Synthesis and biological evaluation of novel indolocarbazoles with anti-angiogenic activity
Synthesis and biological evaluation of novel indolocarbazoles with anti-angiogenic activity
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DOI：
10.1016/j.ejmech.2011.11.040
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发表时间：
2012-02-01
影响因子：
6.7
通讯作者：
Piulats, Jaume
中科院分区：
文献类型：
--
作者：
Acero, Nuria;Brana, Miguel F.;Piulats, Jaume
合成了一系列新型吲哚咔唑类化合物，并研究了它们对HUVEC、LoVo、DLD-1和ST-486细胞株的增殖抑制作用。将取代的二甲氨基烷氧基链连接到吲哚氮上的星形孢子素类似物在HUVEC增殖方面显示出有趣的活性和选择性。以活性最高的化合物为研究对象，研究了三维基质中毛细管形成的影响因素。还分析了它们在小鼠Lewis肺癌模型中的体内抗血管生成活性。(C)2011年爱思唯尔·马森公司。版权所有。
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.