title: Synthesis and biological evaluation of novel indolocarbazoles with anti-angiogenic activity.
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.
authors.affiliation: Departamento de Biología, Facultad de Farmacia, Universidad CEU San Pablo, Urb. Montepríncipe, 28660 Boadilla del Monte, Madrid, Spain. nacemes@ceu.es
authors.forename: Nuria
authors.initials: N
authors.lastname: Acero
authors.forename: Miguel F
authors.initials: MF
authors.lastname: Braña
authors.forename: Loreto
authors.initials: L
authors.lastname: Añorbe
authors.forename: Gema
authors.initials: G
authors.lastname: Domínguez
authors.forename: Dolores
authors.initials: D
authors.lastname: Muñoz-Mingarro
authors.forename: Francesc
authors.initials: F
authors.lastname: Mitjans
authors.forename: Jaume
authors.initials: J
authors.lastname: Piulats
mesh_terms: D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D002196:Capillaries / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003094:Collagen / Q000494:pharmacology; D004338:Drug Combinations; D006801:Humans; D007797:Laminin / Q000494:pharmacology; D008175:Lung Neoplasms / Q000098:blood supply* / Q000188:drug therapy*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D015394:Molecular Structure; D009389:Neovascularization, Pathologic / Q000188:drug therapy; D011509:Proteoglycans / Q000494:pharmacology; D013055:Spectrophotometry, Infrared; D019311:Staurosporine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D020533:Angiogenesis Inhibitors; D004338:Drug Combinations; D007797:Laminin; D011509:Proteoglycans; C059485:matrigel; D003094:Collagen; D019311:Staurosporine