Further in vitro biological activity evaluation of amino-, thio- and ester- derivatives of avarol (Articolo in rivista)

Type
Label
  • Further in vitro biological activity evaluation of amino-, thio- and ester- derivatives of avarol (Articolo in rivista) (literal)
Anno
  • 2014-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.3109/14756366.2014.913037 (literal)
Alternative label
  • Tommonaro G., Pejin B., Iodice C., Tafuto A. and De Rosa S (2014)
    Further in vitro biological activity evaluation of amino-, thio- and ester- derivatives of avarol
    in Journal of enzyme inhibition and medicinal chemistry (Print)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Tommonaro G., Pejin B., Iodice C., Tafuto A. and De Rosa S (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • National Research Council of Italy, Institute of Biomolecular Chemistry, CNR-ICB, Pozzuoli-Naples, Italy Department of Life Sciences, Institute for Multidisciplinary Research - IMSI, University of Belgrade, Belgrade, Serbia (literal)
Titolo
  • Further in vitro biological activity evaluation of amino-, thio- and ester- derivatives of avarol (literal)
Abstract
  • The acetylcholinesterase inhibitory and/or antitumour activities of amino-, thio- and esterderivatives of avarol selected were evaluated for the first time at in vitro conditions. Avarol-30,40- dithioglycol (1) and avarol-40-(3)mercaptopropionic acid (3) were shown to be the best inhibitors of the enzyme tested (0.50 mg and IC50 0.05mM and 0.50 mg and IC50 0.12 mM, respectively), while 40-tryptamine-avarone (9) and avarol-30-(3)mercaptopropionic acid (2) exhibited the highest cytotoxicity against the human breast T-47D cancer cell line (IC50 0.66 mg/ mL and 1.25 mg/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. (literal)
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