Köpf-Maier P, Tornieporth-Oetting I C
Institut für Anatomie, Freie Universität Berlin, Germany.
Biometals. 1996 Jul;9(3):267-71. doi: 10.1007/BF00817926.
Seven ionic titanocene alpha-amino acid (aa) complexes [(C5H5)2Ti(aa)2]2+[X]2- with aa = glycine, L-alanine, 2-methylalanine, D-L-phenylalanine, D,L-4-fluorophenylalanine and X = Cl or AsF6, were investigated for antitumor activity against fluid Ehrlich ascites tumor growing in CF1 mice. These complexes are the first stable model compounds of titanocene units with protein components, synthesized from a water-like, methanolic medium. All titanocene amino acid complexes induced antitumor activity which was manifested by maximum cure rates ranging from 30 to 70% and increases in life span from 78 to 276% in comparison with untreated control animals. The complexes containing chloride as anion X were more effective than the hexafluoroarsenate derivatives, which surprisingly showed a low substance toxicity. In all cases, the antitumor activity of the ionic titanocene amino acid complexes tested was less pronounced than that of the neutral parent compound [(C5H5)2TiCl2].
研究了七种离子型二茂钛α-氨基酸（aa）配合物[(C5H5)2Ti(aa)2]2+[X]2-，其中aa分别为甘氨酸、L-丙氨酸、2-甲基丙氨酸、D-L-苯丙氨酸、D,L-4-氟苯丙氨酸，X为Cl或AsF6，考察了它们对CF1小鼠体内生长的艾氏腹水瘤的抗肿瘤活性。这些配合物是由类似水的甲醇介质合成的，是首批含有蛋白质成分的二茂钛单元的稳定模型化合物。所有二茂钛氨基酸配合物均诱导出抗肿瘤活性，与未处理的对照动物相比，最大治愈率在30%至70%之间，寿命延长78%至276%。含氯离子作为阴离子X的配合物比六氟砷酸盐衍生物更有效，令人惊讶的是，六氟砷酸盐衍生物显示出较低的物质毒性。在所有情况下，所测试的离子型二茂钛氨基酸配合物的抗肿瘤活性均不如中性母体化合物[(C5H5)2TiCl2]明显。
