文章基本信息

标题：Discovery of N-{2-Methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}-N′-[2-(propane-2-sulfonyl)phenyl]-1,3,5-triazine-2,4-diamine (ASP3026), a Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor
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作者：Kazuhiko Iikubo ; Yutaka Kondoh ; Itsuro Shimada 等
期刊名称：Chemical and Pharmaceutical Bulletin
印刷版ISSN：0009-2363
电子版ISSN：1347-5223
出版年度：2018
卷号：66
期号：3
页码：251-262
DOI：10.1248/cpb.c17-00784
语种：English
出版社：The Pharmaceutical Society of Japan
摘要：

Anaplastic lymphoma kinase (ALK) is a validated therapeutic target for treating echinoderm microtubule-associated protein-like 4 (EML4)-ALK positive non-small cell lung cancer (NSCLC). We synthesized a series of 1,3,5-triazine derivatives and identified ASP3026 ( 14a ) as a potent and selective ALK inhibitor. In mice xenografted with NCI-H2228 cells expressing EML4-ALK, once-daily oral administration of 14a demonstrated dose-dependent antitumor activity. Here, syntheses and structure–activity relationship (SAR) studies of 1,3,5-triazine derivatives are described.
关键词：1,3,5-triazine;non-small cell lung cancer;anaplastic lymphoma kinase;echinoderm microtubule-associated protein-like 4