13208-61-2Relevant academic research and scientific papers
Design, Biological Evaluation, and Molecular Modeling of Tetrahydroisoquinoline Derivatives: Discovery of A Potent P-Glycoprotein Ligand Overcoming Multidrug Resistance in Cancer Stem Cells
Riganti, Chiara,Contino, Marialessandra,Guglielmo, Stefano,Perrone, Maria G.,Salaroglio, Iris C.,Milosevic, Vladan,Giampietro, Roberta,Leonetti, Francesco,Rolando, Barbara,Lazzarato, Loretta,Colabufo, Nicola A.,Fruttero, Roberta
, p. 974 - 986 (2019)
P-Glycoprotein is a well-known membrane transporter responsible for the efflux of an ample spectrum of anticancer drugs. Its relevance in the management of cancer chemotherapy is increased in view of its high expression in cancer stem cells, a population of cancer cells with strong tumor-promoting ability. In the present study, a series of compounds were synthesized through structure modulation of [4′-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-ylmethyl)biphenyl-4-ol] (MC70), modifying the phenolic group of the lead compound. Among them, compound 5b emerged for its activity against the transporter (EC50 = 15 nM) and was capable of restoring doxorubicin antiproliferative activity at nontoxic concentration. Its behavior was rationalized through a molecular modeling study consisting of a well-tempered metadynamics simulation, which allowed one to identify the most favorable binding pose, and of a subsequent molecular dynamics run, which indicated a peculiar effect of the compound on the motion pattern of the transporter.
Activated Carbamate Reagent as Derivatizing Agent for Amino Compounds in High-Performance Liquid Chromatography
Nimura, Noriyuki,Iwaki, Kazuo,Kinoshita, Toshio,Takeda, Kazuyoshi,Ogura, Haruo
, p. 2372 - 2375 (2007/10/02)
Activated carbamate reagents were developed for the determination of amino compounds.The reagents, succinimido carbamates, were easily prepared by the reaction of disuccinimido carbonate (DSC) with the appropriate amine having a strong chromophore.Succini
