Structural and Biological Studies of Pt(II) and Pd(II) Complexes derived from Pyrrole-2-carboxaldehyde-4N-p-chlorophenylthiosemicarbazone

NAVARRO RANNINGER C; MATESANZ A; RUIZ M.C; LEON I.E; GOMEZ-QUIROGA A.

Bombay

Simposio; 14th International Symposium on Metal Ions in Biology and Medicine and 4th Green Health Conference EMail Print Conferences; 2016

Being cisplatin one of the most active antitumor chemotherapeutic agents, for a long time the research in the area has been characterized by the similarity of new drug candidates to cisplatin and therefore pointing directly to the DNA as the primary target. However the clinical utility of cisplatin is restricted by its nonspecific biodistribution and severe side effects and current research is focused on the development of novel metallo-drugs that are able to interact with specific biological targets. In this regard, thiosemicarbazones and their metal complexes have emerged as new class of compounds targeting RR enzyme, crucial for tumor cell division. As part of our systematic investigations in the field of metal-based anticancer drug design, two new Pt(II) and Pd(II) thiosemicarbazone complexes have been synthesized and characterized. The crystal structure of the palladium derivative reveals that the metal center adopts a square-planar geometry with two deprotonated ligands coordinated through the nitrogen and sulphur atoms in a trans arrangement. The biological activity of these compounds has been evaluated by examining their ability to bind CT-DNA and HEWL. Their antiproliferative activity has been screened in vitro against four cell lines: L929 (normal mouse fibroblast) A-549 (human lung cancer), MG-63 (human osteosarcoma) y Jurkat (human leukemia).