Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175

2015 ◽  
Vol 90 ◽  
pp. 583-594 ◽  
Author(s):  
Luca Piemontese ◽  
Giuseppe Fracchiolla ◽  
Antonio Carrieri ◽  
Mariagiovanna Parente ◽  
Antonio Laghezza ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Peroxisome Proliferator ◽  
The Novel ◽  
Peroxisome Proliferator Activated Receptor ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and Biological Evaluation of 2-Heteroarylthioalkanoic Acid Analogues of Clofibric Acid as Peroxisome Proliferator-Activated Receptor α Agonists

2009 ◽  
Vol 52 (20) ◽  
pp. 6224-6232 ◽  
Author(s):  
Letizia Giampietro ◽  
Alessandra Ammazzalorso ◽  
Antonella Giancristofaro ◽  
Fabio Lannutti ◽  
Giancarlo Bettoni ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Clofibric Acid ◽  
Peroxisome Proliferator ◽  
Peroxisome Proliferator Activated Receptor ◽  
Synthesis And Biological Evaluation

Design, Synthesis and Biological Evaluation of the Novel Antitumor Agent Aurone Derivatives

2013 ◽  
Vol 781-784 ◽  
pp. 1235-1239
Author(s):  
Qian Nan Guo ◽  
Lei Lv ◽  
Yao Zhou ◽  
Peng Yu ◽  
Yuou Teng
Keyword(s):  
Biological Activities ◽  
Antitumor Agent ◽  
Biological Evaluation ◽  
The Novel ◽  
Pharmacological Activities ◽  
Design Synthesis ◽  
H Nmr ◽  
Wide Range ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

Aurones belong to a class of heterocyclic flavonoids which contains a benzofuran element associated with a benzylidene linked in position 2. Aurones possess a wide range of pharmacological activities and biological activities, such as antitumor, antifungal, phytoalexin and so on. A novel series of 2-ayl-yl (5-methacrylate) aurone analogues were synthesized in six steps with the overall yield of 11%-13% and characterized by 1H NMR. Among the key intermediates and target compounds, 2-(2-furan-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7a) and 2-(2-thienyl-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7b) have never been reported before. Primary biological activities evaluation showed that 7a exhibited good inhibitory activities against K562 with an IC50 of 2.18 μM and against HepG2 with an IC50 of 3.95μM.

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