Synthesis of a Resorcylic Acid Lactone (RAL) Library Using Fluorous-Mixture Synthesis and Profile of its Selectivity Against a Panel of Kinases
Synthesis of a Resorcylic Acid Lactone (RAL) Library Using Fluorous-Mixture Synthesis and Profile of its Selectivity Against a Panel of Kinases
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DOI：
10.1002/chem.200901375
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发表时间：
2009-01-01
影响因子：
4.3
通讯作者：
Winssinger, Nicolas
中科院分区：
文献类型：
--
作者：
Jogireddy, Rajamalleswaramma;Dakas, Pierre-Yves;Winssinger, Nicolas
使用氟混合物合成制备了一个含有顺式烯酮部分的雷琐酸内酯（RAL）库，靶向在ATP结合口袋内具有半胱氨酸残基的激酶，并对一组19种激酶进行了评价，从而提供了重要的结构-活性趋势。两个新的类似物，然后分析其对一组402激酶的选择性，提供了最广泛的评价，这种药效团的选择性
A library of resorcylic acid lactones (RAL) containing a cis-enone moiety targeting kinases hearing 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