Synthesis and Biological Activity of Benzopyranyl Urea and Benzopyranyl Thiourea Derivatives as MDR Reversal Agents

摘要

Most cancer patients are subjected to chemotherapy for the treatment of advanced cancers. However, most metastatic solid tumors eventually remain incurable even by treatment with recent anti-cancer drugs. Occurrence of multidrug resistance (MDR) during the course of treatment has been reported as the main factor responsible for the failure of chemotherapy. Although there may be many factors that allow cancer cells to acquire resistance, a significant molecular event of MDR induces the overexpression of ATP-binding cassette (ABC) transporters, such as ABCB1 (P-glycoprotein, P-gp), ABCC1-7 (multidrug resistant related protein 1-7, MRP 1-7) and ABCG2 (breast cancer resistance protein, BCRP), which are responsible for the efflux of a wide range of anticancer drugs.