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Development of new treatment strategies that target pathways involved in resistance of cancer cells is an attractive candidate to overcome therapeutic resistance. A series of complexes containing vanadium as a metal centers have shown to possess a wide spectrum of antitumor properties. These series belong to the non-platinum metal antitumor agents that appear to offer a different alternative for cancer chemotherapy. Vanadium complexes may exert its potential inhibitory effects on cancer cell through modulation of many cellular processes.