Aromatic farnesyl diphosphate analogues: vinyl triflate-mediated synthesis and preliminary enzymatic evaluation.
Aromatic farnesyl diphosphate analogues: vinyl triflate-mediated synthesis and preliminary enzymatic evaluation.
复制标题
芳香族法尼基二磷酸类似物：三氟甲磺酸乙烯酯介导的合成和初步酶促评价。
DOI：
10.1016/s0960-894x(02)00187-7
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发表时间：
2002
影响因子：
2.7
通讯作者：
Gibbs,RichardA
中科院分区：
文献类型：
--
作者：
Zhou,Chunmei;Shao,Ying;Gibbs,RichardA
一个立体控制的乙烯基三氟甲磺酸酯为基础的合成路线已被用来制备四个类似物的法呢基二磷酸（FPP）的末端异戊二烯单元已被取代的芳香族部分。这些类似物中的两个与蛋白质法尼基转移酶没有产生相互作用，但2-萘基衍生物2是酶的适度抑制剂，对联苯衍生物4是令人惊讶的有效替代底物。
A stereocontrolled vinyl triflate-based synthetic route has been used to prepare four analogues of farnesyl diphosphate (FPP) where the terminal isoprene units have been replaced with aromatic moieties. Two of these analogues exhibit no productive interaction with protein farnesyltransferase, but the 2-naphthyl derivative 2 is a modest inhibitor of the enzyme, and the para-biphenyl derivative 4 is a surprisingly effective alternative substrate.