Total synthesis and dual PPARα/γ agonist effects of Amorphastilbol and its synthetic derivatives

Title
Total synthesis and dual PPARα/γ agonist effects of Amorphastilbol and its synthetic derivatives
Authors
김태정이우정정규혁송중호박순혜최필주김수남이석준함정엽
Keywords
Natural product; Amorphastilbol; Type 2 diabetes; Dual PPARα/γ agonists; Suzuki-Miyaura cross-coupling
Issue Date
2012-06
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 22, NO 12, 4122-4126
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/42690
ISSN
0960894X
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KIST Publication > Article
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