title: 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: Faculty of Chemistry, Nicolaus Copernicus University, Gagarina 7, 87-100 Toruń, Poland. dziubek@umk.pl
authors: Iwona
authors: I
authors: Łakomska
authors: Marzena
authors: M
authors: Fandzloch
authors: Tadeusz
authors: T
authors: Muzioł
authors: Tadeusz
authors: T
authors: Lis
authors: Julia
authors: J
authors: Jezierska
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D001393:Azoles / Q000737:chemistry*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D018360:Crystallography, X-Ray; D006801:Humans; D008024:Ligands; D008968:Molecular Conformation; D011743:Pyrimidines / Q000737:chemistry*; D012428:Ruthenium / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D001393:Azoles; D056831:Coordination Complexes; D008024:Ligands; D011743:Pyrimidines; D012428:Ruthenium; C030986:pyrimidine