Synthesis, structural elucidation and DNA-dependant protein kinase and antiplatelet studies of 2-amino-[5, 6, 7, 8-mono and 7, 8-di-substituted]-1, 3-benzoxazines

被引：26

作者：

Ihmaid, Saleh ^{[1
]}

Al-Rawi, Jasim ^{[1
]}

Bradley, Christopher ^{[1
]}

机构：

[1] La Trobe Univ, Sch Pharm & Appl Sci, Bendigo 3552, Australia

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 11期

关键词：

2-Amino-O-subst-1,3-benzoxazines; DNA-dependant protein kinase; Antiplatelet; PHOSPHOINOSITIDE; 3-KINASES; INHIBITOR; LY294002; CANCER; IDENTIFICATION; INFLAMMATION; POTENT;

D O I：

10.1016/j.ejmech.2010.07.066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A number of new 2-amino-[5, 6, 7 and 8]-O-substituted 1,3-benzoxazines, and 2-amino 8-methyl-7-O-substituted-1,3-benzoxazines were synthesized. Thirty one new compounds were tested for their effect on collagen induced platelet aggregation and it was found that the most active compounds were 8-methyl-2-morpholin-4-yl-7-(pyridin-3-ylmethoxy)-4H-1,3-benzoxazin-4-one 9f and 8-methyl-2-morpholin-4-yl-7-(pyridin-4-ylmethoxy)-4H-1,3-benzoxazin-4-one 9j with IC(50) = 2 +/- 1.5 and 4 +/- 2 mu M respectively. Inhibition of DNA-PK activity at concentrations of 1.6-4 mu M were tested for 9 products 5i, 7a-e and 9b, 9f and 9j. Crown Copyright (C) 2010 Published by Elsevier Masson SAS. All rights reserved.

引用

页码：4934 / 4946

页数：13

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