Isoprenoid (phosphinylmethyl) phosphonates as inhibitors of squalene synthetase

SA Biller, C Forster, EM Gordon, T Harrity…

文献索引：Biller; Forster; Gordon; Harrity; Scott; Ciosek Jr. Journal of Medicinal Chemistry, 1988 , vol. 31, # 10 p. 1869 - 1871

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被引用次数: 143

摘要

In this paper, we describe our initial findings on the preparation and biological evaluation of isoprenoid (phosphinylmethy1) phosphonates (PMPs), stable analogues of farnesyl diphosphate (FPP, l), as inhibitors of squalene synthetase. Squalene synthetase14 catalyzes the reductive dimerization of two molecules of FPP to form squalene at the final branchpoint in the cholesterol biosynthesis pathway. Considering the recent clinical ...