Synthesis, characterization, and antitumor biological evaluation of novel fluorine‐containing platinum (IV) complexes

Abstract

A series of antitumor platinum (IV) complexes based on ammonia and fluoropyridine carrier groups with biotin and chloride ions as axial groups have been designed and synthesized in this paper. The structures of platinum (IV) complexes were fully characterized by 1H NMR, ESI‐MS, and IR. Such Pt (IV) complexes have certain tumor targeting properties, and the Pt (II) complexes released in the reducing microenvironment could combine with DNA. Compared with cisplatin, complexes S3 and S4 exhibited similar cytotoxicity against SW480, HCT116, and HepG2 cancer cell lines according to in vitro antitumor activity evaluation. Particularly, Complex S2 showed 1.5–3.0 times higher cytotoxicity than cisplatin and picoplatin against selected cell lines. According to the structure–activity relationship, the introduction of fluorine atoms and axial chloride has an important influence on the strong cytotoxic activity of Pt (IV) complex. In addition, the axial biotin molecule increased the targeting of the complex to tumor cells. Overall, the novel fluorine‐containing Pt (IV) complex S2 is an attractive antitumor lead compound with further research value.