Novel gallium(III) complexes containing phthaloyl derivatives of neutral aminoacids with apoptotic activity in cancer cells

Anticancer Applications and Recent Investigations of Metallodrugs Based on Gallium, Tin and Titanium

“…Comparing the results of cytotoxicity with gallium(III) nitrate, the compounds 1 and 2 presented a higher antiproliferative effect. Both complexes present similar IC 50 values in all the studied cell lines (Table 1) [24].…”

“…However, a more in depth study of compound 21 against HeLa and Fem-x cell showed the induction of an apoptotic cell death [37]. In another study, our group prepared tetraorganotin(IV) compounds containing cyclopentadienyl ligands (22)(23)(24)(25) which were prepared by the simple transmetallation reaction of lithium cyclopentadienide derivatives with SnPh 3 Cl (Scheme 3) [38]. All the compounds were isolated as single isomers even though the position of the double bonds makes possible the formation of a mixture of positional isomers.…”

“…Tin(IV) complexes (22)(23)(24)(25) were tested in vitro against 8505C, A253, A549, A2780, and DLD-1 cell lines by using the sulforhodamine-B microculture colorimetric assay (Table 3) [39]. All the compounds showed a dose-dependent antiproliferative effect toward cell lines and presented lower IC 50 Tin(IV) complexes (22)(23)(24)(25) were tested in vitro against 8505C, A253, A549, A2780, and DLD-1 cell lines by using the sulforhodamine-B microculture colorimetric assay (Table 3) In a subsequent study, a series of rare ionic triphenyltin(IV) chloride carboxylate complexes (26-28, Figure 8) was synthesized and tested against 8505C, A253, A549, A2780, and DLD-1 cell lines (Table 3).…”

“…All the compounds showed a dose-dependent antiproliferative effect toward cell lines and presented lower IC 50 Tin(IV) complexes (22)(23)(24)(25) were tested in vitro against 8505C, A253, A549, A2780, and DLD-1 cell lines by using the sulforhodamine-B microculture colorimetric assay (Table 3) In a subsequent study, a series of rare ionic triphenyltin(IV) chloride carboxylate complexes (26-28, Figure 8) was synthesized and tested against 8505C, A253, A549, A2780, and DLD-1 cell lines (Table 3). All the ionic tin(IV) compounds presented anticancer activities up to 50 times more active than those of cisplatin (for example in DLD-1 complex 26 has an IC50 value of 0.103 µM compared to that of cisplatin of 5.14 µM).…”

Metallomics related to gallium compounds: biochemical and xenobiochemical aspects

“…In vitro studies performed on cell cultures revealed that certain Ga complexes induce effects similar to apoptosis in which the genomic DNA is fragmented. The resulting genomic DNA fragments with lengths of 180 bp (base pairs), or multiples of this, are considered characteristic of the dimension of the nucleosome in the DNA-histone complex [36]. At low ionic concentrations Ga 3+ can bind to phosphate groups in the DNA macromolecule forming stable complexes, with no binding to nucleobases.…”