Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors

被引：26

作者：

Lombardo, LJ ^{[1
]}

Camuso, A ^{[1
]}

Clark, J ^{[1
]}

Fager, K ^{[1
]}

Gullo-Brown, J ^{[1
]}

Hunt, JT ^{[1
]}

Inigo, I ^{[1
]}

Kan, D ^{[1
]}

Koplowitz, B ^{[1
]}

Lee, F ^{[1
]}

McGlinchey, K ^{[1
]}

Qian, LG ^{[1
]}

Ricca, C ^{[1
]}

Rovnyak, G ^{[1
]}

Traeger, S ^{[1
]}

Tokarski, J ^{[1
]}

Williams, DK ^{[1
]}

Wu, LI ^{[1
]}

Zhao, YF ^{[1
]}

Manne, V ^{[1
]}

Bhide, RS ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 07期

关键词：

farnesyltransferase inhibitor; BMS-316810;

D O I：

10.1016/j.bmcl.2005.02.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Tetrahydroquinoline-based small molecule inhibitors of farnesyltransferase (FT) have been identified. Lead compounds were shown to have nanomolar to sub-nanomolar activity in biochemical assays with excellent potency in a Ras-mutated cellular reversion assay. BMS-316810 (9e), a 0.7 nM FT inhibitor, was orally-active in a nude mouse tumor allograft efficacy study. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1895 / 1899

页数：5

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