Novel fluorinated platinum(II) complexes with pyridine-2-carboxylate ligand as potent radiosensitizer and antiviral agent

• Published in: Inorganic chemistry communications Vol. 94; pp. 92 - 97
• Main Authors: Zhang, Xiaoxiao, Wang, Fang, Zhang, Chao, Wu, Shuang, Zheng, Xuyang, Gong, Tuotuo, Ding, Ruike, Chen, Kai, Bai, Dan
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.08.2018
• Subjects: Antiviral agent; Pt(II) complex; Radiochemotherapy (RT-CT); Radiosensitizer; Radiosensitizer; Antiviral agent; Radiochemotherapy (RT-CT); Pt(II) complex
• ISSN: 1387-7003; 1879-0259
• DOI: 10.1016/j.inoche.2018.06.013

Novel Pt(II) complexes, (TFPPy)PtPic and (TFPQ)PtPic, containing fluorinated phenylpyridine or phenylquinoline with pyridine-2-carboxylate as chelating ligands were synthesized according to rational design, their therapeutical activities examined. Remarkable radiosensitization SER values were observed even in radio-resistant cell line after treated with these complexes. Furthermore, the two complexes have shown antiviral activity against DNA virus HSV-1. Comply with live cell imaging results, molecular docking have revealed the complexes forms stable hydrogen bond and hydrophobic interactions to the minor groove of target DNA double helix. These findings demonstrate the non-classical structure complexes are promising for further evaluation as a new type of prodrug radiochemotherapy and antiviral treatment. [Display omitted] •Two novel Pt complexes with fluorinated inactive leaving group synthesized.•Both complexes exhibit radiation sensitivity enhancement and antiviral functionality.•Proposed DNA strand targeting and cell phase arrest mechanism proven.