Synthesis, characterization and antitumor activity of quinolone-platinum(II) conjugates

Abstract

A new series of quinolone-platinum(II) conjugates, [Pt(Q'-NH2)(dmso)X-2] and cis-[Pt(Q"-en)X-2], where Q' and Q" are quinolones (flumequine, nalidixic acid or oxolinic acid) linked to monodentate and bidentate amine ligands, respectively, and X-2 is Cl-2 or 1,1-cyclobutanedicarboxy late, have been synthesized with the aim of examining the synergetic antitumor activity of quinolone intercalation and platinum(II) chelation. The complexes were characterized by elemental analyses and IR and multinuclear (H-1 and Pt-195) NMR spectroscopies, and then subjected to in vitro and in vivo bioassays using the leukemia L1210 cell line. (C) 2001 Elsevier Science B.V. All rights reserved.