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
-
- Iikubo Kazuhiko
- Drug Discovery Research, Astellas Pharma Inc.
-
- Kondoh Yutaka
- Drug Discovery Research, Astellas Pharma Inc.
-
- Shimada Itsuro
- Drug Discovery Research, Astellas Pharma Inc.
-
- Matsuya Takahiro
- Drug Discovery Research, Astellas Pharma Inc.
-
- Mori Kenichi
- Drug Discovery Research, Astellas Pharma Inc.
-
- Ueno Yoko
- Drug Discovery Research, Astellas Pharma Inc.
-
- Okada Minoru
- Drug Discovery Research, Astellas Pharma Inc.
書誌事項
- タイトル別名
-
- Discovery of <i>N</i>-{2-Methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}-<i>N</i>′-[2-(propane-2-sulfonyl)phenyl]-1,3,5-triazine-2,4-diamine (ASP3026), a Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor
この論文をさがす
抄録
<p>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.</p>
収録刊行物
-
- CHEMICAL & PHARMACEUTICAL BULLETIN
-
CHEMICAL & PHARMACEUTICAL BULLETIN 66 (3), 251-262, 2018
公益社団法人 日本薬学会
- Tweet
キーワード
詳細情報 詳細情報について
-
- CRID
- 1390001204178754048
-
- NII論文ID
- 130006407116
-
- NII書誌ID
- AA00602100
-
- ISSN
- 13475223
- 00092363
-
- NDL書誌ID
- 028853992
-
- PubMed
- 29491259
-
- 本文言語コード
- en
-
- データソース種別
-
- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可