A novel metal-chelating inhibitor of protein farnesyltransferase

被引：17
|
作者：
Hamasaki, A
Naka, H
Tamanoi, F
Umezawa, K
Otsuka, M
机构：
[1] Kumamoto Univ, Grad Sch Pharmaceut Sci, Kumamoto 8620973, Japan
[2] Keio Univ, Fac Sci & Technol, Kohoku Ku, Yokohama, Kanagawa 2230061, Japan
[3] Univ Calif Los Angeles, Dept Microbiol & Mol Genet, Inst Mol Biol, Los Angeles, CA 90095 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 09期
关键词：
D O I：
10.1016/S0960-894X(03)00183-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A novel metal chelator comprising a 4-(naphthalen-1-yl)pyridine and 2-aminoethanethiol was synthesized. This showed inhibitory activity against human protein farnesyltransferase with IC50 1.9 muM, induced morphological change in K-ras-NRK cells at 0.5 mug/mL and showed growth inhibition of K-ras-NRK cells with IC50 0.32 mug/mL. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1523 / 1526
页数：4
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