Synthesis and Biological Evaluation of Curcumin-Nitroxide-Based Molecular Hybrids as Antioxidant and Anti-Proliferative Agents
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Tartalom: http://real.mtak.hu/55329/
Archívum: MTA Könyvtár
Gyűjtemény: Status = In Press

Type = Article
Cím:
Synthesis and Biological Evaluation of Curcumin-Nitroxide-Based Molecular Hybrids as Antioxidant and Anti-Proliferative Agents
Létrehozó:
Bognár, Balázs
Kuppusamy, Laksmi
Madan, Esha
Kálai, Tamás
Balog, Mária
Jekö, József
Kuppusamy, Periannan
Hideg, Kálmán
Kiadó:
Bentham
Dátum:
2017
Téma:
QD04 Organic chemistry / szerves kémia
Tartalmi leírás:
Abstract: Background: Natural products and their derivatives are widely used to treat cancer and other diseases associated with ROS- and RNS-induced damages.
Methods: A series of paramagnetic modified curcumin analogs and 3,5-diarylidene-piperidones
(DAP) have been designed, synthesized, and characterized on their anti-proliferative and antioxidant activity.
Results: Biological characterization of the new compounds supported the earlier results that incorporation
of a nitroxide moiety or its precursor into curcumin or diarylidenylpiperidone (DAP) scaffolds
resulted in anti-proliferative effect toward cancerous cell-lines in case of aryl hydroxy and/or
methoxy substituent containing derivatives, suggesting their potential for targeted therapeutic applications.
In case of basic side chain derivatives, nitroxide incorporation gave unambiguous results, however
in tendency the more accessible DAP derivatives had stronger anti-proliferative effect. In most
cases, the nitroxide incorporation increased the TEAC value (proton and electron donation capability)
of DAP derivatives.
Conclusions: Among the compounds synthesized and investigated the spin-labeled curcumin and
3,5-bis(4-hydroxy-3-methoxybenzylidene)piperidin-4-one derivatives were the most effective antiproliferative
and antioxidant derivatives.
Nyelv:
magyar
Típus:
Article
PeerReviewed
info:eu-repo/semantics/article
Formátum:
text
Azonosító:
Bognár, Balázs and Kuppusamy, Laksmi and Madan, Esha and Kálai, Tamás and Balog, Mária and Jekö, József and Kuppusamy, Periannan and Hideg, Kálmán (2017) Synthesis and Biological Evaluation of Curcumin-Nitroxide-Based Molecular Hybrids as Antioxidant and Anti-Proliferative Agents. MEDICINAL CHEMISTRY. pp. 1-12. ISSN 1573-4064 (In Press)
Kapcsolat:
https://doi.org/10.2174/1871520617666170522124712
10.2174/1871520617666170522124712