New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity

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• 作者：Luca Piemontese^a ; ^b ; Carmen Cerchia^c ; Antonio Laghezza^a ; Pamela Ziccardi^d ; Sabina Sblano^a ; Paolo Tortorella^a ; Vito Iacobazzi^e ; ^f ; Vittoria Infantino^e ; ^g ; Paolo Convertini^e ; ^g ; Fabrizio Dal Piaz^h ; Angelo Lupo^d ; Vittorio Colantuoni^d ; Antonio Lavecchia^c ; ^{antonio.lavecchia@unina.it} ; Fulvio Loiodice^a ; ^{fulvio.loiodice@uniba.it}
• 关键词：PPAR ; Docking experiments ; Mitochondrial biogenesis ; Anti-proliferative effects ; Gene expression analysis
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：379-397
• 全文大小：3508 K
• 卷排序：127

文摘

new diphenylmethane derivatives act as potent dual PPARα/γ partial agonists. docking explains the unusual lack of stereoselectivity for these compounds. these compounds exhibit strong activation of mitochondrial functions and biogenesis. they also show anti-proliferative effects only partly due to PPAR activity.