-1 enzyme potency and inhibit the proliferation of BRCA deficient cells in the low double-digit nanomolar range showing excellent selectivity over BRCA proficient cancer cells. |
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