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-α 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.

The synthesis of new bisindolyl and diphenylpirazolone derivatives are reported. Many showed inhibition against TPA induced TNF-α production in HL-60 cells. Several of these analogues also showed apoptotic activity.Figure optionsDownload as PowerPoint slide