Ruthenium‐Based Anticancer Compounds: Insights into Their Cellular Targeting and Mechanism of Action

Bis(bipyridine)ruthenium(II) Ferrocenyl β‐Diketonate Complexes: Exhibiting Nanomolar Potency against Human Cancer Cell Lines

“…Ruthenium( Ru) complexes have been frequently assessed as potentialc ancert herapeutics due to their air-stable synthesis, kinetic and thermodynamic stability,a nd the ease of modifying their ligand environments. [1,2] NAMI-A, (ImH)[trans-RuCl 4 (DMSO)(Im)] (Im = imidazole, Figure1A) was the first Ru compound to be studied in humans [3][4][5] and this drug was based on the findings by Keppler and co-workers, who highlighted that Ru III -azoles, for example, KP1019 (IndH)[trans-Ru-Cl 4 (Ind) 2 ]( Ind = indazole, Figure 1B), displayed anticancera ctivity in severala nimal models. [6,7] Unlike the clinicalP t-based drugs, NAMI-A is active against Lewis lung carcinoma, B16 melanoma and MCa mammary carcinoma, with increased cytotox-icity against xenograft studies.…”

Unprecedented inhibition of P-gp activity by a novel ruthenium-cyclopentadienyl compound bearing a bipyridine-biotin ligand

“…[5] During the last decade we have been developing new [RuCpR(PPh 3 )(bipyridine-R')] + (CpR = η 5 -C 5 H 5 or η 5 -C 5 H 4 (CH 3 ), R' = -H, -CH 3 , -CH 2 OH, -OC 3 H 6 -C 8 F 17 ) compounds as anticancer agents. [6][7][8][9][10][11][12][13] These compounds are highly cytotoxic against a wide panel of cancer cell lines with different degrees of aggressiveness, stable under physiologic conditions and their cell uptake and cellular distribution is dependent on the substituents of the bipyridine ligand. Recently we tested some of those compounds bearing 2,2'bipyridine-4,4'-subtituints as MDR inhibitors.…”