RSK 对 SL0101 的环己醇类似物的亲和力严重依赖于 B 环 C-4'-羟基。
The affinity of RSK for cylitol analogues of SL0101 is critically dependent on the B-ring C-4'-hydroxy.
机构信息
Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115, USA.
Departments of Pathology, Microbiology & Immunology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
出版信息
Chem Commun (Camb). 2020 Mar 10;56(20):3058-3060. doi: 10.1039/d0cc00128g.
Abstract
Five cyclitol analogues of SL0101 with variable substitution at the C-4' position (i.e., OH, Cl, F, H, OMe) were synthesized. The series of analogues were evaluated for their ability to inhibit p90 ribosomal S6 kinase (RSK) activity. The study demonstrated the importance of the B-ring C-4' hydroxy group for RSK1/2 inhibition.
摘要
合成了 SL0101 的 5 个环糖醇类似物，它们在 C-4' 位置（即 OH、Cl、F、H、OMe）具有不同的取代基。该系列类似物被评估抑制 p90 核糖体 S6 激酶（RSK）活性的能力。该研究表明 B 环 C-4' 羟基对 RSK1/2 抑制的重要性。
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