The acetylcholinesterase inhibitory and/or antitumour activities of amino-, thio-and ester-derivatives of avarol selected were evaluated for the first time at in vitro conditions. Avarol-3',4'-dithioglycol (1) and avarol-4'-(3) mercaptopropionic acid (3) were shown to be the best inhibitors of the enzyme tested (0.50 mu g and IC50 0.05mM and 0.50 mg and IC50 0.12 mM, respectively), while 4'-tryptamine-avarone (9) and avarol-3'-(3) mercaptopropionic acid (2) exhibited the highest cytotoxicity against the human breast T-47D cancer cell line (IC50 0.66 mu g/mL and 1.25 mu g/mL, respectively). According to experimental data obtained, the sesquiterpenoid hydroquinone structure of bioactive avarol derivatives may inspire development of new pharmacologically useful substances to be used in the treatment of Alzheimer's disease and/or human breast tumour.
TY - JOUR
AU - Tommonaro, Giuseppina
AU - Pejin, Boris
AU - Iodice, Carmine
AU - Tafuto, Antonietta
AU - De Rosa, Salvatore
PY - 2015
UR - http://rimsi.imsi.bg.ac.rs/handle/123456789/827
AB - The acetylcholinesterase inhibitory and/or antitumour activities of amino-, thio-and ester-derivatives of avarol selected were evaluated for the first time at in vitro conditions. Avarol-3',4'-dithioglycol (1) and avarol-4'-(3) mercaptopropionic acid (3) were shown to be the best inhibitors of the enzyme tested (0.50 mu g and IC50 0.05mM and 0.50 mg and IC50 0.12 mM, respectively), while 4'-tryptamine-avarone (9) and avarol-3'-(3) mercaptopropionic acid (2) exhibited the highest cytotoxicity against the human breast T-47D cancer cell line (IC50 0.66 mu g/mL and 1.25 mu g/mL, respectively). According to experimental data obtained, the sesquiterpenoid hydroquinone structure of bioactive avarol derivatives may inspire development of new pharmacologically useful substances to be used in the treatment of Alzheimer's disease and/or human breast tumour.
PB - Taylor & Francis Ltd, Abingdon
T2 - Journal of Enzyme Inhibition and Medicinal Chemistry
T1 - Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol
EP - 335
IS - 2
SP - 333
VL - 30
DO - 10.3109/14756366.2014.913037
ER -
@article{
author = "Tommonaro, Giuseppina and Pejin, Boris and Iodice, Carmine and Tafuto, Antonietta and De Rosa, Salvatore",
year = "2015",
abstract = "The acetylcholinesterase inhibitory and/or antitumour activities of amino-, thio-and ester-derivatives of avarol selected were evaluated for the first time at in vitro conditions. Avarol-3',4'-dithioglycol (1) and avarol-4'-(3) mercaptopropionic acid (3) were shown to be the best inhibitors of the enzyme tested (0.50 mu g and IC50 0.05mM and 0.50 mg and IC50 0.12 mM, respectively), while 4'-tryptamine-avarone (9) and avarol-3'-(3) mercaptopropionic acid (2) exhibited the highest cytotoxicity against the human breast T-47D cancer cell line (IC50 0.66 mu g/mL and 1.25 mu g/mL, respectively). According to experimental data obtained, the sesquiterpenoid hydroquinone structure of bioactive avarol derivatives may inspire development of new pharmacologically useful substances to be used in the treatment of Alzheimer's disease and/or human breast tumour.",
publisher = "Taylor & Francis Ltd, Abingdon",
journal = "Journal of Enzyme Inhibition and Medicinal Chemistry",
title = "Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol",
pages = "335-333",
number = "2",
volume = "30",
doi = "10.3109/14756366.2014.913037"
}
Tommonaro, G., Pejin, B., Iodice, C., Tafuto, A.,& De Rosa, S.. (2015). Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol. in Journal of Enzyme Inhibition and Medicinal Chemistry
Taylor & Francis Ltd, Abingdon., 30(2), 333-335.
https://doi.org/10.3109/14756366.2014.913037
Tommonaro G, Pejin B, Iodice C, Tafuto A, De Rosa S. Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol. in Journal of Enzyme Inhibition and Medicinal Chemistry. 2015;30(2):333-335.
doi:10.3109/14756366.2014.913037 .
Tommonaro, Giuseppina, Pejin, Boris, Iodice, Carmine, Tafuto, Antonietta, De Rosa, Salvatore, "Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol" in Journal of Enzyme Inhibition and Medicinal Chemistry, 30, no. 2 (2015):333-335,
https://doi.org/10.3109/14756366.2014.913037 . .
