143883-74-3Relevant academic research and scientific papers
Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors
Gu, Xiaoke,Ren, Zhiguang,Tang, Xiaobo,Peng, Hui,Zhao, Qing,Lai, Yisheng,Peng, Sixun,Zhang, Yihua
, p. 137 - 144 (2012/07/28)
Overexpression of P-glycoprotein (P-gp) is one of the major problems in successful treatment of cancers. To find new P-gp inhibitors, a series of bifendate (DDB) derivatives bearing dibenzo[c,e]azepine scaffold were synthesized and evaluated. Compound 4i more potently reversed P-gp-mediated multidrug resistance (MDR) than DDB and verapamil (VRP) by blocking P-gp mediated drug efflux function and increasing drug accumulation in K562/A02 MDR cells, and persisted longer chemo-sensitizing effect (>24 h) than VRP (6 h). Interestingly, unlike VRP, 4i showed no stimulation on the P-gp ATPase activity, suggesting it is not a substrate of P-gp. Given the low intrinsic cytotoxicity of 4i in vitro, it may represent a promising lead for developing therapeutics targeting P-gp-mediated MDR in combinational cancer chemotherapy.
Synthesis and antihepatotoxicity of some Wuweizisu analogues
Wu,Chen,Chang,Chen,Lee
, p. 353 - 358 (2007/10/02)
A preparation of dimethyl 4,4'-dimethoxy-5,6,5',6'-dimethylenedioxybiphenyl-2,2'-dicarboxylate (VII) was readily achieved. It provided the advantages of specificity, simplicity, and efficiency in reactions. 6-Phenyl-3,9-dimethoxy-1,2-methylenedioxy-10,11-methylenedioxy-6,7- dihydro-5H-dibenz(c, e)azepin (X) was successfully synthesized from VII (DDB) and its liver-protective property proved to be more effective than DDB and silymarin in the in vitro test of carbon tetrachloride-induced damage of primary cultured rat hepatocytes.
