Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase.
Basic Information
ID: ALA1138134
Journal: Bioorg Med Chem Lett
Title: Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase.
Authors: Cockcroft XL, Dillon KJ, Dixon L, Drzewiecki J, Kerrigan F, Loh VM, Martin NM, Menear KA, Smith GC.
Abstract: We have previously described the discovery of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors based on a phthalazinone scaffold. Subsequent optimisation of inhibitory activity, metabolic stability and pharmacokinetic parameters has led to a novel series of meta-substituted 4-benzyl-2H-phthalazin-1-one PARP-1 inhibitors which retain low nM cellular activity and show good stability in vivo and efficacy in cell based models.
CiteXplore: 16290932
DOI: 10.1016/j.bmcl.2005.10.081
Patent ID: ┄