BCRP/ABCG2, a second member of ABC transporter subclass G, has been shown to be overexpressed in several solid tumors, acute myelogenous leukemia and chronic myeloid leukemia. A variety of chemically unrelated anticancer drugs have been found to be transported by ABCG2 leading to their lower intracellular accumulation and hence causing chemoresistance. Until now several efforts have been taken to identify potent and selective inhibitors of ABCG2. Recent studies carried out to deign BCRP inhibitors have been able to point out the effect of the substitution pattern in compound scaffolds on the potency, selectivity and cytotoxicity of ABCG2 inhibitors.