Otani T T, Briley M R
J Pharm Sci. 1978 Apr;67(4):520-6. doi: 10.1002/jps.2600670421.
A series of N-acetyl,-N-propionyl, and N-chloroacetyl derivatives of amino acids and amino acid analogs was tested for growth-inhibitory activity using a Lactobacillus casei system as a prescreen for possible antitumor activity. While none of the acetyl or propionyl derivatives of these amino acids and amino acid analogs caused any remarkable inhibition, certain chloroacetyl derivatives exhibited significant activity. The chloroacetyl derivatives, especially those of essential amino acids and of analogs of essential amino acids, showed modest, but pharmacologically significant, inhibition; those of nonessential amino acids exhibited no activity. When two such inhibitory acyl derivatives were combined in a single assay, the extent of inhibition was neither additive nor synergistic but was that of the more active of the two test components.
使用干酪乳杆菌系统作为可能的抗肿瘤活性的预筛选，测试了一系列氨基酸和氨基酸类似物的N - 乙酰基、N - 丙酰基和N - 氯乙酰基衍生物的生长抑制活性。虽然这些氨基酸和氨基酸类似物的乙酰基或丙酰基衍生物均未引起任何显著抑制，但某些氯乙酰基衍生物表现出显著活性。氯乙酰基衍生物，特别是必需氨基酸和必需氨基酸类似物的衍生物，表现出适度但具有药理学意义的抑制作用；非必需氨基酸的衍生物则无活性。当在单一试验中组合两种这样的抑制性酰基衍生物时，抑制程度既不是相加的也不是协同的，而是两种测试成分中活性较高者的抑制程度。
