Otani T T, Briley M R
Res Commun Chem Pathol Pharmacol. 1983 May;40(2):321-4.
The fluoro-, chloro-, methoxy- and nitro-substituted benzoyl derivatives of m-fluoro-DL-phenylalanine, substituted singly at the ortho, meta or para position of the benzoyl phenyl ring, were prepared and tested for growth-inhibitory activity in a Lactobacillus casei system used as an antitumor prescreen. The substituted benzoyl derivatives that were previously found to be the most active for o-fluoro-DL-phenylalanine were also the most active for the m-fluoro-DL-phenylalanine. The position of the fluorine substituent in the phenylalanine also appeared to be important for inhibitory activity as the derivatives of m-fluoro-phenylalanine were in general better inhibitors than those of the corresponding o-fluorophenylalanine.
制备了间氟-DL-苯丙氨酸的氟代、氯代、甲氧基和硝基取代的苯甲酰衍生物，这些衍生物在苯甲酰苯环的邻位、间位或对位单取代，并在用作抗肿瘤预筛的干酪乳杆菌系统中测试其生长抑制活性。先前发现对邻氟-DL-苯丙氨酸最具活性的取代苯甲酰衍生物，对间氟-DL-苯丙氨酸也最具活性。苯丙氨酸中氟取代基的位置对抑制活性似乎也很重要，因为间氟苯丙氨酸的衍生物通常比相应的邻氟苯丙氨酸的衍生物是更好的抑制剂。
