Identification of substituted pyrazolo [1, 5-a] quinazolin-5 (4H)-one as potent poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors

F Orvieto, D Branca, C Giomini, P Jones, U Koch…

文献索引：Orvieto, Federica; Branca, Danila; Giomini, Claudia; Jones, Philip; Koch, Uwe; Ontoria, Jesus M.; Palumbi, Maria Cecilia; Rowley, Michael; Toniatti, Carlo; Muraglia, Ester Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 15 p. 4196 - 4200

全文：HTML全文

被引用次数: 31

摘要

A novel series of pyrazolo[1,5-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. ... Synthesis and SAR studies of a novel series of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one derivatives as potent class of PARP-1 inhibitors are reported. ... Structure of PARP-1 inhibitors. Structure of ...