957828-45-4Relevant articles and documents
Thyroid receptor ligands. Part 4: 4′-amido bioisosteric ligands selective for the thyroid hormone receptor beta
Li, Yi-Lin,Litten, Chris,Koehler, Konrad F.,Mellstroem, Karin,Garg, Neeraj,Garcia Collazo, Ana Maria,Faernegard, Mathias,Grynfarb, Marlena,Husman, Bolette,Sandberg, Johnny,Malm, Johan
, p. 884 - 886 (2007/10/03)
Based on the examination of the X-ray crystallographic structures of the LBD of TRα and TRβ in complex with KB-141 (2), a number of novel 4′-hydroxy bioisosteric thyromimetics were prepared. Optimal affinity and β-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 TRβ-selective synthetic thyromimetics.