Author/Authors :
Yi-Lin Li، نويسنده , , Chris Litten، نويسنده , , Konrad F. Koehler، نويسنده , , Karin Mellstr?m، نويسنده , , Neeraj Garg، نويسنده , , Ana Maria Garcia Collazo، نويسنده , , Mathias F?rneg?rd، نويسنده , , Marlena Grynfarb، نويسنده , , Bolette Husman، نويسنده , , Johnny Sandberg، نويسنده , , Johan Malm، نويسنده ,
Abstract :
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.
