新型生物反应调节剂：具有肿瘤坏死因子-α产生调节活性的邻苯二甲酰亚胺
Novel biological response modifiers: phthalimides with tumor necrosis factor-alpha production-regulating activity.
作者信息
Miyachi H, Azuma A, Ogasawara A, Uchimura E, Watanabe N, Kobayashi Y, Kato F, Kato M, Hashimoto Y
机构信息
Institute of Molecular and Cellular Biosciences, University of Tokyo, Japan.
出版信息
J Med Chem. 1997 Aug 29;40(18):2858-65. doi: 10.1021/jm970109q.
Novel N-substituted phthalimides (2-substituted 1H-isoindole-1,3-diones) were prepared, and their effects on tumor necrosis factor-alpha (TNF-alpha) production by human leukemia cell line HL-60 stimulated with 12-O-tetradecanoylphorbol 13-acetate (TPA) or okadaic acid (OA) were examined. A structure-activity relationship study of the N-phenylphthalimides and N-benzylphthalimides revealed that their enhancing effect on TPA-induced TNF-alpha production by HL-60 cells and their inhibiting effect on OA-induced TNF-alpha production by HL-60 cells are only partially correlated.
制备了新型N-取代邻苯二甲酰亚胺（2-取代-1H-异吲哚-1,3-二酮），并研究了它们对用12-O-十四烷酰佛波醇-13-乙酸酯（TPA）或冈田酸（OA）刺激的人白血病细胞系HL-60产生肿瘤坏死因子-α（TNF-α）的影响。对N-苯基邻苯二甲酰亚胺和N-苄基邻苯二甲酰亚胺的构效关系研究表明，它们对HL-60细胞TPA诱导的TNF-α产生的增强作用以及对HL-60细胞OA诱导的TNF-α产生的抑制作用仅部分相关。
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