title: Synthesis and biological activity of N,N-dialkylaminoalkyl-substituted bisindolyl and diphenyl pyrazolone derivatives.
abstract: New compounds, structurally related to the potent protein kinase C inhibitor staurosporine, with a bisindolylpyrazolone framework and substituted on the pyrazolone nitrogens with N,N-dialkylaminoalkyl side chain, were synthesized and evaluated for growth-inhibitory properties in several human cell lines. Many showed inhibition of TNF-alpha production in response to the tumor promotor TPA on HL-60 cells. The apoptotic activity on HeLa cells has been examined for several of these compounds.
authors.affiliation: Departamento de Química, Bioquímica y Biología Molecular, Facultad de Farmacia, Universidad San Pablo CEU, Urb. Montepríncipe, 28668-Boadilla del Monte, Madrid, Spain. mfbrana@ceu.es
authors.forename: Miguel F
authors.initials: MF
authors.lastname: Braña
authors.forename: Ana
authors.initials: A
authors.lastname: Gradillas
authors.forename: Angel G
authors.initials: AG
authors.lastname: Ovalles
authors.forename: Berta
authors.initials: B
authors.lastname: López
authors.forename: Nuria
authors.initials: N
authors.lastname: Acero
authors.forename: Francisco
authors.initials: F
authors.lastname: Llinares
authors.forename: Dolores
authors.initials: D
authors.lastname: Muñoz Mingarro
mesh_terms: D002855:Chromatography, Thin Layer; D018360:Crystallography, X-Ray; D018922:HL-60 Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D015394:Molecular Structure; D047069:Pyrazolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization; D013056:Spectrophotometry, Ultraviolet
chemical_list: D047069:Pyrazolones; C038362:pyrazolone