A New Class of High Affinity Thyromimetics Containing a Phenyl-Naphthylene Core

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4579-84. doi: 10.1016/j.bmcl.2005.06.093.

Abstract

High affinity thyromimetics containing a novel phenyl-naphthylene core are reported. The functionalized core is readily accessible via a Suzuki coupling protocol. Examples of this new class of TR ligands have sub-nanomolar binding affinities for the TRbeta receptor and low to modest selectivity for TRbeta. They also exhibit an SAR that diverges from other thyromimetics that are based on the diaryl ether core found in 3,5,3'-triiodothyronine.

MeSH terms

  • Models, Molecular
  • Naphthalenes / chemistry*
  • Receptors, Thyroid Hormone / metabolism*
  • Structure-Activity Relationship
  • Thyroid Hormones / chemistry
  • Thyroid Hormones / metabolism*

Substances

  • Naphthalenes
  • Receptors, Thyroid Hormone
  • Thyroid Hormones
  • phenyl-naphthylene