1. Arene Ru(II) Complexes Acted as Potential KRAS G-Quadruplex DNA Stabilizer Induced DNA Damage Mediated Apoptosis to Inhibit Breast Cancer Progress.
- Author
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Qian J, Liu R, Liu N, Yuan C, Wu Q, Chen Y, Tan W, and Mei W
- Subjects
- DNA Damage, Female, Humans, MCF-7 Cells, Molecular Docking Simulation, Phenanthrolines chemistry, Phenanthrolines pharmacology, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Apoptosis, Breast Neoplasms drug therapy, G-Quadruplexes, Proto-Oncogene Proteins p21(ras) genetics, Ruthenium chemistry, Ruthenium pharmacology
- Abstract
A series of arene Ru(II) complexes, [( η
6 -MeC6 H5 )Ru(L)Cl]Cl, (L= o -ClPIP, 1 ; m -ClPIP, 2 and p -ClPIP, 3 ) ( o -ClPIP=2-(2-chlorophenyl)imidazo[4,5-f][1,10]phenanthroline; m -ClPIP=2-(4-chlorophenyl)imidazo[4,5-f][1,10]phenanthroline) was synthesized and investigated as a potential apoptosis inducer in chemotherapy. Spectroscopy and molecular docking simulations show that p -ClPIP=2-(4-chlorophenyl)imidazo[4,5-f][1,10]phenanthroline) was synthesized and investigated as a potential apoptosis inducer in chemotherapy. Spectroscopy and molecular docking simulations show that 1 exhibits moderated binding affinity to KRAS G-quadruplex DNA by groove mode. Further, in vitro studies reveal that 1 displays inhibitory activity against MCF-7 growth with IC50 can induce the apoptosis of MCF-7 cells and G0/G1 phase arrest through DNA damage. In summary, the prepared arene Ru(II) complexes can be developed as a promising candidate for targeting G-quadruplex structure to induce the apoptosis of breast cancer cells via binding and stabilizing 1 can induce the apoptosis of MCF-7 cells and G0/G1 phase arrest through DNA damage. In summary, the prepared arene Ru(II) complexes can be developed as a promising candidate for targeting G-quadruplex structure to induce the apoptosis of breast cancer cells via binding and stabilizing KRAS G-quadruplex conformation on oncogene promoter.- Published
- 2022
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