Synthesis and evaluation of methylsulfonylnitrobenzamides (MSNBAs) as inhibitors of the thyroid hormone receptor-coactivator interaction.

@article{Hwang2013SynthesisAE,
  title={Synthesis and evaluation of methylsulfonylnitrobenzamides (MSNBAs) as inhibitors of the thyroid hormone receptor-coactivator interaction.},
  author={Jong Yeon Hwang and Ramy Attia and Angela K Carrillo and Michele C. Connelly and R. Kiplin Guy},
  journal={Bioorganic & medicinal chemistry letters},
  year={2013},
  volume={23 6},
  pages={1891-5}
}
We previously identified the methylsulfonylnitrobenzoates (MSNBs) that block the interaction of the thyroid hormone receptor with its obligate transcriptional coactivators and prevent thyroid hormone signaling. As part of our lead optimization work we demonstrated that sulfonylnitrophenylthiazoles (SNPTs), which replace the ester linkage of MSNBs with a thiazole, also inhibited coactivator binding to TR. Here we report that replacement of the ester with an amide (methylsulfonylnitrobenzamides… CONTINUE READING
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