☆ 4.7 Article

Discovery of a Potent Class I Selective Ketone Histone Deacetylase Inhibitor with Antitumor Activity in Vivo and Optimized Pharmacokinetic Properties

JOURNAL OF MEDICINAL CHEMISTRY (2009)

期刊

JOURNAL OF MEDICINAL CHEMISTRY

卷 52, 期 11, 页码 3453-3456

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AMER CHEMICAL SOC

DOI: 10.1021/jm9004303

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Chemistry, Medicinal

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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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