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J Med Chem. 2009 Jun 11;52(11):3453-6. doi: 10.1021/jm9004303.

Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties.

Author information

1
IRBM/Merck Research Laboratories, Pomezia, Italy. olaf_kinzel@merck.com

Abstract

The optimization of a potent, class I selective ketone HDAC inhibitor is shown. It possesses optimized pharmacokinetic properties in preclinical species, has a clean off-target profile, and is negative in a microbial mutagenicity (Ames) test. In a mouse xenograft model it shows efficacy comparable to that of vorinostat at a 10-fold reduced dose.

PMID:
19441846
DOI:
10.1021/jm9004303
[Indexed for MEDLINE]

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