使用氟混合物合成法合成一个雷锁酸内酯（RAL）文库及其对一系列激酶的选择性特征分析。
Synthesis of a resorcylic acid lactone (RAL) library using fluorous-mixture synthesis and profile of its selectivity against a panel of kinases.
机构信息
Institut de Science et Ingénierie Supramoléculaires (ISIS-UMR 7006), Université de Strasbourg-CNRS, 8 allée Gaspard Monge, 67000 Strasbourg, France.
出版信息
Chemistry. 2009 Nov 2;15(43):11498-506. doi: 10.1002/chem.200901375.
A library of resorcylic acid lactones (RAL) containing a cis-enone moiety targeting kinases bearing a cysteine residue within the ATP-binding pocket was prepared using a fluorous-mixture synthesis and evaluated against a panel of 19 kinases thus providing important structure-activity trends. Two new analogues were then profiled for their selectivity against a panel of 402 kinases providing the broadest evaluation of this pharmacophores' selectivity.
使用氟混合物合成法制备了一个含有 cis-烯酮部分的雷锁辛酸内酯 (RAL) 文库，该文库针对 ATP 结合口袋内含有半胱氨酸残基的激酶，对 19 种激酶进行了评估，从而提供了重要的构效关系趋势。然后对两个新类似物进行了针对 402 种激酶的选择性分析，这是对该药效团选择性的最广泛评估。
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