Modulating the antitumoral activity by the design of new platinum(II) compounds: Synthesis, characterization, DFT, ultrastructure and mechanistic studies

A novel star-shaped trinuclear platinum(ii) complex based on a 1,3,5-triazine core displaying potent antiproliferative activity against TNBC by the mitochondrial injury and DNA damage mechanism

“…S4 and S13†), also suggesting that the phenol groups were deprotonated. 46 The result confirmed the formation of the trinuclear platinum( ii ) complex and the coordinated chlorides in the complex could be dissociable in solution, which may be essential for the binding to DNA bases. The molar conductivity of the complex ( Λ M ) in DMF at room temperature is 63 S cm 2 mol −1 , which falls within the range of non-electrolytes.…”

“…S8 and S9†), suggesting that the phenol group is deprotonated and it is coordinated to the Pt II centre as phenolate. 46 The molar conductivity of the complex ( Λ M ) in DMF at room temperature is 60 S cm 2 mol −1 , which falls within the range of non-electrolytes and suggests that one chloride ion is present in the inner sphere of the complex rather than the outer sphere. 47 So the probable structure of 2 is shown in Scheme 1.…”

In Vitro and In Vivo Relevant Antineoplastic Activity of Platinum(II) Complexes toward Triple-Negative MDA-MB-231 Breast Cancer Cell Line

“…The platinum(II) complexes were synthesized and characterized as previously reported, and their structures are presented in Scheme 1 [ 24 ]. For in vitro testing, stock solutions (20 mM) of the platinum(II) complexes and of the ligands were prepared in dimethyl sulfoxide (DMSO).…”

“…Our group has been evaluating the cytotoxic activities of a series of coordination compounds containing different metal ions both in vitro and in vivo [ 20 , 21 , 22 , 23 , 24 ]. We previously showed the synthesis, characterization, and cytotoxic activity of four complexes containing platinum(II) as a metallic coordinating center ( Scheme 1 ), where treatment against U937 cell line with complex ( 3 ) [Pt(HL3)Cl]·H 2 O could induce the activation of both intrinsic and extrinsic apoptotic cascades, as well as perturbations in cell cycle and dysfunction of mitochondrial membrane potential [ 24 ]. Aiming to advance this field, we decided to investigate the antineoplastic activity of the Pt(II) complexes ( 3 ) and ( 4 ), since the higher activities exhibited by these complexes seem to be related to the presence of the α- and β-naphthyl groups in the ligand structure [ 24 ].…”

“…We previously showed the synthesis, characterization, and cytotoxic activity of four complexes containing platinum(II) as a metallic coordinating center ( Scheme 1 ), where treatment against U937 cell line with complex ( 3 ) [Pt(HL3)Cl]·H 2 O could induce the activation of both intrinsic and extrinsic apoptotic cascades, as well as perturbations in cell cycle and dysfunction of mitochondrial membrane potential [ 24 ]. Aiming to advance this field, we decided to investigate the antineoplastic activity of the Pt(II) complexes ( 3 ) and ( 4 ), since the higher activities exhibited by these complexes seem to be related to the presence of the α- and β-naphthyl groups in the ligand structure [ 24 ]. Therefore, in these studies, we selected a panel of five cancer cells (MDA-MB-231, MCF7, A549, PC-3, and BXPC-3) and normal cells (PBMC); then, after identifying the most cytotoxic complex, we analyzed its effects on the underlying mechanisms of cell death.…”