Novel Mononuclear Ruthenium(II) Compounds in Cancer Therapy

Antitumor effectiveness and mechanism of action of Ru(II)/amino acid/diphosphine complexes in the peritoneal carcinomatosis progression

“…Treatment of the mice led to an MST of 21 days (p > 0.05) and an ILS of 17% (Table 4), which were not effective for prolonging the life span. Progression of Ehrlich carcinoma has been reported in the literature by means of hematological changes, such as a decrease in Hb and the erythrocyte count, 15,25,39 and the same were observed in our data (Table 2). The values of erythrocytes, Hb, and HCT obtained from the negative control and vehicle groups were reduced, when compared to values for Swiss male tumor-free mice (Table 2).…”

“…Prolongation of an animal's life span has been considered a reliable criterion for the antitumor efficacy of new prototypes. 15,39 In this study, the clinical symptoms and hematological, biochemical, and histopathological parameters were analyzed to evaluate possible toxicological effect from treatment in EAC-beating mice. The treatment with complexes 1 and 2 did not induce any behavioral change, signs of toxicity, or animal deaths during the evaluation of antitumor activity.…”

“…10 They show less toxicity, they are selective of tumor cells, and present a novel mechanism of action, the prospect of non-cross-resistance and a different spectrum of activity. [11][12][13][14][15][16][17][18][19] In a previous study, we recently reported that complexes with the general formula [Ru(AA-H)(dppb)(bipy)] PF 6 (AA-H = amino acid anion) inhibited the growth of Ehrlich carcinoma cells in vitro. 20 Among the Ru(II)/ amino acid/diphosphine complexes evaluated, those with l-methionine and l-tryptophan present the best activity against Ehrlich carcinoma cells, with IC 50 values (concentration that results in a 50% reduction in cellular viability) of 10.2 ± 2.3 µM and 8.7 ± 3.1 µM, respectively.…”

“…10 They show less toxicity, they are selective of tumor cells, and present a novel mechanism of action, the prospect of non-cross-resistance and a different spectrum of activity. 11–19…”

ComparativeIn VitroBinding Studies of TiCl2(dpme)2, Ti(ada)2(bzac)2, and TiCl2(bzac)(bpme) Titanium Complexes with Calf-Thymus DNA

“…It acts by forming covalent bonds with nucleophilic N7-sites of purine bases in DNA, exposed in the major groove of the double helix of DNA [ 8 ]. But due to its side effects, many efforts have been made worldwide to synthesize new novel nonplatinum anticancer drugs [ 9 – 12 ] with the hope of discovering new class of drugs with better chemotherapeutic effects and reduced side effects. After cisplatin the first nonplatinum anticancer drugs were titanium based budotitane and titanocene dichloride [ 13 ].…”