Antitumor activity of titanocene amino acid complexes.
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].
Köpf-Maier
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Institut für Anatomie, Freie Universität Berlin, Germany.
Tornieporth-Oetting
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IC
D000596:Amino Acids / Q000737:chemistry*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001681:Biological Assay; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D005260:Female; D051379:Mice; D008958:Models, Molecular; D009942:Organometallic Compounds / Q000494:pharmacology*
D000596:Amino Acids; D000970:Antineoplastic Agents; D009942:Organometallic Compounds