Citation: Yan SU, Meng-Meng WANG, Hong-Ke LIU, Zhi SU. Synthesis and Antitumor Properties of Temozolomide-Based Platinum(Ⅳ) Complexes[J]. Chinese Journal of Inorganic Chemistry, ;2022, 38(3): 430-440. doi: 10.11862/CJIC.2022.044 shu

Synthesis and Antitumor Properties of Temozolomide-Based Platinum(Ⅳ) Complexes

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  • Temozolomide is the first-line anticancer drug for the clinical treatment of glioblastoma. In this work, temozolomide was chemically modified and introduced into the platinum(Ⅳ) complex. Two new Pt(Ⅳ) complexes P1T and P2T were successfully synthesized and characterized by 1H NMR and 13C NMR. The results show that both complexes had good lipid solubility with a fast hydrolysis rate. The anticancer activity and the mechanism of P1T and P2T were investigated with the MTT assay, flow cytometry, confocal imaging, and western blot. The results demonstrate that complexes P1T and P2T owned high cytotoxicity to glioma cell line A261, but low toxicity to normal nerve cell HT-22, indicating good cancer cell selectivity. Flow cytometry reveals that complexes P1T and P2T arrest the cell cycle in the G2/M phase, leading to DNA damage and ultimately inducing tumor cell apoptosis.
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