2. Academic Validation
  3. Synthesis and biological evaluation of novel indolocarbazoles with anti-angiogenic activity

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

  • Eur J Med Chem. 2012 Feb:48:108-13. doi: 10.1016/j.ejmech.2011.11.040.
Nuria Acero 1,  Miguel F Braña,  Loreto Añorbe,  Gema Domínguez,  Dolores Muñoz-Mingarro,  Francesc Mitjans,  Jaume Piulats
Affiliations

Affiliation

  • 1 Departamento de Biología, Facultad de Farmacia, Universidad CEU San Pablo, Urb. Montepríncipe, 28660 Boadilla del Monte, Madrid, Spain. nacemes@ceu.es
PMID: 22182929 DOI: 10.1016/j.ejmech.2011.11.040
Abstract

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.

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