Synthesis and biological evaluation of novel indolocarbazoles with anti-angiogenic activity

被引：15

作者：

Acero, Nuria ^{[1
]}

Brana, Miguel F. ^{[2
]}

Anorbe, Loreto ^{[3
]}

Dominguez, Gema ^{[3
]}

Munoz-Mingarro, Dolores ^{[3
]}

Mitjans, Francesc ^{[4
]}

Piulats, Jaume ^{[4
]}

机构：

[1] Univ CEU San Pablo, Fac Farm, Dept Biol, Madrid 28660, Spain

[2] Inst Canario Invest Canc, Madrid 28110, Spain

[3] Univ CEU San Pablo, Fac Farm, Dept Quim, Madrid 28660, Spain

[4] Merck Farma & Quim SA, Lab Bioinvest, Barcelona 08010, Spain

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 48卷

关键词：

Angiogenesis; Indolocarbazole; HUVEC; Staurosporine analogs; IN-VITRO; STAUROSPORINE AGLYCONE; CELLS; BISINDOLYLMALEIMIDES; MODELS; VIVO;

D O I：

10.1016/j.ejmech.2011.11.040

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of indolocarbazoles were synthesized and their antiproliferative activity against HUVEC, LoVo, DLD-1 and ST-486 cell lines, was investigated. Those staurosporine analogs in which a substituted dimethylaminoalkoxy chain was attached to the indolic nitrogen showed interesting activity and selectivity with respect to HUVEC proliferation. The effect on capillary tube formation in 3-dimensional matrigel matrix was studied using the most active compounds. Evaluation of their in vivo anti-angiogenic activity in a murine Lewis lung cancer model was also analyzed. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：108 / 113

页数：6

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