| Literature DB >> 24900179 |
Stephen Hanessian1, Luciana Auzzas2, Andreas Larsson3, Jianbin Zhang1, Giuseppe Giannini4, Grazia Gallo4, Andrea Ciacci4, Walter Cabri4.
Abstract
The inhibitory activity of an ω-alkoxy analogue of the HDAC inhibitor, Vorinostat (SAHA), against the 11 isoforms of HDAC is described and evaluated with regard to structural biology information retrieved through computational methods. Preliminary absorption and metabolism studies were performed, which positioned this compound as a potential candidate for further preclinical studies and delineated measures for improving its pharmacokinetic profile.Entities:
Keywords: HDAC promiscuous inhibitors; HDAC1−11 profile; SAHA analogues; absorption and metabolism; class IIa-specific profile
Year: 2010 PMID: 24900179 PMCID: PMC4007911 DOI: 10.1021/ml100028g
Source DB: PubMed Journal: ACS Med Chem Lett ISSN: 1948-5875 Impact factor: 4.345