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Bioorg Med Chem Lett. 2007 Oct 1;17(19):5300-9. Epub 2007 Aug 16.

The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors.

Author information

1
Department of Drug Design and Optimization-Medicinal Chemistry, Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. christopher-hamblett@merck.com

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.

PMID:
17761416
DOI:
10.1016/j.bmcl.2007.08.023
[Indexed for MEDLINE]

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