Synthesis of novel 1,4-benzoxazin-3-one derivatives as inhibitors against tyrosine kinases

被引：18

作者：

Honda, Takahiro ^{[1
,2
]}

Terao, Takahiro ^{[2
]}

Aono, Hiroyuki ^{[1
,2
]}

Ban, Masakazu ^{[1
,2
]}

机构：

[1] Santen Pharmaceut Co Ltd, Ctr Res & Dev, Ikoma, Nara 6300101, Japan

[2] Nara Inst Sci & Technol, Grad Sch Mat Sci, Ikoma, Nara 6300192, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 02期

关键词：

1,4-Benzoxazin-3-one chemical library; Tyrosine kinase inhibitor; TFP resin; KDR; ABL; Intramolecular S-O non-bonded interaction; GROWTH-FACTOR RECEPTOR;

D O I：

10.1016/j.bmc.2008.11.060

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We designed and synthesized a novel 1,4-benzoxazin-3-one derivative 4 which would have inhibitory activities against tyrosine kinases. They could be synthesized easily from various carboxylic acids 10 and commercially available amines using TFP resin without purification. In this article, we will report the design and synthesis of a novel 1,4-benzoxazin-3-one chemical library 4 and the inhibitory activities against KDR and ABL which are closely related to chronic diseases such as cancer. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：699 / 708

页数：10

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