Design, synthesis, and preliminary biological evaluation of 2,3-dihydro-3-hydroxymethyl-1,4-benzoxazine derivatives

被引：56
作者：
Jiao, PF
Zhao, BX [1 ]
Wang, WW
Shin, DS
He, QX
Wan, MS
Shin, DS
Miao, JY
机构：
[1] Shandong Univ, Sch Chem & Chem Engn, Inst Organ Chem, Jinan 250100, Peoples R China
[2] Shandong Univ, Sch Life Sci, Inst Dev Biol, Jinan 250100, Peoples R China
[3] Changwon Natl Univ, Dept Chem, Chang Won 641773, South Korea
[4] Changwon Natl Univ, Res Inst Nat Sci, Chang Won 641773, South Korea
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 11期
关键词：
2,3-dihydro-3-hydroxymethl-1,4-benzoxazines; vascular endothelial cells; A549; cells; apoptosis;
D O I：
10.1016/j.bmcl.2006.03.013
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We synthesized a series of novel small Molecules, 2,3-dihydro-3-hydroxymethyl-1,4-benzoxazine derivatives, by tandem reduction-oxirane opening of 2-nitroaroxymethyloxiranes in moderate or excellent yields. We investigated the effects of all of the Compounds on HUVEC apoptosis and A549 cell growth. The results showed that 6,8-dichloro-2,3-dihydro-3-hydroxymethyl-1,4-benzoxazine was the most effective small molecule in promoting HUVEC apoptosis and inhibiting A549 cell proliferation, but 6-amino-2,3-dihydro-3-hydroxymethyl-1,4-benzoxazine could remarkably inhibit HUVEC apoptosis and might induce the formation of microvessel. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2862 / 2867
页数：6
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