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Bioorg Med Chem. 2013 Feb 1;21(3):766-78. doi: 10.1016/j.bmc.2012.11.040. Epub 2012 Dec 3.

The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.

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Faculty of Pharmacy, The University of Sydney, Sydney, NSW 2006, Australia.


Twenty three dual PPARα and γ molecules of natural product origin, previously reported by our group, were further investigated for pan PPAR transactivation against PPARδ. The in vitro cell toxicity profile, as well as, in silico study of the most active molecules within this new class of pan PPAR agonists are also described. 3',5' Dimethoxy-7 hydroxyisoflavone 6, Ψ-baptigenin 7, 4' fluoro-7 hydroxyisoflavone 8, and 3' methoxy-7 hydroxyisoflavone 9 were identified as the most potent molecules studied within the set compared to the commercially available pan PPAR agonist, bezafibrate 1. These novel active molecules may thus be useful as future leads in PPAR-related disorders, including type II diabetes mellitus and metabolic syndrome.

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