100412-70-2Relevant academic research and scientific papers
The key role of coligands in novel ruthenium(II)-cyclopentadienyl bipyridine derivatives: Ranging from non-cytotoxic to highly cytotoxic compounds
C?rte-Real, Leonor,Paula Robalo,Marques, Fernanda,Nogueira, Guilherme,Avecilla, Fernando,Silva, Tiago J.L.,Santos, Filipa C.,Isabel Tomaz,Helena Garcia,Valente, Andreia
, p. 148 - 159 (2015)
A new family of eight ruthenium(II)-cyclopentadienyl bipyridine derivatives, bearing nitrogen, sulfur, phosphorous and carbonyl sigma bonded coligands, has been synthesized. Compounds bearing nitrogen bonded coligands were found to be unstable in aqueous
Half-Sandwich Cyclopentadienylruthenium(II) Complexes: A New Antimalarial Chemotype
Florindo, Pedro R.,Fontinha, Diana,Gon?alves, Joana,Lobo, Lis,Lopes, Andreia,Lopes, Ricardo M. R. M.,M. Piedade, M. Fátima,Madureira, Margarida,Milheiro, Sofia A.,Moreira, Rui,Nogueira, Fátima,Pinto, Sandra N.,Prudêncio, Miguel
, p. 12722 - 12732 (2020/09/12)
A small library of half-sandwich cyclopentadienylruthenium(II) compounds of the general formula [(η5-C5R5)Ru(PPh3)(N-N)][PF6], a scaffold hitherto absent from the toolbox of antiplasmodials, was screened for activity against the blood stage of CQ-sensitive 3D7-GFP, CQ-resistant Dd2, and artemisinin-resistant IPC5202 Plasmodium falciparum strains and the liver stage of Plasmodium berghei. The best-performing compounds displayed dual-stage activity, with single-digit nanomolar IC50 values against blood-stage malaria parasites, nanomolar activity against liver-stage parasites, and residual cytotoxicity against HepG2 and Huh7 mammalian cells. The parasitic absorption/distribution of 7-nitrobenzoxadiazole-appended fluorescent compounds Ru4 and Ru5 was investigated by confocal fluorescence microscopy, revealing parasite-selective absorption in infected erythrocytes and nuclear accumulation of both compounds. The lead compound Ru2 impaired asexual parasite differentiation, exhibiting fast parasiticidal activity against both ring and trophozoite stages of a synchronized culture of the P. falciparum 3D7 strain. These results point to cyclopentadienylruthenium(II) complexes as a highly promising chemotype for the development of dual-stage antiplasmodials.
