253329-09-8Relevant articles and documents
Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors
Kim, Boyoung,Park, Hwanggue,Lee, Seul Ki,Park, Sung Jean,Koo, Tae-Sung,Kang, Nam Sook,Hong, Ki Bum,Choi, Sungwook
, p. 777 - 787 (2016/08/23)
Wild type transthyretin (TTR) and mutant TTR misfold and misassemble into a variety of extracellular insoluble amyloid fibril and/or amorphous aggregate, which are associated with a variety of human amyloid diseases. To develop potent TTR amyloidogenesis
Synthesis and pharmacological characterization of 1-benzyl-4-aminoindole- based thyroid hormone receptor β agonists
Takahashi, Naoki,Maeda, Koji,Asano, Yukiyasu,Watanabe, Nobuhide
, p. 488 - 498 (2014/01/17)
A series of 1-benzylindole-based TRβ agonists were prepared and evaluated. Compounds 11b′ and 11c′ were found to have cholesterol-lowering in a rat model with marginal effects on cardiac function and HPT axis. The present work illustrates the potential use of indoles as inner ring isosteres.
Characterization of thyroid hormone receptor α (TRα)-specific analogs with varying inner- and outer-ring substituents
Ocasio, Cory A.,Scanlan, Thomas S.
, p. 762 - 770 (2008/09/17)
Analogs of the TRα-specific thyromimetic CO23 were synthesized and analyzed in vitro using competitive binding and transactivation assays. Like CO23, all analogs bind to both thyroid hormone receptor subtypes with about the same affinity; however, modification of CO23 by derivatization of the 3′ position of the outer-ring or replacement of the inner-ring iodides with bromides attenuates binding. Despite lacking a preference in binding to TRα, all analogs display TRα-specificity in transactivation assays using U2OS and HeLa cells. At best, several agonists exhibit an approximately 6-12-fold preference in transactivation when tested with TRα in HeLa cells. One analog, CO24, showed in vivo TRα-specific action in a tadpole metamorphosis assay.