Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.

@article{Yao2017DesignAS,
  title={Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.},
  author={Lianbin Yao and Nurulhuda Mustafa and Eng Chong Tan and Anders Poulsen and Prachi Singh and Minh-Dao Duong-Thi and Jeannie T Lee and Pondy Murugappan Ramanujulu and Wee Joo Chng and Jeffrey Jong-Young Yen and Sten Ohlson and Brian W Dymock},
  journal={Journal of medicinal chemistry},
  year={2017},
  volume={60 20},
  pages={8336-8357}
}
Concomitant inhibition of multiple oncogenic pathways is a desirable goal in cancer therapy. To achieve such an outcome with a single molecule would simplify treatment regimes. Herein the core features of ruxolitinib (1), a marketed JAK1/2 inhibitor, have been merged with the HDAC inhibitor vorinostat (2), leading to new molecules that are bispecific… CONTINUE READING