jm980434t_si_001.pdf (628.15 kB)
Synthesis of 1-(2-Aminophenyl)isoquinolines and the Biological Activity of Their cis-Dichloro Platinum(II) Complexes
journal contribution
posted on 1999-08-21, 00:00 authored by Franz von Nussbaum, Bernhard Miller, Stefan Wild, Christoph S. Hilger, Susanne Schumann, Haralabos Zorbas, Wolfgang Beck, Wolfgang SteglichThe broad biological effects of isoquinolines prompted us to use them as chelating, nonleaving
ligands in cis-platinum(II) antitumor complexes. The synthesis of several 1-(2-aminophenyl)isoquinoline derivatives with different levels of hydrogenation and varying substitution of the
phenyl ring is reported. These compounds constitute a new class of ligands for the synthesis
of oligocyclic platinum(II) complexes. In vitro cytotoxicity tests indicate that the most basic
amine ligands afford the most effective complexes. Two of the new complexes were more potent
against L1210 murine leukemia cells than the well-established antitumor compound cisplatinum.