Development of new inhibitors for N-acylethanolamine-hydrolyzing acid amidase as promising tool against bladder cancer

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• 作者：Riccardo Vago^a ; ^b ; ^{vago.riccardo@hsr.it} ; Arianna Bettiga^a ; ^{bettiga.arianna@hsr.it} ; Andrea Salonia^a ; ^b ; ^{andrea.salonia@hsr.it} ; Pierangela Ciuffreda^c ; ^{pierangela.ciuffreda@unimi.it} ; Roberta Ottria^c ; ^{roberta.ottria@guest.unimi.it}
• 关键词：Endocannabinoid ; Enzyme inhibition ; N-acylethanolamine-hydrolyzing acid amidase ; Bladder cancer
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 February 2017
• 年：2017
• 卷：25
• 期：3
• 页码：1242-1249
• 全文大小：1071 K
• 卷排序：25

文摘

New eight palmitamine derivatives were synthesized as NAAA inhibitors. Compounds inhibition activity was evaluated by a fluorimetric analysis on human NAAA. Fluorimetric screening allowed to select three promising compounds. New NAAA inhibitors can induce bladder cancer cell death and reduce cell migration. Effects on bladder cancer cells are due to a selective inhibition of NAAA.