Abstract
Under microwave irradiation, eighteen new aroylhydrazone diorganotin complexes (1a–9b) were produced through the reaction of aroylhydrazine, 2-ketobutyric acid, and the corresponding diorganotin. Fourier transform infrared spectroscopy, 1H, 13C, and 119Sn nuclear magnetic resonance spectroscopies, high-resolution mass spectroscopy, X-ray crystallography, and thermogravimetric analysis (TGA) were performed to characterize the complexes. The in vitro anticancer activity for complexes were assessed using a CCK-8 assay on human cancer cells of HepG2, NCI-H460, and MCF-7. Complex 4b revealed more intensive anticancer activity against MCF-7 cells than the other complexes and cisplatin. Flow cytometry analysis and transmission electron microscope observation demonstrated that complex 4b mediated cell apoptosis of MCF-7 cells and arrested cell cycle in S phase. Western blotting analysis showed that 4b induced DNA damage in MCF-7 cells and led to apoptosis by the ATM-CHK2-p53 pathway. The single cell gel electrophoreses assay results showed that 4b induced DNA damage. The DNA binding activity of 4b was studied by UV–Visible absorption spectrometry, fluorescence competitive, viscosity measurements, gel electrophoresis, and molecular docking, and the results show that 4b can be well embedded in the groove and cleave DNA.
Highlights
During the last few years, it has been noticeable that organotin compounds occupy an important place in cancer chemotherapy reports [15–17] because of their cytotoxic effects, ability to bind with DNA, anti-proliferating nature, and apoptotic-inducing nature
Complexes 1a–9b were synthesized by the microwave-assisted method
As indicated by the data, 4b can mediate MCF-7 cancer cell apoptosis, which is consistent with the strong anticancer activity in 4b
Summary
As standards of living have increased, the incidence and mortality of cancer have increased gradually. During the last few years, it has been noticeable that organotin compounds occupy an important place in cancer chemotherapy reports [15–17] because of their cytotoxic effects, ability to bind with DNA, anti-proliferating nature, and apoptotic-inducing nature. During the research and development of anticancer drugs, the growth inhibition experiment of drugs in vitro cancer cells is the first step in verifying the drug anticancer effects It is significant in clarifying drug anticancer spectrums and screening efficient anticancer drugs. Group studied the structure–activity relationships of new organotin (IV) anticancer agents and their cytotoxicity profile on HL-60, MCF-7, and HeLa human cancer cell lines [22]. Due to its good biological properties, and electron-donating atoms such as carbonyl oxygen and imino nitrogen, aroylhydrazone ligands have received extensive attention in the design of organotin anticancer drugs [23–26].
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