Mixed lineage kinase activity of indolocarbazole analogues

被引:90
作者
Murakata, C
Kaneko, M
Gessner, G
Angeles, TS
Ator, MA
O'Kane, TM
McKenna, BAW
Thomas, BA
Mathiasen, JR
Saporito, MS
Bozyczko-Coyne, D
Hudkins, RL
机构
[1] Cephalon Inc, Dept Med Chem, W Chester, PA 19380 USA
[2] Cephalon Inc, Dept Biochem, W Chester, PA 19380 USA
[3] Cephalon Inc, Dept Neurobiol, W Chester, PA 19380 USA
[4] Kyowa Hakko Kogyo Co Ltd, Tokyo, Japan
关键词
D O I
10.1016/S0960-894X(01)00690-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The MLKI-3 activity for a series of analogues of the indolocarbazole K-252a is reported. Addition of 3,9-bis-alkylthiomethyl groups to K-252a results in potent and selective MLK inhibitors. The in vitro and in vivo survival promoting activity of bis-isopropylthiomethyl-K-252a (16, CEP-11004/KT-8138)is reported. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:147 / 150
页数:4
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