Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 11, Pages 3453-3456Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm9004303
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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.
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