Bioorganic and Medicinal Chemistry p. 4954 - 4961 (2012)
Update date:2022-07-29
Topics:
Xiao, Bin
Yin, Jun
Park, Minhi
Liu, Juan
Li, Jian Lin
Kim, Eun La
Hong, Jongki
Chung, Hae Young
Jung, Jee H.
On the basis of a marine fungal phthalide (paecilocin A) skeleton, we synthesized 20 analogs and evaluated them for peroxisome proliferator-activated receptor gamma (PPAR-γ) binding and activation. Among these analogs, 6 and 7 had significant PPAR-γ binding activity, and 7 showed further PPAR-γ activation in rat liver Ac2F cells. In docking simulation, 7 formed H bonds with key amino acid residues of the PPAR-γ binding domain, and the overall positioning was similar to rosiglitazone. This new phthalide derivative is considered an interesting new molecular class of PPAR-γ ligands.
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