Yin, Huanhuan; Dong, Jingjing; Cai, Yingchun; Shi, Ximeng; Wang, Hao; Liu, Guixia; Tang, Yun; Liu, Jianwen; Ma, Lei published the artcile< Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance>, Application of C16H22N2O3, the main research area is chalcone design synthesis anticancer reversers glycoprotein multidrug resistance; Chalcones; Inhibitors docking; Multidrug resistance reversers; P-glycoprotein inhibitors; Structure-activity relationship.
Overexpression of P-glycoprotein (P-gp) is one of the major causes for multidrug resistance (MDR), which has become a major obstacle in cancer therapy. One hopeful approach to reverse the MDR is to develop inhibitors of P-gp in expression and/or function. Here, we designed and synthesized a series of chalcone derivatives as P-gp inhibitors and evaluated their potential reversal activities against MDR. Among them, the most active compound I had little intrinsic cytotoxicity and showed the highest activity (RF = 50.19) in reversing DOX resistance in MCF-7/DOX cells. Further studies demonstrated that I could increase intracellular accumulation of DOX and inhibit expression of P-gp at mRNA and protein levels. More importantly, I significantly enhanced the efficacy of DOX against the tumor xenografts bearing MCF-7/DOX cells with the precondition of unchanged body weight Therefore, I might represent a promising lead to develop MDR reversal agents for cancer chemotherapy.
European Journal of Medicinal Chemistry published new progress about Antitumor agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Application of C16H22N2O3.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics