Synthesis and biological activity of N,N-dialkylaminoalkyl-substituted bisindolyl and diphenyl pyrazolone derivatives.
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.
Braña
Miguel F
MF
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
Gradillas
Ana
A
Ovalles
Angel G
AG
López
Berta
B
Acero
Nuria
N
Llinares
Francisco
F
Muñoz Mingarro
Dolores
D
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
D047069:Pyrazolones; C038362:pyrazolone