A2780 human ovarian cancer

It was carried out according to Schwikkard et al. [9] and Actinomycin D was used as a positive control [ 16]. Cytotoxicity was determined against A2780 human ovarian cancer cells, using a microtiter plate assay. The plates were seeded with cells and... 

The inert hydroxo-bridged species were also a product of (very fast) hydrolysis of p-cymene osmium complexes with glycinate, L-alaninate, a-aminobutyrate and p-alaninate. However, complexes with picolinate as the chelating ligand, [Os(r 6-/> cym)Cl(pic)] 8 and [Os(r 6-biph)Cl(pic)] 9, with pyridine as /V-donor and carboxy-late as O-donor, hydrolyzed with half-lives of 0.20 and 0.52 h (298 K), and aqua adduct pKa values (pk L value for solutions in D20) of 6.67 and 6.33, respectively. Complexes 8 and 9 were cytotoxic towards A2780 human ovarian cancer cells, with IC50 values of 8 and 4.2 pM, respectively [64],... 

Figure 3.12 Antiproliferative activity (IC50 values) of the diastereoisomers [M(n V cym)(lmpyMe)l]PF6 (M = Ru, Os (/ )- or (S)-lmpyMe ligands) in the A2780 human ovarian cancer cell line.

In our initial studies [61], we found that Ru(II) arene complexes with three monodentate ligands [(ri -arene) Ru(X) (Y) (Z)], where X,Y or Z = halide, acetonitrile or isonicotinamide, were inactive towards A2780 human ovarian cancer cells in vitro. These complexes may be too reactive with components of the cell culture... 

Fig. 2.10 Five [(r -arene)Ru(en)Q complexes (arenes shown separately) for which activity against A2780 human ovarian cancer cells has been investigated [75. ...

We obtained [61] reproducible cytotoxicity against A2780 human ovarian cancer cells for chelated diamine complexes of the type [(r -arene)Ru(N,N)pC)] where N,N is typically ethylenediamine, and X is chloride (Fig. 2.10). Cells were incubated with the drug for 24 h, washed, and then the cell numbers were determined after growth on fresh medium for a further three days. 

Table 2.1 IC50 values for Ru(ll) arene complexes [(r -arene)Ru(X)(Y)(CI) A (A = PFg for positively-charged complexes) in A2780 human ovarian cancer cells after 24 h drug exposure, and comparison with carboplatin and cisplatin [75].

The complex [(q -benzene)Ru(proline)Cl] was reported [98] to have significant antitumor activity towards P388 leukemia in vivo but there appears to be no further report on this activity and we have found that similar amino acid complexes are inactive against A2780 human ovarian cancer cells [77]. 

SH-SY5Y neuroblastoma, cisplatin-sensitive A2780 and cispla-tin-resistant A2780cis human ovarian cancer cells was observed, but upon irradiation 7 strongly reduced the viability of the cancer cells (Fig. 8). In the A2780 cell line, the complex was 80x more toxic than cisplatin under identical conditions, and ca. 15 x more effective against the cisplatin-resistant A2780cis cell line (33). The trans diazido-Pt(IV) complex therefore has remarkable cytotoxic properties. 

Li Q, Gardner K, Zhang L et al. Cisplatin induction of ERCC-1 mRNA expression in A2780/CP70 human ovarian cancer cells. J Biol Chem 1998 273 23419-23425. 

Zheng LD, Tong QS, Wu CH. 2006. Growth inhibition and apoptosis inducing mechanisms of curcumin on human ovarian cancer cell line A2780. Chin J Integr Med 12 1. 

In more recent attempts to map the cellular distribution of cisplatin, Beretta et al. (50) incubated human ovarian cancer cells (A2780) with cisplatin concentrations of up to 100 xM for 30 minutes and observed electron dense spots, identified as large platinum deposits, distributed in the cell cytoplasm and nucleus. Additionally, it was observed that the platinum deposits made blunt contacts with the plasma membrane, which suggests that the cellular influx of cisplatin is through an endocytosis-independent manner that is consistent with the passive diffusion theory of cisplatin uptake (50). 

Nishiyama N, Nori A, Malugin A, Kasuya Y, Kopeckova P, Kopecek J. Free and N-(2-hydroxypropyl)methacrylamide copolymer-bound geldanamycin derivative induce different stress responses in A2780 human ovarian carcinoma cells. Cancer Res 2003 63(22) 7876-7882. 

Dyson and coworkers have reported the biological effect of dichlorido and oxalato derivatives of enantiomerically pure RAPTA-type ruthenium(II) complexes [14]. The enantiomers were synthesized by using a chiral arene (R)- or (S)-2-phenyl-iV-(l-phenylethylene)acetamide) as a ligand (Figure 3.9b). The cytotoxicity of all the epimers was evaluated in human ovarian cancer cells (A2780 and A2780cisR) with the S-enantiomers being more active than the R-enantiomers in both cell lines. Additionally, the dichlorido derivatives showed in vitro selectivity toward cancer cells over healthy HEK cells. 

Mohr and coworkers, inspired by the previous work on thiolato derivatives, combined the thiolato moieties with the NHC ligands (Figure 7.19) [20]. These complexes were studied with two human ovarian cancer cell lines (A2780S and... 

Sadler has focused on the synthesis of novel (arene)Ru(II) complexes with phenylazo-pyrazoles (Fig. 21.18) and on their cytotoxicity toward A2780 human ovarian or A549 human lung cancer cells. 

Bratasz et al. (2008) NO-NSAID/ cisplatin Human ovarian cancer (A2780 and cisplatin-resistant clone, A2780 cDDP) Cell viability (MTT) Reduced to 25% (NCX 4040,25 p,M -1- cisplatin) compared with 80% for cisplatin alone Human ovarian cancer xenograft (A2780cDDP) Growth delayed by 5 days compared with cisplatin alone (NCX 4040, 5 mg/kg, i.p. daily)... 

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