Novel PARP-1 inhibitors based on a 2-propanoyl-3H-quinazolin-4-one scaffold

…, M Barbarino, MB Guglielmi, V Carollo, G Gallo…

Index: Giannini, Giuseppe; Battistuzzi, Gianfranco; Vesci, Loredana; Milazzo, Ferdinando M.; De Paolis, Francesca; Barbarino, Marcella; Guglielmi, Mario Berardino; Carollo, Valeria; Gallo, Grazia; Artali, Roberto; Dallavalle, Sabrina Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 2 p. 462 - 466

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Citation Number: 8

Abstract

Abstract Poly (ADP-ribose) polymerase-I (PARP-1) enzyme is involved in maintaining DNA integrity and programmed cell death. A virtual screening of commercial libraries led to the identification of five novel scaffolds with inhibitory profile in the low nanomolar range. A hit-to- lead optimization led to the identification of a group of new potent PARP-1 inhibitors, acyl- piperazinylamides of 3-(4-oxo-3, 4-dihydro-quinazolin-2-yl)-propionic acid. Molecular ...