73292-99-6Relevant academic research and scientific papers
Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance
Yin, Huanhuan,Dong, Jingjing,Cai, Yingchun,Shi, Ximeng,Wang, Hao,Liu, Guixia,Tang, Yun,Liu, Jianwen,Ma, Lei
, p. 350 - 366 (2019/07/19)
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 MY3 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 MY3 could increase intracellular accumulation of DOX and inhibit expression of P-gp at mRNA and protein levels. More importantly, MY3 significantly enhanced the efficacy of DOX against the tumor xenografts bearing MCF-7/DOX cells with the precondition of unchanged body weight. Therefore, MY3 might represent a promising lead to develop MDR reversal agents for cancer chemotherapy.
Synthesis of a natural chalcone and its prenyl analogs - Evaluation of tumor cell growth-inhibitory activities, and effects on cell cycle and apoptosis
Neves, Marta P.,Lima, Raquel T.,Choosang, Kanthima,Pakkong, Panee,De Sao Jose Nascimento, Maria,Vasconcelos, M. Helena,Pinto, Madalena,Silva, Artur M. S.,Cidade, Honorina
experimental part, p. 1133 - 1143 (2012/09/22)
Six prenyl (= 3-methylbut-2-en-1-yl) chalcones (=1,3-diphenylprop-2-en-1- ones), 2-7, and one natural non-prenylated chalcone, 1, have been synthesized and evaluated for their in vitro growthinhibitory activity against three human tumor cell lines. A pron
