436151-27-8Relevant academic research and scientific papers
Flexible and Chemoselective Oxidation of Amides to α-Keto Amides and α-Hydroxy Amides
De La Torre, Aurélien,Kaiser, Daniel,Maulide, Nuno
, p. 6578 - 6581 (2017/05/29)
A suite of flexible and chemoselective methods for the transition-metal-free oxidation of amides to α-keto amides and α-hydroxy amides is presented. These highly valuable motifs are accessed in good to excellent yields and stereoselectivities with high functional group tolerance. The utility of the method is showcased by the formal synthesis of a potent histone deacetylase inhibitor.
α-Keto amides as inhibitors of histone deacetylase
Wada, Carol K.,Frey, Robin R.,Ji, Zhiqin,Curtin, Michael L.,Garland, Robert B.,Holms, James H.,Li, Junling,Pease, Lori J.,Guo, Jun,Glaser, Keith B.,Marcotte, Patrick A.,Richardson, Paul L.,Murphy, Shannon S.,Bouska, Jennifer J.,Tapang, Paul,Magoc, Terrance J.,Albert, Daniel H.,Davidsen, Steven K.,Michaelides, Michael R.
, p. 3331 - 3335 (2007/10/03)
α-Keto ester and amides were found to be potent inhibitors of histone deacetylase. Nanomolar inhibitors against the isolated enzyme and sub-micromolar inhibitors of cellular proliferation were obtained. The α-keto amide 30 also exhibited significant anti-tumor effects in an in vivo tumor model.
Inhibitors of histone deacetylase
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, (2008/06/13)
Substituted trifluoromethyl ketones, ketooxazoles, ketoamides, ketoesters, and diketones having the formula or therapeutically acceptable salts thereof, are histone deacetylase (HDAC) inhibitors. Preparation of the compounds, compositions containing the c
