关于抗肿瘤药物的研究  Ⅰ.207种合成化合物对动物移植性肿瘤的影响

STUDIES ON ANTITUMOR DRUGS——I.SCREENING OF 207 COMPOUNDS ON TRANSPLANTABLE TUMORS IN MICE AND RATS

摘要: 本文报告几年来从合成化合物中筛选抗肿瘤药的结果,在207种合成化合物中,有效药物主要都是氮芥衍生物,计有N-甲酰溶肉瘤素(M₂),N-乙酰溶肉瘤素(M₃),N-甲酰溶肉瘤素酰苯丙氨酸乙酯(M₄),邻苯二甲谷氨酰溶肉瘤秦(M₅)及α-硝基-β-双(2-氯乙基)氨基己酸乙酯(M₉),α-硝基-β-双(2-氯乙基)氨基-β-(p-二甲苯基氨基)丙酸乙酯(M₁₀)。在其他类型化合物中,只丙烷异硫脲酒石酸锑对吉田腹水肉瘤有一定疗效。有效化合物中以N-甲酰溶肉瘤素(M₂),N-乙酰溶肉瘤素(M₃),N-甲酰溶肉瘤素酰苯丙氨酸乙酯(M₄)及邻苯二甲谷氨酰溶肉瘤素(M5)的疗效比较突出。已经在临床前药理研究的基础上,将N-甲酰溶肉瘤素及N-甲酰溶肉瘤素酰苯丙氨酸乙酯推荐给临床试用。

Abstract: The screening data on the antitumor activity of 207 compds, were reported. Most of the effective compds, were nitrogen mustard derivatives, among which M₂ (N-formylsarcolysine), M₃ (N-acetylsarcolysine), M₄ (N-formylsarcolysine phenylalanine), M₅ (Glutamylsarcolysine), M₉ (Ethyl-α-nitro-β-di-(2-chloroethyl) amino caproate), M₁₀ (Ethyl-α-nitro-β-di-(2-chloroethyl)amino-β-(p-dimethylaminophenyl)-propionate) were most potent. Among these, M₂ (N-formylsarcolysine) and M₁ (N-formylsarcolysine phenylalanine)have been recommended for clinical trials.