Jeney A, Kopper L, Nagy P, Lapis K, Süli-Vargha H, Medzihradszky K
Cancer Chemother Pharmacol. 1986;16(2):129-32. doi: 10.1007/BF00256162.
The antitumor action of the 2-chloroethylnitrosocarbamoyl derivatives of peptides related to the 9-13 amino acid residues of alpha-MSH/ACTH and of the C-terminal tetrapeptide analogue of gastrin have been investigated. Series of 2-chloroethylnitrosoureas attached to amino acids, di-, tri-, tetra-, or pentapeptides were examined in a primary screening system. Among these compounds the Pro-Val-, Lys-Pro-Val-, and Trp-Gly-Lys-Pro-Val-containing 2-chloroethylnitrosocarbamoyl groups were the most effective in the L1210 system. The human melanoma xenograft line was also affected by these agents, while colorectal xenografts were insensitive. A combination of tripeptide-2-chloroethyl-nitrosourea with BCNU induced more than additive growth inhibition of L1210 leukemia.
已对与α-MSH/ACTH的9 - 13个氨基酸残基相关的肽以及胃泌素C端四肽类似物的2-氯乙基亚硝基氨基甲酰衍生物的抗肿瘤作用进行了研究。在一个初步筛选系统中检测了连接到氨基酸、二肽、三肽、四肽或五肽上的一系列2-氯乙基亚硝基脲。在这些化合物中，含2-氯乙基亚硝基氨基甲酰基的脯氨酸-缬氨酸、赖氨酸-脯氨酸-缬氨酸和色氨酸-甘氨酸-赖氨酸-脯氨酸在L1210系统中最有效。人黑色素瘤异种移植系也受到这些药物的影响，而结直肠癌异种移植则不敏感。三肽-2-氯乙基-亚硝基脲与卡莫司汀联合使用对L1210白血病产生了超过相加的生长抑制作用。
