7-取代法呢基二磷酸类似物的合成
Synthesis of 7-substituted farnesyl diphosphate analogues.
作者信息
Rawat Diwan S, Gibbs Richard A
机构信息
Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907, USA.
出版信息
Org Lett. 2002 Sep 5;4(18):3027-30. doi: 10.1021/ol026176i.
PMID:12201708
Abstract
[structure: see text] Six farnesyl diphosphate analogues modified in the central isoprene unit have been prepared via our stereoselective vinyl triflate-mediated route to isoprenoids. The 7-allyl compound 6 is a modest inhibitor of mammalian protein-farnesyl transferase, but surprisingly the other five analogues are effective alternative substrates for this enzyme.
摘要
[结构：见正文] 通过我们立体选择性的三氟甲磺酸乙烯酯介导的类异戊二烯合成路线，制备了六种在中心异戊二烯单元修饰的法尼基二磷酸类似物。7-烯丙基化合物6是哺乳动物蛋白法尼基转移酶的一种适度抑制剂，但令人惊讶的是，其他五种类似物是该酶的有效替代底物。
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