The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.
Article Details
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Matin A, Doddareddy MR, Gavande N, Nammi S, Groundwater PW, Roubin RH, Hibbs DE
The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.
Bioorg Med Chem. 2013 Feb 1;21(3):766-78. doi: 10.1016/j.bmc.2012.11.040. Epub 2012 Dec 3.
- PubMed ID
- 23265844 [ View in PubMed]
- Abstract
Twenty three dual PPARalpha and gamma molecules of natural product origin, previously reported by our group, were further investigated for pan PPAR transactivation against PPARdelta. 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, Psi-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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Bezafibrate Peroxisome proliferator-activated receptor alpha EC 50 (nM) 46580 N/A N/A Details Bezafibrate Peroxisome proliferator-activated receptor delta EC 50 (nM) 35740 N/A N/A Details Bezafibrate Peroxisome proliferator-activated receptor gamma EC 50 (nM) 70360 N/A N/A Details Fenofibrate Peroxisome proliferator-activated receptor alpha EC 50 (nM) 33510 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 43710 N/A N/A Details