一类含有苯基萘核心的新型高亲和力甲状腺激素模拟物。
A new class of high affinity thyromimetics containing a phenyl-naphthylene core.
作者信息
Hangeland Jon J, Friends Todd J, Doweyko Arthur M, Mellström Karin, Sandberg Johnny, Grynfarb Marlena, Ryono Denis E
机构信息
Pharmaceutical Research Institute, Bristol-Myers Squibb, Princeton, NJ 08543-5400, USA.
出版信息
Bioorg Med Chem Lett. 2005 Oct 15;15(20):4579-84. doi: 10.1016/j.bmcl.2005.06.093.
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.
据报道，含有新型苯基萘核心的高亲和力甲状腺激素模拟物。通过铃木偶联协议可以很容易地获得功能化的核心。这类新型TR配体的例子对TRβ受体具有亚纳摩尔结合亲和力，对TRβ具有低至中等的选择性。它们还表现出与其他基于3,5,3'-三碘甲状腺原氨酸中发现的二芳基醚核心的甲状腺激素模拟物不同的构效关系。
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