Synthesis of Phthalimide Derivatives as Potential PPAR-γ Ligands
AbstractPaecilocin A, a phthalide derivative isolated from the jellyfish-derived fungus Paecilomyces variotii, activates PPAR-γ (Peroxisome proliferator-activated receptor gamma) in rat liver Ac2F cells. Based on a SAR (Structure-activity relationships) study and in silico analysis of paecilocin A-mimetic derivatives, additional N-substituted phthalimide derivatives were synthesized and evaluated for PPAR-γ agonistic activity in both murine liver Ac2F cells and in human liver HepG2 cells by luciferase assay, and for adipogenic activity in 3T3-L1 cells. Docking simulation indicated PD6 was likely to bind most strongly to the ligand binding domain of PPAR-γ by establishing crucial H-bonds with key amino acid residues. However, in in vitro assays, PD1 and PD2 consistently displayed significant PPAR-γ activation in Ac2F and HepG2 cells, and adipogenic activity in 3T3-L1 preadipocytes. View Full-Text
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Eom, S.H.; Liu, S.; Su, M.; Noh, T.H.; Hong, J.; Kim, N.D.; Chung, H.Y.; Yang, M.H.; Jung, J.H. Synthesis of Phthalimide Derivatives as Potential PPAR-γ Ligands. Mar. Drugs 2016, 14, 112.
Eom SH, Liu S, Su M, Noh TH, Hong J, Kim ND, Chung HY, Yang MH, Jung JH. Synthesis of Phthalimide Derivatives as Potential PPAR-γ Ligands. Marine Drugs. 2016; 14(6):112.Chicago/Turabian Style
Eom, So H.; Liu, Sen; Su, Mingzhi; Noh, Tae H.; Hong, Jongki; Kim, Nam D.; Chung, Hae Y.; Yang, Min H.; Jung, Jee H. 2016. "Synthesis of Phthalimide Derivatives as Potential PPAR-γ Ligands." Mar. Drugs 14, no. 6: 112.
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