1579305-77-3Relevant academic research and scientific papers
Synthesis, characterization, and antitumor activity of water-soluble (arene)ruthenium(II) derivatives of 1,3-dimethyl-4-acylpyrazolon-5-ato ligands. First example of Ru(arene)(ligand) antitumor species involving simultaneous Ru-N7(guanine) bonding and ligand intercalation to DNA
Caruso, Francesco,Monti, Elena,Matthews, Julian,Rossi, Miriam,Gariboldi, Marzia Bruna,Pettinari, Claudio,Pettinari, Riccardo,Marchetti, Fabio
, p. 3668 - 3677 (2014)
We report on the synthesis of novel water-soluble [(arene)Ru II(Q)Cl] and [(arene)RuII(Q)(X)]BF4 compounds (arene = p-cymene, benzene, hexamethylbenzene; HQ = 1,3-dimethyl-4-R-(C=O)-5- pyrazolone, HQMe, R = methyl, HQPh, R = phenyl, HQ Naph, R = naphthyl; X = H2O, 9-ethylguanine), and their in vitro antitumor activity toward the cell lines MCF7 (HTB-22, human breast adenocarcinoma), HCT116 (CCL-247, human colorectal carcinoma), A2780 (human ovarian carcinoma), A549 (CCL-185, human lung carcinoma), and U87 MG (HTB-1, human glioblastoma). The X-ray crystal structures of two complexes were determined. One of them, {chlorido-(p-cymene)-[(1,3-dimethyl-4-(1-naphthoyl)- pyrazolon-5-ato]ruthenium(II)}, was also studied with density functional theory methods and was selected for docking on a DNA octamer showing intercalation between DNA bases by the naphthyl moiety and for Ru-N7(guanine) bonding.
