Otani T T, Briley M R
J Pharm Sci. 1979 Apr;68(4):496-9. doi: 10.1002/jps.2600680428.
Eighteen trifluoroacetyl derivatives of amino acids and of amino acid analogs were prepared and tested for growth-inhibitory activity using a Lactobacillus casei system as a prescreen for antitumor activity. Of the compounds tested, the trifluoroacetyl derivatives of o-, m-, and p-fluorophenylalanine and of beta-3-thienylalanine showed modest activity; trifluoroacetyl derivatives of phenylalanine and of beta-2-thienylalanine showed marginal activity. The activity exhibited by the active trifluoroacetyl compounds was equal to that noted for most active chloroacetyl derivatives reported previously, as judged by comparison of their activity with that of chloroacetyl-m-fluorophenylalanine. No reversal of inhibition was noted when a representative of these inhibitors was challenged with a corresponding natural metabolite, both as a free amino acid and as a noninhibitory acylated compound.
制备了18种氨基酸及其类似物的三氟乙酰衍生物，并使用干酪乳杆菌系统作为抗肿瘤活性的预筛选方法，测试了它们的生长抑制活性。在所测试的化合物中，邻、间、对氟苯丙氨酸和β-3-噻吩丙氨酸的三氟乙酰衍生物表现出适度的活性；苯丙氨酸和β-2-噻吩丙氨酸的三氟乙酰衍生物表现出微弱的活性。通过将活性三氟乙酰化合物的活性与氯乙酰基间氟苯丙氨酸的活性进行比较判断，活性三氟乙酰化合物所表现出的活性与先前报道的大多数活性氯乙酰衍生物相当。当这些抑制剂中的一种代表物与相应的天然代谢物（以游离氨基酸和非抑制性酰化化合物两种形式）进行挑战时，未观察到抑制作用的逆转。
