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Bioorg Med Chem Lett. 2006 Feb 15;16(4):1040-4. Epub 2005 Nov 15.

Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase.

Author information

1
KuDOS Pharmaceuticals Ltd 327 Cambridge Science Park, Milton Road, Cambridge, CB4 0WG, UK. xcockcroft@kudospharma.co.uk

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.

PMID:
16290932
DOI:
10.1016/j.bmcl.2005.10.081
[Indexed for MEDLINE]

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