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The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Oct2007, Vol. 17 Issue 19, p5300-5309. 10p. - Publication Year :
- 2007
-
Abstract
- 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. [Copyright &y& Elsevier]
- Subjects :
- *NICOTINAMIDE
*AMIDES
*NIACIN
*HISTONE deacetylase
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 17
- Issue :
- 19
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 26570640
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.08.023