420846-57-7Relevant 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 (2007/10/03)
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.
PHTHALAZINONE DERIVATIVES
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Page/Page column 64-65, (2008/06/13)
A compound of formula (I); or an isomer, salt, solvate, chemically protected form, or prodrug thereof, wherein A and B together represent an optionally substituted, fused aromatic ring; RL is a C5-7aryl group substituted in the meta position by the group R2, and optionally further substituted; wherein R2 is selected from formula (II) and formula (III); and its use as a pharmaceutical, in particular for the treatment of diseases ameliorated by inhibiting the activity of PARP
