A new class of high affinity thyromimetics containing a phenyl-naphthylene core.
High affinity thyromimetics containing a novel phenyl-naphthylene core are reported. The functionalized core is readily accessible via a Suzuki coupling protocol. Examples of this new class of TR ligands have sub-nanomolar binding affinities for the TRbeta receptor and low to modest selectivity for TRbeta. They also exhibit an SAR that diverges from other thyromimetics that are based on the diaryl ether core found in 3,5,3'-triiodothyronine.
Hangeland
Jon J
JJ
Pharmaceutical Research Institute, Bristol-Myers Squibb, Princeton, NJ 08543-5400, USA. jon.hangeland@bms.com
Friends
Todd J
TJ
Doweyko
Arthur M
AM
Mellström
Karin
K
Sandberg
Johnny
J
Grynfarb
Marlena
M
Ryono
Denis E
DE
D008958:Models, Molecular; D009281:Naphthalenes / Q000737:chemistry*; D011988:Receptors, Thyroid Hormone / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013963:Thyroid Hormones / Q000737:chemistry / Q000378:metabolism*
D009281:Naphthalenes; D011988:Receptors, Thyroid Hormone; D013963:Thyroid Hormones; C505999:phenyl-naphthylene