Synthesis of new ethylenediamine-platinum(II) complexes starting from amino acids and their antitumor activity

Amino acids, obtained by azlactone or hydantoin synthesis were converted to ethylenediamines RCH2CH(NH2)CH2NH2 via esters, amides, and LiAlH4 redn. Pt complexes I were prepd. from these diamines and tested for antitumor activity with the hormone independent human mammary carcinoma cell line MDA-MB 231 along with I complexes with Cl ligands replaced by a series of monodentate and bidentate anions. All compds. tested had high antitumor activity in the inhibition of cell proliferation and 3H-thymidine incorporation tests. Chloro-substituted Ph I derivs. were the most active substances. Replacement of chloro ligands in DL-I (R = Ph) [104975-44-2] by, other leaving groups led to complexes exhibiting higher or lower activity with PhCH2CH(NH2)CH2NH2.Pt (H2O)2(NO3)2 having the most activity. Of the bidentate ligand-contg. compds. PhCH2CH(NH2)CH2NH2.Pt.malonate was the most active