New imidoyl-indazole platinum (II) complexes as potential anticancer agents: Synthesis, evaluation of cytotoxicity, cell death and experimental-theoretical DNA interaction studies.

摘要: Four new neutral N,N imidoyl-indazole ligands (L1, L3, L6, L7) and six Pt(II)-based complexes (C1-5 C7) were synthesized characterized by spectroscopic spectrometric techniques. Additionally, compounds L7, C3, C5 C7 analyzed using X-ray diffraction. An evaluation of cytotoxicity cell death in vitro for both was performed colorimetric assay flow cytometry, four cancer lines VERO cells as the control, respectively. Cytotoxicity selectivity demonstrated each compound dependent on line assayed. IC50 values C1-5 lower than those exhibited reference drug cisplatin, these general terms greater cisplatin three studied. In HL60 cells, C1 lowest almost five times more selective cisplatin. Flow cytometry results suggest that complex predominantly induced necrosis, its variant necroptosis, instead apoptosis all DNA binding assays, agarose gel electrophoresis UV-visible spectrophotometry studies, displayed a strong interaction only between C4 DNA. fact, theoretical calculations showed C4-DNA most thermodynamic favorable among study. Overall, induction independent-DNA-metal interactions possible Pt(II) anticancer agents.