Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.

@article{Sodji2013SynthesisAS,
  title={Synthesis and structure-activity relationship of 3-hydroxypyridine-2-thione-based histone deacetylase inhibitors.},
  author={Quaovi H Sodji and Vishal R. Patil and James Richard Kornacki and Milan Mrksich and Adegboyega K. Oyelere},
  journal={Journal of medicinal chemistry},
  year={2013},
  volume={56 24},
  pages={9969-81}
}
We previously identified 3-hydroxypyridine-2-thione (3HPT) as a novel zinc binding group for histone deacetylase (HDAC) inhibition. Early structure-activity relationship (SAR) studies led to various small molecules possessing selective inhibitory activity against HDAC6 or HDAC8 but devoid of HDAC1 inhibition. To delineate further the depth of the SAR of 3HPT-derived HDAC inhibitors (HDACi), we have extended the SAR studies to include the linker region and the surface recognition group to… CONTINUE READING

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