Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.

@article{Chen2013DesignAS,
  title={Design and synthesis of dual-action inhibitors targeting histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme A reductase for cancer treatment.},
  author={Jhih-Bin Chen and Ting-Rong Chern and Tzu-Tang Wei and C C Chen and Jung-Hsin Lin and Jim-Min Fang},
  journal={Journal of medicinal chemistry},
  year={2013},
  volume={56 9},
  pages={3645-55}
}
A series of dual-action compounds were designed to target histone deacetylase (HDAC) and 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) by having a hydroxamate group essential for chelation with the zinc ion in the active site of HDAC and the key structural elements of statin for binding with both proteins. In our study, the statin hydroxamic acids prepared by a fused strategy are most promising in cancer treatments. These compounds showed potent inhibitory activities against HDACs and… CONTINUE READING