Suami T, Kato T, Takino H, Hisamatsu T
J Med Chem. 1982 Jul;25(7):829-32. doi: 10.1021/jm00349a012.
Fourteen (2-chloroethyl)nitrosourea congeners of L-amino acid amides have been synthesized as potential antineoplastic agents. Almost all the congeners tested were found to be highly active against experimental leukemia L1210 in mice. The chemical decomposition rates of the congeners were measured in a buffered solution (pH 7.4) at 37 degrees C. Acute toxicities of some of the congeners were determined for mice. The congener of sarcosinamide shows the longest half-life (T0.5 = 329.7 min) and the lowest toxicity, LD50 = 392.0 mg/kg (ip) and 426.6 mg/kg (iv), in this series.
已合成了十四种L-氨基酸酰胺的（2-氯乙基）亚硝基脲类似物作为潜在的抗肿瘤药物。几乎所有测试的类似物对小鼠实验性白血病L1210都具有高活性。在37℃的缓冲溶液（pH 7.4）中测量了这些类似物的化学分解速率。测定了其中一些类似物对小鼠的急性毒性。在该系列中，肌氨酸酰胺类似物显示出最长的半衰期（T0.5 = 329.7分钟）和最低的毒性，腹腔注射LD50 = 392.0 mg/kg，静脉注射LD50 = 426.6 mg/kg。
