一种强效且选择性的p90核糖体S6激酶抑制剂的合成。
Synthesis of a potent and selective inhibitor of p90 Rsk.
作者信息
Maloney David J, Hecht Sidney M
机构信息
Departments of Chemistry and Biology, University of Virginia, Charlottesville, Virginia 22901, USA.
出版信息
Org Lett. 2005 Mar 17;7(6):1097-9. doi: 10.1021/ol0500463.
[reaction: see text] The synthesis of the naturally occurring kaempferol glycoside SL0101 has been accomplished, as has its biochemical evaluation. SL0101 exhibits selective and potent p90 Rsk inhibitory activity at nanomolar concentrations without inhibiting the function of upstream kinases such as MEK, Raf, or PKC. The synthesis verified the structural assignment of the natural product and has provided access to material sufficient for detailed biological evaluation.
[反应：见正文] 天然存在的山奈酚糖苷SL0101的合成已经完成，其生化评估也已完成。SL0101在纳摩尔浓度下表现出选择性和强效的p90 Rsk抑制活性，而不抑制上游激酶如MEK、Raf或PKC的功能。该合成验证了天然产物的结构归属，并提供了足以进行详细生物学评估的材料。
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