多亚甲基双［酰胺］类化合物：合成及对HL－60细胞的分化诱导作用

报导了一系列多亚甲基双［酰胺］类化合物的合成，由－摩尔多亚甲基二甲酰氯分别和二摩尔２－氨基噻唑啉及５－氨基－１－甲基吡啶酮反应制得。测定了其体外对ＨＬ－６０人早幼粒白血病细胞的分化诱导活性，初步结果表明：Ｎ，Ｎ｀－双吡啶酮基六二甲酰胺和Ｎ，Ｎ｀－双噻唑啉基八亚甲基二甲酰胺分别在０．１ｍｍｏｌ／Ｌ和０．５ｍｍｏｌ／Ｌ浓度时，诱导分化百分率可达６０％。此浓度下细胞存活率分别为２６％及２２％，其有效诱导浓度比ＨＭＢＡ低十倍。     

多亚甲基双[酰胺]类化合物：合成及对HL—60细胞的分化诱导作用

报导了一系列多亚甲基双[酰胺]类化合物的合成，由一摩尔多亚甲基二甲酰氯分别为二摩尔2－氨基噻唑啉及5－氨基－1－甲基吡啶酮反应制得。测定了其体外对HL－60人是幼粒白血病细胞的分化诱导活性，初步结果表明：N，N′－双吡啶酮基六二甲酰胺和N，N′－双噻唑啉基八亚甲基二甲酰胺分别在0.1mmol/L和0.5mmol/L浓度时，诱导分化百分率可达60％。此浓度下细胞存活率分别为26％及22％，其有效诱导浓度比HMBA低十倍。     

N-取代多亚甲基二甲酰胺类癌细胞分化诱导剂的合成

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-hexamethylenedicarboxamide (Ⅱ₃) were shown to be relatively effective inducers of differentiation.