Abstract: Provided is an oral Pt(IV) anticancer prodrug containing a 3-bromopyruvate as an axial ligand, with a molecular formula of cis,trans,cis-[Pt(1R,2R-diaminocyclohexane)(OH)(3-bromopyruvate)(C2O4)]. It is a prodrug of oxaliplatin and 3-bromopyruvic acid is a small molecular glycolysis inhibitor. The prodrug is able to simultaneously act on DNA replication and glycolytic pathways of cancer cells, giving full play to the advantage of double-acting targets. The oral Pt(IV) anticancer prodrug is synthesized by using oxaliplatin as a starting material, performing axial oxidation with H2O2 and neutralizing the oxidized product with 3-bromopyruvic acid.

Abstract: Disclosed herein are methods of treatments with a telomerase-mediated telomere-targeting drug, 6-thio-2?-deoxyguanosine (6-thio-dG), checkpoint inhibitors and/or radiation therapy for treating cancers. eads to tumor regression in innate and adaptive immune-dependent manners in syngeneic and humanized mouse cancer models.