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Bioorg Med Chem Lett ; 17(19): 5300-9, 2007 Oct 01.
Article in English | MEDLINE | ID: mdl-17761416

ABSTRACT

This communication highlights the development of a nicotinamide series of histone deacetylase inhibitors within the benzamide structural class. Extensive exploration around the nicotinamide core led to the discovery of a class I selective HDAC inhibitor that possesses excellent intrinsic and cell-based potency, acceptable ancillary pharmacology, favorable pharmacokinetics, sustained pharmacodynamics in vitro, and achieves in vivo efficacy in an HCT116 xenograft model.


Subject(s)
6-Aminonicotinamide/analogs & derivatives , 6-Aminonicotinamide/pharmacology , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Histone Deacetylase Inhibitors , 6-Aminonicotinamide/chemical synthesis , Animals , Area Under Curve , Benzamides/chemistry , Biological Availability , Cell Line, Tumor , Cell Membrane Permeability/drug effects , Dogs , Drug Design , Drug Screening Assays, Antitumor , Enzyme Inhibitors/pharmacokinetics , Half-Life , Humans , Isoenzymes/antagonists & inhibitors , Models, Molecular , Neoplasm Transplantation , Protein Binding , Rats , Structure-Activity Relationship , Substrate Specificity
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