New porphyrin platinum conjugates for the cytostatic and photodynamic tumor therapy

The combination of a porphyrin system and a platinum fragment in the same molecule should not only result in the additivity of the photodynamic activity of the porphyrin and the cytostatic activity of the platinum, but also in the enrichment of the porphyrin platinum conjugate in tumors, which platinum compounds alone do not show. New porphyrin platinum conjugates were obtained from the platinum complexes of a series of 1,2-diamines and hematoporphyrin or 13,17-bis(2-carboxyethyl)-3,8-bis [1-(ethyleneglycolmonoethylether)oxvethyl]-2,7,12,18-tetramethylporphin. The 1,2-diamines were synthesized starting from the corresponding stilbenes via 1,2-diazides. The new platinum porphyrin conjugates showed promising antitumor activity in tests with the mammary carcinoma cell line MDA-MB-231. (C) 2003 Elsevier Science B.V. All rights reserved.