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Elsevier, Bioorganic and Medicinal Chemistry Letters, 6(23), p. 1891-1895

DOI: 10.1016/j.bmcl.2012.12.055

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

Journal article published in 2013 by Jong Yeon Hwang, R. Kiplin Guy, Ramy R. Attia, Angela K. Carrillo, Michele C. Connelly, R. Kiplin Guy ORCID
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This paper is available in a repository.

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Abstract

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, MSNBA) also provides active TR antagonists.