Synthese und Antitumoraktivität neuer Porphyrin‐Platin(II)‐Komplexe mit an den Porphyrin‐Seitenketten gebundenem cytostatischen Platin‐Rest

Abstract

Synthesis and Antitumor Activity of New Porphyrin‐Platinum(II) Complexes with the Cytostatic Platinum Fragment Attached to the Porphyrin Side ChainsFifteen ligands of the porphyrin type, all derived from natural porphyrins, and their platinum(II) complexes, in which the Pt fragment is attached to the porphyrin side chains, were synthesized and characterized. Two different kinds of ligands were prepared: eight compounds with propionic acid substituents in the positions 6 and 7 of the porphyrin skeleton and seven ligands with 3‐aminopropyl side chains in the same positions. The ligands were transformed into eight diammine(dicarboxylato)platinum(II) complexes and into seven diaminedichloroplatinum(II) complexes. One of the water‐insoluble dichloroplatinum(II) compounds was converted into a water‐soluble complex by replacement of the chloride ligands by the lactate anion. The antitumor activity of the complexes was tested in vitro towards the MDA‐MB 231 mammary carcinoma cell line, and in vivo towards the P 388 leukemia of the mouse, the hormone‐independent MXT mammary carcinoma of the mouse and the Sarcoma 180 of the mouse. The best results in antitumor activity were obtained with diammine(dicarboxylato)platinum(II) complexes.