As associated with tumor progression, metastasis and resistance to treatment, HIF-1α inhibitors have shown great promise in cancer therapy.20–23 1-Benzyl-3-(5′-hydroxymethyl-2′-furyl)indazole (YC-1), an effective HIF-1α inhibitor, can inhibit the overexpression of HIF-1α induced by hypoxia, thus exerting a potent antitumor effect.24,25 Based on the above, we attempted to develop a bifunctional prodrug, which contains both a hypoxia-activated prodrug and a hypoxia-targeted inhibitor (YC-1) in a small-molecule entity. This evidence concerns the gene HIF1A and cancer.