891263-91-5Relevant articles and documents
Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties
Kinzel, Olaf,Llauger-Bufi, Laura,Pescatore, Giovanna,Rowley, Michael,Schultz-Fademrecht, Carsten,Monteagudo, Edith,Fonsi, Massimiliano,Paz, Odalys Gonzalez,Fiore, Fabrizio,Steinkühler, Christian,Jones, Philip
supporting information; experimental part, p. 3453 - 3456 (2010/03/05)
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.
