Wen X X, Hu Z Y, Guo D S, Wang H C, Zhao Y W
Faculty of Pharmacy, Shandong Medical University, Jinan.
Yao Xue Xue Bao. 1993;28(3):234-7.
N-Alkyl polymethylene dicarboxamides are known potent inducers of erythroid differentiation in murine erythroleukemia cells. The most active inducer N,N,N',N'-tetramethyl-1, 6-hexane-dicarboxamide has the same effectiveness as HMBA which has entered clinical trials as a differentiating agent. These compounds also have inducing activity in HL-60 human promyelocytic leukemia cells. In this paper, the synthesis of a series of N,N'-bis[2-(2-thiazolinyl)], N,N'-bis[5-(1-methyl-2-pyridonyl)], N,N'-bis[3-(1-phenyl-5-pyrazolonyl)] polymethylene dicarboxamides and 3,3'-(polymethylene dicarbonyl)bis(1-methyl-2-imidazolidine-thiones) is reported. The inducing activities of the compounds were evaluated in vitro with HL-60 human promyelocytic leukemia cell line. Among them, N,N'-bis[2-(2-thiazolinyl)]-1,8-octamethylene- dicarboxamide (I4) and N,N'-bis[5-(1-methyl-2-pyridonyl)]-1,6-hexamethylenedicarboxami de (II3) were shown to be relatively effective inducers of differentiation.
N-烷基聚亚甲基二羧酰胺是已知的鼠红细胞白血病细胞中红细胞分化的有效诱导剂。活性最高的诱导剂N,N,N',N'-四甲基-1,6-己烷二羧酰胺与已作为分化剂进入临床试验的HMBA具有相同的效力。这些化合物在HL-60人早幼粒细胞白血病细胞中也具有诱导活性。本文报道了一系列N,N'-双[2-(2-噻唑啉基)]、N,N'-双[5-(1-甲基-2-吡啶酮基)]、N,N'-双[3-(1-苯基-5-吡唑啉酮基)]聚亚甲基二羧酰胺和3,3'-(聚亚甲基二羰基)双(1-甲基-2-咪唑烷硫酮)的合成。用HL-60人早幼粒细胞白血病细胞系体外评估了这些化合物的诱导活性。其中，N,N'-双[2-(2-噻唑啉基)]-1,8-辛亚甲基二羧酰胺（I4）和N,N'-双[5-(1-甲基-2-吡啶酮基)]-1,6-己亚甲基二羧酰胺（II3）被证明是相对有效的分化诱导剂。
