| 17363258 |
Komatsu T, Hirano T, Songkram C, Kawachi E, Kagechika H: Novel thyroid hormone receptor antagonists with an N-alkylated diphenylamine skeleton. Bioorg Med Chem. 2007 May 1;15(9):3115-26. Epub 2007 Mar 3.
Thyroid hormones play important roles in growth, development and homeostasis, and disruption of their functions induces serious disease, so novel synthetic thyroid hormone analogues are candidates for clinical application. We designed and synthesized novel diphenylamine derivatives with a thiazolidinedione moiety as the terminal polar group as thyroid hormone receptor (TR) antagonists. Compounds bearing an appropriately sized N-alkyl group showed antagonistic activities towards both the hTRalpha1 and hTRbeta1 subtypes. |
62(0,2,2,2) |