853650-63-2Relevant academic research and scientific papers
Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase
Loh Jr., Vincent M.,Cockcroft, Xiao-Ling,Dillon, Krystyna J.,Dixon, Lesley,Drzewiecki, Jan,Eversley, Penny J.,Gomez, Sylvie,Hoare, Janet,Kerrigan, Frank,Matthews, Ian T.W.,Menear, Keith A.,Martin, Niall M.B.,Newton, Roger F.,Paul, Jane,Smith, Graeme C.M.,Vile, Julia,Whittle, Alan J.
, p. 2235 - 2238 (2005)
Screening of the Maybridge compound collection identified 4-arylphthalazinones as micromolar inhibitors of PARP-1 catalytic activity. Subsequent optimisation of both inhibitory activity and metabolic stability led to a novel series of meta-substituted 4-benzyl-2H-phthalazin-1-ones with low nanomolar, cellular activity as PARP-1 inhibitors and promising metabolic stability in vitro.
