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

摘要

A number of cis-dichloroplatinum(II) derivatives containing aromatic N-donor ligands such as pyridine and/or 5-substituted isoquinolines have been synthesized and fully characterized, with particular use of Raman spectroscopy and mass spectrometry. These complexes have been tested for specific inhibition of telomerase, which could represent a selective target for cancer chemotherapy. The screening of such potential drugs has been performed by a biochemical assay on the isolated enzyme, It is noteworthy that the cis -[PtCl2(pyridine)(5-SO3H-isoquinoline)] compound exhibited remarkable telomerase inhibition at a concentration as low as 10(-7) M. (C) 2000 Elsevier Science S.A. All rights reserved. [References: 25]