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

Autor: Orvieto F; IRBM - Merck Research Laboratories Rome, Via Pontina km 30,600, Pomezia, 00040 Rome, Italy. federica_orvieto@merck.com, Branca D, Giomini C, Jones P, Koch U, Ontoria JM, Palumbi MC, Rowley M, Toniatti C, Muraglia E
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Aug 01; Vol. 19 (15), pp. 4196-200. Date of Electronic Publication: 2009 Jun 02.
DOI: 10.1016/j.bmcl.2009.05.113
Abstrakt: 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.
Databáze: MEDLINE