Synthesis and biological activity of N, N-dialkylaminoalkyl-substituted bisindolyl and diphenyl pyrazolone derivatives

…, B López, N Acero, F Llinares, DM Mingarro

Index: Brana, Miguel F.; Gradillas, Ana; Ovalles, Angel G.; Lopez, Berta; Acero, Nuria; Llinares, Francisco; Mingarro, Dolores Munoz Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 1 p. 9 - 16

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Citation Number: 84

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-α production in response to the tumor promotor TPA on HL-60 cells. The apoptotic activity on HeLa cells ...