【文章名】Use of the Nitrile Oxide Cycloaddition (NOC) Reaction for Molecular Probe Generation: A New Class of Enzyme Selective Histone Deacetylase Inhibitors (HDACIs) Showing Picomolar Activity at HDAC6.
Use of the Nitrile Oxide Cycloaddition (NOC) Reaction for Molecular Probe Generation: A New Class of Enzyme Selective Histone Deacetylase Inhibitors (HDACIs) Showing Picomolar Activity at HDAC6.
作者
Kozikowski, Alan P.;Tapadar, Subhasish;Luchini, Doris N.;Kim, Ki Hwan;Billadeau, Daniel D.;
[摘要]：A series of hydroxamate based HDAC inhibitors contg. a phenylisoxazole as the CAP group has been synthesized using nitrile oxide cycloaddn. chem. An HDAC6 selective inhibitor having a potency of ~2 picomolar was identified. Some of the compds. were examd. for their ability to block pancreatic cancer cell growth and found to be about 10-fold more potent than SAHA (suberoylanilidehydroxamic acid). This research provides valuable, new mol. probes for use in exploring HDAC biol.
