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  • Title: Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.
    Author: Li YL, Litten C, Koehler KF, Mellström K, Garg N, Garcia Collazo AM, Färnegård M, Grynfarb M, Husman B, Sandberg J, Malm J.
    Journal: Bioorg Med Chem Lett; 2006 Feb 15; 16(4):884-6. PubMed ID: 16303304.
    Abstract:
    Based on the examination of the X-ray crystallographic structures of the LBD of TRalpha and TRbeta in complex with KB-141 (2), a number of novel 4'-hydroxy bioisosteric thyromimetics were prepared. Optimal affinity and beta-selectivity (33 times), was found with a medium-sized alkyl-substituted amido group; iso-butyl (12c). It can be concluded that bioisosteric replacements of the 4'-hydroxy position represent a new promising class of TRbeta-selective synthetic thyromimetics.
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