抗肿瘤药物—9-氨基吖啶和对-氨基水杨酸甲酯衍生物的合成(Ⅳ)  

Antitumor Compounds—(Ⅳ)Syntheses of the 9-Amino Acridine and p-Aminosalcyl-methyl-ester Derivatives

作　　者：郑懿雅 陈海英[2] 潘启超[2] 

机构地区：[1]中山大学化学系 [2]中山医科大学肿瘤研究所

出　　处：《中山大学学报（自然科学版）》1990年第4期51-55,共5页Acta Scientiarum Naturalium Universitatis Sunyatseni

摘　　要：本文选择9-氨基吖啶及对-氨基水杨酸甲酯为载体合成了8个新的植物生长控制剂衍生物,分别为9-(对-氯苯氧乙酰氨基)吖啶(Ⅰ),9-(2′,4′-二氯苯氧乙酰氨基)吖啶(Ⅱ),9-(2′,4′,5′-三氯苯氧乙酰氨基)吖啶(Ⅲ),9-(α-萘乙酰氨基)吖啶(Ⅳ),4-(对-氯苯氧乙酰氨基)水杨酸甲酯(Ⅴ),4-(2′,4′-二氯苯氧乙酰氨基)水杨酸甲酯(Ⅵ),4-(2′,4′,5′-三氯苯氧乙酰氨基)水杨酸甲酯(Ⅶ)和4-(α-萘乙酰氨基)水杨酸甲酯(Ⅷ)。给出了上述化合物的核磁共振和质谱数据,确证它们化学结构。初步抗癌试验结果表明化合物Ⅰ、Ⅱ、Ⅲ、Ⅴ和Ⅵ(在浓度100μg/ml下)对低分化鼻咽癌上皮细胞株(CNE_2)的生长有明显的抑制作用(IR>50％),其中Ⅱ和Ⅲ的抑制率在90％以上。In view of the antitumor activity of some 9-aminoacridine (9ACD) derivativesand the biological activity of p-aminosalicylic acid (PAS), these two compoundswere selected as the carriers of plant growth regulators, Thus, 8 new compoundswere synthesied, namely 9-(p-chloro-phenoxyacetyl-amino)-acridine(Ⅰ), 9-(2', 4'-dichloro-phenoxyacetyl-amino)-acridine(Ⅱ), 9-(2', 4', 5'-trichloro-phenoxyacetyl-amino)-acridine(Ⅲ), 9-(α-naphythlacetyl-amino) acridine (Ⅳ), 4-(p-chloro-phen-oxyacetyl-amino)-salicyl-methyl ester(Ⅴ), 4-(2',4'-dichloro-phenoxyacetyl-amino)-salicyl-methyl ester (Ⅵ), 4-(2', 4', 5'-trichloro-phenoxyacetyl-amino)-salicyl-methyl ester(Ⅶ) and 4-(α-naphthylacetyl-amino)-salicyl-methyl ester (Ⅷ). Basedon the NMR and MS data given in this paper, their chemical structures wereconfirmed. The preliminary results of in vitro antitumoral experiments show thatcompounds Ⅰ, Ⅱ,Ⅴ and Ⅵ(under 100μg/ml) possess significant inhibitory actionon the growth of the epithelial cell lines of poorly differentiated nasopharnygealcarcinoma CNE_2 (the inhibition rate(IR) is 50% or higher). Among them the IRsfor compounds Ⅱ and Ⅲ>90%.

关 键 词：抗肿瘤药物 氨基吖啶 水杨酸甲酯 

分 类 号：R979.1[医药卫生—药品]