Trifluoromethyl ketones as inhibitors of histone deacetylase
The synthesis and evaluation of a series of non-hydroxamate histone deacetylase (HDAC) inhibitors such as 16 (HDAC IC50 380 nM) is described.
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Acknowledgements
The authors wish to thank Kent Stewart for molecular modeling studies and Carole Goodfellow for assisting in pharmacokinetic characterization of these compounds.
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2018, Journal of Fluorine ChemistryCitation Excerpt :This bioisosteric property can be used to adjust the steric and electronic properties of a compound, or to prevent metabolic degradation [6]. A range of synthetic strategies are available for performing trifluoromethylation reactions [7], examples being the use of the Umemoto [8], Togni [9], Langlois [10], and Rupert-Prakash [11] reagents (Fig. 1). One approach to the direct trifluoromethylation of substrates involves the use of trifluoromethyl radical sources [12].