Abstract: A new synthetic method of bis (α-furancarboxylato) oxovanadium (BFOV) was developed with a yield of up to 93%. The content of barium ions remaining in the product was minimized to less than 10 mg/kg. The data of the element analysis and structural measurements were well consistent with the formulae VO(C₅H₃O₃)₂·2H₂O. The standard MTT assay was used to evaluate anticancer activity of BFOV against several human cancer cell lines, including lung and ovarian cancer cells (A549 and SKOV3) as well as their respective cisplatin-resistant cells (A549/DDP and SKOV3/DDP). Moreover, the effect of BFOV on human normal lung epithelial cells (Beas-2B) was determined also by using MTT assay. Its acute toxicity was also tested on mice. BFOV has a good water-solubility and water-stability. The biological tests reveal that BFOV is able to inhibit the growth of cancer cell A549 and SKOV3 and its anticancer activity is higher than or comparable to that of cisplatin as a control drug. More importanly, BFOV has greater potency on cisplatin-resistant A549/DPP, indicating it can overcome the resistance of these cancer cells to cisplatin. BFOV, a vanadium complex, displays much milder inhibitory effect than cisplatin. Furthermore, the acute toxicity of BFOV on mice, expressed in terms of LD₁₀ and LD₅₀, is also less than that of cisplatin.