Synthesis and evaluation of 3-and 7-substituted geranylgeranyl pyrophosphate analogs

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:18

Article

Maynor, Michelle¹  Scott, Sarah A.¹  Rickert, Emily L.¹  Gibbs, Richard A.¹ 

[1] Purdue Univ, Sch Pharm & Pharmaceut Sci, Dept Med Chem & Mol Pharmacol, W Lafayette, IN 47907 USA

关键词: geranylgeranylation;    isoprenoids;    palladium-catalyzed coupling;    post-translational modification;   

DOI  :  10.1016/j.bmcl.2008.02.014

来源: Elsevier

【 摘 要 】

Protein prenyl transferases have been a focus of anti-cancer drug discovery in recent years due to their roles in post-translational modi. cation of small GTP binding proteins. Attention is now turning to the development of GGTase I inhibitors. Here, we present the synthesis and biological evaluation of four GGPP analogs versus mammalian GGTase I and the discovery that 7-allyl GGPP is a surprisingly efficient GGTase I substrate. (C) 2008 Elsevier Ltd. All rights reserved.

【 授权许可】

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