1381781-05-0Relevant articles and documents
Total synthesis and dual PPARα/γ agonist effects of Amorphastilbol and its synthetic derivatives
Kim, Taejung,Lee, Woojung,Jeong, Kyu Hyuk,Song, Jung Ho,Park, Soon-Hye,Choi, Pilju,Kim, Su-Nam,Lee, Seokjoon,Ham, Jungyeob
, p. 4122 - 4126 (2012)
Amorphastilbol (APH-1), isolated from a Robinia pseudoacacia var. umbraculifer seed extract, is a biologically interesting natural trans-stilbene compound with dual peroxisome proliferator-activated receptor (PPAR) α/γ agonist activity. After total synthesis of APH-1 and its derivatives by Pd-catalyzed Suzuki-Miyaura cross-coupling of a common (E)-styryl bromide intermediate and various aromatic trifluoroborate compounds, we biologically evaluated APH-2-APH-12 for PPAR agonist activity. APH-4 and APH-11 were effective PPARα/γ transcriptional activators, compared with APH-1. Therefore, we suggest that APH-4 and APH-11 are novel dual PPARα/γ agonists and are potentially useful for treating type 2 diabetes by enhancing glucose and lipid metabolism.