自旋标记氨基酸亚硝基脲衍生物——合成与抗肿瘤活性

Spin labeled amino acid nitrosourea derivatives--synthesis and antitumour activity.

作者信息

Zheleva A, Raikov Z, Ilarionova M, Todorov D

机构信息

Higher Medical Institute, Stara Zagora, Bulgaria.

出版信息

Pharmazie. 1995 Jan;50(1):25-6.

Abstract

The synthesis of three spin labeled derivatives of N-[N'-(chloroethyl)-N'-nitrosocarbamoyl] amino acids is reported. The new nitrosoureas are obtained by condensation of the corresponding N-[N'-(2-chloroethyl)-N'-nitrosocarbamoyl] amino acid with 2,2,6,6-tetramethyl-1-oxyl-4-aminopiperidine using dicyclohexylcarbodiimide. Their chemical structures are confirmed by elemental analysis, IR, MS, and EPR spectroscopy. All newly synthesized compounds showed high antitumour activity against the lymphoid leukemia L1210 in BDF1 mice.

摘要

报道了三种N-[N'-(氯乙基)-N'-亚硝基氨基甲酰基]氨基酸自旋标记衍生物的合成。通过相应的N-[N'-(2-氯乙基)-N'-亚硝基氨基甲酰基]氨基酸与2,2,6,6-四甲基-1-氧代-4-氨基哌啶使用二环己基碳二亚胺缩合得到新的亚硝基脲。通过元素分析、红外光谱、质谱和电子顺磁共振光谱确认了它们的化学结构。所有新合成的化合物对BDF1小鼠的淋巴白血病L1210均显示出高抗肿瘤活性。

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