Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	Novel quinolinone-pyrazoline hybrids: Synthesis and evaluation of antioxidant and lipoxygenase inhibitory activity
Δημιουργός/Συγγραφέας:	Kostopoulou, Ioanna Diassakou, Antonia Kavetsou, Eleni Kritsi, Eftichia [EL] Ζουμπουλάκης, Παναγιώτης[EN] Zoumpoulakis, Panagiotis Pontiki, Eleni Hadjipavlou-Litina, Dimitra Detsi, Anastasia
Ημερομηνία:	2021-05
Γλώσσα:	Αγγλικά
ISSN:	1381-1991 1573-501X
DOI:	10.1007/s11030-020-10045-x
Άλλο:	32065346
Περίληψη:	The present project deals with the investigation of structure-activity relationship of several quinolinone-chalcone and quinolinone-pyrazoline hybrids, in an effort to discover promising antioxidant and anti-inflammatory agents. In order to accomplish this goal, four bioactive hybrid quinolinone-chalcone compounds (8a-8d) were synthesized via an aldol condensation reaction, which were then chemically modified, forming fifteen new pyrazoline analogues (9a-9o). All the synthesized analogues were in vitro evaluated in terms of their antioxidant and soybean lipoxygenase (LOX) inhibitory activity. Among all the pyrazoline derivatives, compounds 9b and 9m were found to possess the best combined activity, whereas 9b analogue exhibited the most potent LOX inhibitory activity, with IC50 value 10 μM. The in silico docking results revealed that the synthetic pyrazoline analogue 9b showed high AutoDock Vina score (- 10.3 kcal/mol), while all the tested derivatives presented allosteric interactions with the enzyme.
Τίτλος πηγής δημοσίευσης:	Molecular diversity
Τόμος/Κεφάλαιο:	25
Τεύχος:	2
Σελίδες:	723–740
Θεματική Κατηγορία:	[EL] Χημική Βιολογία[EN] Chemical Biology [EL] Χημεία (Γενικά)[EN] Chemistry (General) [EL] Βιοτεχνολογία[EN] Biotechnology
Λέξεις-Κλειδιά:	Antioxidant activity Chalcones LOX inhibition Lipoxygenase Pyrazolines Quinolinones Biphenyl Compounds Linoleic Acid Lipoxygenases Molecular Docking Simulation Picrates Soybeans Anti-Inflammatory Agents Antioxidants Lipoxygenase Inhibitors Pyrazoles Quinolones
Κάτοχος πνευματικών δικαιωμάτων:	Copyright © 2020 Springer Nature Switzerland AG
Ηλεκτρονική διεύθυνση περιοδικού (link) :	https://www.springer.com/journal/11030
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο