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氨基酸的Nα-苄氧羰基-N,N-双-(2-卤代乙基)-酰肼衍生物的抗肿瘤作用

Antitumor effect of N alpha-benzyloxycarbonyl-N,N-bis-(2-halogenethyl)-hydrazide derivatives of amino acids.

作者信息

Karaivanova M H, Zakhariev S G, Golovinsky E V

出版信息

Neoplasma. 1980;27(2):137-42.

PMID:7393353
Abstract

The antitumor effect of some N alpha-benzyloxycarbonyl-N,N-bis-(2-halogenethyl)hydrazide derivatives of lysine, glycine, cystine, phenylalanine and p-chlorophenylalanine, was studied. Six of eight newly synthesized compounds show considerable antitumor effect on solid Walker carcinosarcoma 256 (about 95% tumor growth inhibition). Three of these compounds under study increased the lifespan of mice with leukemia L1210. The investigation of the effect of N alpha-benzyloxycarbonyl,D,L-phenylalanine-N,N-bis(2-chloroethyl)hydrazine on various mouse tumors showed remarkable growth inhibition of the Ehrlich ascites carcinoma, sarcoma 37, colon adenocarcinoma akatol and lesser antitumor effect also on solid adenocarcinoma 755, Lewis lung carcinoma and melanoma B16. All investigated compounds exhibited depression of leukocyte count--their toxicity being, however, lower than that of sarcolysine in parallel experiments.

摘要

研究了赖氨酸、甘氨酸、胱氨酸、苯丙氨酸和对氯苯丙氨酸的一些Nα-苄氧羰基-N,N-双(2-卤代乙基)酰肼衍生物的抗肿瘤作用。新合成的8种化合物中有6种对实体Walker癌肉瘤256显示出相当大的抗肿瘤作用(约95%的肿瘤生长抑制率)。所研究的这些化合物中有3种延长了患白血病L1210小鼠的寿命。对Nα-苄氧羰基-D,L-苯丙氨酸-N,N-双(2-氯乙基)肼对各种小鼠肿瘤作用的研究表明,艾氏腹水癌、肉瘤37、结肠腺癌akatol有显著的生长抑制,对实体腺癌755、Lewis肺癌和黑色素瘤B16也有较小的抗肿瘤作用。所有研究的化合物均表现出白细胞计数降低——然而,在平行实验中它们的毒性低于溶肉瘤素。

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