@article{5659547b80744e1e84399cfc37b276d2,
title = "Quinoxalinetacrine QT78, a cholinesterase inhibitor as a potential ligand for Alzheimer{\textquoteright}s disease therapy",
abstract = "We report the synthesis and relevant pharmacological properties of the quinoxalinetacrine (QT) hybrid QT78 in a project targeted to identify new non-hepatotoxic tacrine derivatives for Alzheimer{\textquoteright}s disease therapy. We have found that QT78 is less toxic than tacrine at high concentrations (from 100 µM to 1 mM), less potent than tacrine as a ChE inhibitor, but shows selective BuChE inhibition (IC50 (hAChE) = 22.0 ± 1.3 µM; IC50 (hBuChE) = 6.79 ± 0.33 µM). Moreover, QT78 showed effective and strong neuroprotection against diverse toxic stimuli, such as rotenone plus oligomycin-A or okadaic acid, of biological significance for Alzheimer{\textquoteright}s disease.",
keywords = "Alzheimer{\textquoteright}s disease, Cholinesterase inhibitor, Hepatotoxicity, Molecular modeling, Neuroprotection, Quinoxalines, Quinoxalinetacrines, Tacrine",
author = "Eva Ramos and Alejandra Palomino-Antol{\'i}n and Manuela Bartolini and Isabel Iriepa and Ignacio Moraleda and Daniel Diez-Iriepa and Abdelouahid Samadi and Cortina, {Carol V.} and Mourad Chioua and Javier Egea and Alejandro Romero and Jos{\'e} Marco-Contelles",
note = "Funding Information: Funding: J.M.-C is indebted to MICINN (SAF2006-08764-C02-01 and ISCIII [RED RENEVAS (RD06/0026/1002)] for financial support. Also this work was supported by grants from Fondo de Investigaciones Sanitarias (FIS)(ISCIII/FEDER)(Programa MIguel Servet CP14/00008;PI16/00735) and Fundaci{\'o}n Mutua Madrile{\~n}a to J.E. Funding Information: J.M.-C is indebted to MICINN (SAF2006-08764-C02-01 and ISCIII [RED RENEVAS (RD06/0026/1002)] for financial support. Also this work was supported by grants from Fondo de Investigaciones Sanitarias (FIS)(ISCIII/FEDER)(Programa MIguel Servet CP14/00008;PI16/00735) and Fundaci{\'o}n Mutua Madrile{\~n}a to J.E. J.M.-C. is indebted to Nico Justin for reading and correcting the manuscript. Publisher Copyright: {\textcopyright} 2019 by the authors.",
year = "2019",
month = apr,
day = "17",
doi = "10.3390/molecules24081503",
language = "English",
volume = "24",
journal = "Molecules",
issn = "1420-3049",
publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",
number = "8",
}