Departamento de Biología, Facultad de Farmacia, Universidad CEU San Pablo, Urb. Montepríncipe, 28660 Boadilla del Monte, Madrid, Spain.
Eur J Med Chem. 2012 Feb;48:108-13. doi: 10.1016/j.ejmech.2011.11.040. Epub 2011 Dec 7.
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.
合成了一系列新型吲哚咔唑，并研究了它们对 HUVEC、LoVo、DLD-1 和 ST-486 细胞系的抗增殖活性。那些吲哚氮上连接取代的二甲氨基烷氧基链的司他夫定类似物对 HUVEC 增殖显示出有趣的活性和选择性。使用最活性的化合物研究了它们在 3 维基质胶中的毛细血管形成的影响。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的评价。
