Anticancer Activity of Picolinamide and Sulfur Chelated Pt(II) Complexes Against Breast Cancer: In Vitro Interaction...

Herein, picolinamide (pica) and sulfur chelated Pt(II) complexes were focused to investigate for their bioactivity and cytotoxic property. For better anticancer activity and less toxicity of Pt(II) complex, l-cysteine (L-cys) and N-acetyl-l-cysteine (N-acetyl-l-cys) were used to synthesize Pt(II) complexes. Complex [Pt(pica)(OH₂)₂](NO₃)₂, C-2 was obtained on hydrolysis of [Pt(pica)Cl₂], C-1. The complex [Pt(pica)(l-cys)]⁺; C-3 and [Pt(pica)(N-ac-l-cys)]; C-4 were synthesized from C-2 with thiols l-cys and N-ac-l-cys, respectively. The binding activity of Pt(II) complexes with DNA and BSA were performed for their binding mode and binding constants. The binding modes of the Pt(II) complexes were executed by electronic and fluorescence spectroscopic methods. Synchronous and 3D fluorescence spectroscopic investigations were performed to observe the insight interaction and conformational change of BSA, when interacts with the complex. The drug likeness property was conducted by PASS prediction and ADMET software programs. Molecular docking of the complexes was carried out with DNA, HSA, and HER-2 cancer protein. The cytotoxic activity of the complexes was tested on breast cancer cell lines; MCF-7, MDA MB-231 and normal human embryonic kidney HEK293T cells. Necrotic cell death mechanism was confirmed by Annexin-V-FITC/PI assay by flow cytometric method and the production of reactive oxygen species (ROS) was assessed through DCFDA assay.