Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.

@article{Nguyen2002RationalDA,
  title={Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.},
  author={N N Nguyen and James W. Apriletti and Suzana T Cunha Lima and Paul D. Webb and J. D. Baxter and Thomas S. Scanlan},
  journal={Journal of medicinal chemistry},
  year={2002},
  volume={45 15},
  pages={3310-20}
}
Recent efforts have focused on the design and synthesis of thyroid hormone (T(3)) antagonists as potential therapeutic agents and chemical probes to understand hormone-signaling pathways. We previously reported the development of novel first-generation T(3) antagonists DIBRT, HY-4, and GC-14 using the "extension hypothesis" as a general guideline in hormone antagonist design.(1-3) These compounds contain extensions at the 5'-position (DIBRT, GC-14) of the outer thyronine ring or from the… CONTINUE READING

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