title: Design, Synthesis, and Structure-Activity Relationships of Bavachinin Analogues as Peroxisome Proliferator-Activated Receptor γ Agonists.
abstract: Peroxisome proliferator-activated receptor γ (PPARγ) agonists have been used for the treatment of diabetes with the effect of lowering blood glucose levels and improving insulin sensitivity. Natural compounds such as flavones, flavanones, and isoflavones have shown excellent PPARγ agonist activity. In this study, analogues of bavachinin were designed, synthesized, and evaluated by reporter gene assays for PPARγ agonist activity. Preliminary structure-activity relationships for these bavachinin analogues have been summarized, and seven compounds were found to have higher PPARγ agonist activities than the parent flavanone bavachinin.
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, China.
authors.forename: Guoxin
authors.initials: G
authors.lastname: Du
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, China.
authors.forename: Yuanyuan
authors.initials: Y
authors.lastname: Zhao
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, China.
authors.forename: Li
authors.initials: L
authors.lastname: Feng
authors.affiliation: Key Laboratory of Receptor Research & Drug Discovery and Design Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai, 201203, China.
authors.forename: Zhuo
authors.initials: Z
authors.lastname: Yang
authors.affiliation: Informatics Department, UCB Pharma, 216 Bath Road, Slough, SL1 4EN, UK.
authors.forename: Jiye
authors.initials: J
authors.lastname: Shi
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, China.
authors.forename: Cheng
authors.initials: C
authors.lastname: Huang
authors.affiliation: Key Laboratory of Receptor Research & Drug Discovery and Design Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai, 201203, China.
authors.forename: Bo
authors.initials: B
authors.lastname: Li
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, China.
authors.forename: Fujiang
authors.initials: F
authors.lastname: Guo
authors.affiliation: Key Laboratory of Receptor Research & Drug Discovery and Design Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai, 201203, China.
authors.forename: Weiliang
authors.initials: W
authors.lastname: Zhu
authors.affiliation: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, China.
authors.forename: Yiming
authors.initials: Y
authors.lastname: Li
mesh_terms: D002460:Cell Line; D015195:Drug Design; D005419:Flavonoids / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D017930:Genes, Reporter; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D008024:Ligands; D047495:PPAR gamma / Q000819:agonists* / Q000378:metabolism; D011485:Protein Binding; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D047309:Flavones
chemical_list: D005419:Flavonoids; D007004:Hypoglycemic Agents; D008024:Ligands; D047495:PPAR gamma; C468752:bavachinin; D047309:Flavones
keywords: PPARγ; bavachinin; diabetes mellitus; reporter gene assays; structure-activity relationships