Convenient Synthetic Method for 3-(3-Substituted indol-2-yl)quinoxalin-2-ones as VEGF Inhibitor

Author:

Aoki Katsuyuki12,Koseki Jyun-ichi1,Takeda Shuichi1,Aburada Masaki3,Miyamoto Ken-ichi2

Affiliation:

1. Research Division, Tsumura & Co.

2. Department of Clinical Pharmacy, Graduate School of Natural Science and Technology, Kanazawa University

3. Faculty of Pharmacy, Musashino University

Publisher

Pharmaceutical Society of Japan

Subject

Drug Discovery,General Chemistry,General Medicine

Reference10 articles.

1. 1) Ladouceur G. H., Bear B., Bi C., Brittelli D. R., Burke M. J., Chen G., Cook J., Dumas J., Sibley R., Turner M. R., WO 2004043950 (2004).

2. 2) Inhibitory effect of 9 toward the VEGF-induced proliferation of human glomerular endothelium cells in vitro [IC50 (μmol/l)=0.04]. Inhibitory effect of 9 toward the VEGF-induced auto-phosphorylation with human umbilical vein endothelial cells in vitro [IC50 (μmol/l)=0.02]. Inhibitory effect of the derivative 9 on VEGF-induced dye leakage in rat skin (7 week-old male Wistar rats were used in this study) [70% against control at 25 mg/kg p.o.].

3. Potent Platelet-Derived Growth Factor-.BETA. Receptor (PDGF-.BETA.R) Inhibitors: Synthesis and Structure-Activity Relationships of 7-[3-(Cyclohexylmethyl)ureido]-3-{1-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl}quinoxalin-2(1H)-one Derivatives

4. 5) Similar indolenine and/or direct pathway as in the mechanism of Pictet–Spengler reaction may be engaged in this TFA-promoted coupling process of 3-substituted indoles with quinoxalin-2-ones. For review on discussion about this mechanism, see: Enrique L. L., Marcela A., Andrea B. J. B., Teodoro S. K., ARKIVOC. Issue in Honor of Prof. Rosa Lederkremer, (xii), 98—153 (2005).

全球学者库

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"全球学者库"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前全球学者库共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2023 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3