Aryl tetrahydropyridine inhibitors of farnesyltransferase: Bioavailable analogues with improved cellular potency

被引：16

作者：

Gwaltney, SL ^{[1
]}

O'Connor, SJ ^{[1
]}

Nelson, LTJ ^{[1
]}

Sullivan, GM ^{[1
]}

Imade, H ^{[1
]}

Wang, WB ^{[1
]}

Hasvold, L ^{[1
]}

Li, Q ^{[1
]}

Cohen, J ^{[1
]}

Gu, WZ ^{[1
]}

Tahir, SK ^{[1
]}

Bauch, J ^{[1
]}

Marsh, K ^{[1
]}

Ng, SC ^{[1
]}

Frost, DJ ^{[1
]}

Zhang, HY ^{[1
]}

Muchmore, S ^{[1
]}

Jakob, CG ^{[1
]}

Stoll, V ^{[1
]}

Hutchins, C ^{[1
]}

Rosenberg, SH ^{[1
]}

Sham, HL ^{[1
]}

机构：

[1] Abbott Labs, Pharmaceut Discovery, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(03)00094-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered bioavailable aryl tetrahydropyridines that are potent in cell culture. The design, synthesis, SAR and biological properties of these compounds will be discussed. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1363 / 1366

页数：4

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