Pt(II) complexes with different N-donor aromatic ligands for specific inhibition of telomerase

A number of cis-dichloroplatinum(II) derivatives containing aromatic N-dono r ligands such as pyridine and/or 5-substituted isoquinolines have been syn thesized and fully characterized, with particular use of Raman spectroscopy and mass spectrometry. These complexes have been tested for specific inhib ition of telomerase, which could represent a selective target for cancer ch emotherapy. The screening of such potential drugs has been performed by a b iochemical assay on the isolated enzyme, It is noteworthy that the cis -[Pt Cl2(pyridine)(5-SO3H-isoquinoline)] compound exhibited remarkable telomeras e inhibition at a concentration as low as 10(-7) M. (C) 2000 Elsevier Scien ce S.A. All rights reserved.