Synthesis of two maleimide derivatives of cis-configurated platinum (II) complexes for the preparation of chemoimmunoconjugates

Article abstract of DOI:10.1016/S0020-1693(97)05551-5

By attaching maleimide groups to anticancer drugs, derivatives are obtained which bind selectively to thiolated carrier proteins. Two maleimide ester derivatives of platinum(II) complexes which consist of an active cis-configurated platinum(II) moiety and a maleimide group capable of binding to thiolated carriers were prepared, i.e. N-(O-(3-maleimidobenzoyl)-2-hydroxyethyl)-1,2-diaminoethanedichloroplatinum(II) (7) and N-(O-(2-(4-maleimidophenyl)acetyl)-2-hydroxyethyl)-1,2- diaminoethanedichloroplatinum(II) (8). 7 and 8 were characterized through ¹H and ¹³C NMR spectroscopy, IR spectroscopy, elemental analysis and mass spectrometry (FAB).