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Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol

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2016
992.pdf (155.3Kb)
Authors
Tommonaro, Giuseppina
Pejin, Boris
Iodice, Carmine
Tafuto, Antonietta
De Rosa, Salvatore
Article (Published version)
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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 0.05 mM and 0.50 mu g 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.
Keywords:
sesquiterpenoid hydroquinone derivatives / Dysidea avara / antitumour activity / Acetylcholinesterase inhibitory activity
Source:
Journal of Enzyme Inhibition and Medicinal Chemistry, 2016, 31, 4, 684-686
Publisher:
  • Taylor & Francis Ltd, Abingdon

DOI: 10.3109/14756366.2015.1057724

ISSN: 1475-6366

PubMed: 26114310

WoS: 000379783200022

Scopus: 2-s2.0-84964612009
[ Google Scholar ]
3
1
URI
http://rimsi.imsi.bg.ac.rs/handle/123456789/995
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Institut za multidisciplinarna istraživanja
TY  - JOUR
AU  - Tommonaro, Giuseppina
AU  - Pejin, Boris
AU  - Iodice, Carmine
AU  - Tafuto, Antonietta
AU  - De Rosa, Salvatore
PY  - 2016
UR  - http://rimsi.imsi.bg.ac.rs/handle/123456789/995
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 0.05 mM and 0.50 mu g 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  - 686
IS  - 4
SP  - 684
VL  - 31
DO  - 10.3109/14756366.2015.1057724
ER  - 
@article{
author = "Tommonaro, Giuseppina and Pejin, Boris and Iodice, Carmine and Tafuto, Antonietta and De Rosa, Salvatore",
year = "2016",
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 0.05 mM and 0.50 mu g 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 = "686-684",
number = "4",
volume = "31",
doi = "10.3109/14756366.2015.1057724"
}
Tommonaro, G., Pejin, B., Iodice, C., Tafuto, A.,& De Rosa, S.. (2016). 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., 31(4), 684-686.
https://doi.org/10.3109/14756366.2015.1057724
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. 2016;31(4):684-686.
doi:10.3109/14756366.2015.1057724 .
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, 31, no. 4 (2016):684-686,
https://doi.org/10.3109/14756366.2015.1057724 . .

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