N,N-二烷基氨基烷基取代的双吲哚基和二苯基吡唑啉酮衍生物的合成及生物活性
Synthesis and biological activity of N,N-dialkylaminoalkyl-substituted bisindolyl and diphenyl pyrazolone derivatives.
作者信息
Braña Miguel F, Gradillas Ana, Ovalles Angel G, López Berta, Acero Nuria, Llinares Francisco, Muñoz Mingarro Dolores
机构信息
Departamento de Química, Bioquímica y Biología Molecular, Facultad de Farmacia, Universidad San Pablo CEU, Urb. Montepríncipe, 28668-Boadilla del Monte, Madrid, Spain.
出版信息
Bioorg Med Chem. 2006 Jan 1;14(1):9-16. doi: 10.1016/j.bmc.2005.09.059. Epub 2005 Nov 2.
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.
合成了与强效蛋白激酶C抑制剂星形孢菌素结构相关的新型化合物，其具有双吲哚基吡唑啉酮骨架，并在吡唑啉酮氮原子上被N，N - 二烷基氨基烷基侧链取代，并在几种人类细胞系中评估了其生长抑制特性。许多化合物显示出对HL-60细胞中肿瘤促进剂TPA刺激的TNF-α产生的抑制作用。已对其中几种化合物检测了对HeLa细胞的凋亡活性。
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