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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(M_2),N-乙酰溶肉瘤素(M_3),N-甲酰溶肉瘤素酰苯丙氨酸乙酯(M_4),邻苯二甲谷氨酰溶肉瘤秦(M_5)及α-硝基-β-双(2-氯乙基)氨基己酸乙酯(M_9),α-硝基-β-双(2-氯乙基)氨基-β-(p-二甲苯基氨基)丙酸乙酯(M_(10))。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(M_2),N-乙酰溶肉瘤素(M_3),N-甲酰溶肉瘤素酰苯丙氨酸乙酯(M_4)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。
In this paper, we report the results of screening antitumor drugs from synthetic compounds over the past few years. Among the 207 synthetic compounds, the effective drugs are mainly nitrogen mustard derivatives, including N-formylcystein (M_2), N- (M_3), N-formylcysteinyl sphingosine (M_4), p-xylosyl-sarcosine Qin (M_5) and α-nitro-β-bis (M_9), ethyl α-nitro-β-bis (2-chloroethyl) amino-β- (p-xylylamino) propionate (M_ (10)). Of the other types of compounds, only propane isothiourea antimony tartrate Yoshida ascites sarcoma have a certain effect. Among the active compounds, N-formyl lysomatin (M_2), N-acetyl lysomatosin (M_3), N-formylcysarginin (M_4) and o- The efficacy of lysozyme (M5) is more prominent. On the basis of preclinical pharmacological studies, N-formylcysteinyl and N-formylcysarcoma acyl alanine have been recommended for clinical trials.