Synthesis, characterization and antitumor properties of two highly cytotoxic ruthenium(iii) complexes with bulky triazolopyrimidine ligands.

Abstract

Two ruthenium(III) complexes composed of 5,7-ditertbutyl-1,2,4-triazolo[1,5-a]pyrimidine (dbtp) ligands were prepared and structurally characterized by X-ray crystallography, IR, UV-Vis, EPR spectroscopies and cyclic voltammetry (CV). The crystal structures of trans-[RuCl(3)(H(2)O)(dbtp)(2)] 1 and mer-[RuCl(3)(dbtp)(3)]·0.815OCMe(2) 2 showed slightly distorted octahedral geometries with two 1 or three 2 monodentate dbtp ligands bound in a head-to-head orientation. In both complexes, the heterocyclic dbtp ligands were bound to the ruthenium(III) ion through the N3 nitrogen atom. A cytotoxicity assay of both ruthenium(III) compounds against two human cell lines (A549 - non-small cell lung carcinoma and T47D - breast carcinoma) was performed. The ruthenium(III) complexes showed excellent cytotoxicity with IC(50) values in the range of 0.02-2.4 μM against both cancer cell lines. In addition, the in vitro cytotoxic values of the ruthenium(III) compounds were 35-times for 1 and 172-times for 2 higher against T47D than the clinically used antitumor drug cisplatin.

• Authors: Iwona Łakomska, Marzena Fandzloch, Tadeusz Muzioł, Tadeusz Lis, Julia Jezierska
• Journal: Dalton transactions (Cambridge, England : 2003) (Dalton Trans) Vol. 42 Issue 17 Pg. 6219-26 (May 07 2013) ISSN: 1477-9234 [Electronic] England
• PMID: 23328694 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Azoles
• Coordination Complexes
• Ligands
• Pyrimidines
• Ruthenium
• pyrimidine

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, toxicity)
• Azoles (chemistry)
• Cell Line, Tumor
• Cell Survival (drug effects)
• Coordination Complexes (chemical synthesis, chemistry, toxicity)
• Crystallography, X-Ray
• Humans
• Ligands
• Molecular Conformation
• Pyrimidines (chemistry)
• Ruthenium (chemistry)