N-alkanol-N-cyclohexanol amine aryl esters: Multidrug resistance (MDR) reversing agents with high potency and efficacy

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• 作者：Elisabetta Teodori^a ; ^{elisabetta.teodori@unifi.it} ; Silvia Dei^a ; Marcella Coronnello^b ; Elisa Floriddia^a ; Gianluca Bartolucci^a ; Dina Manetti^a ; Maria Novella Romanelli^a ; Diego Santo Domingo Porqueras^c ; Milena Salerno^c
• 关键词：MDR reversers ; P-gp modulators ; N-alkanol-N-cyclohexanol amine aryl esters ; Chemosensitizers ; Doxorubicin-resistant human erythroleukemia K562 cells (K562/DOX) ; Pirarubicin uptake
• 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：586-598
• 全文大小：926 K
• 卷排序：127

文摘

A series of N-alkanol-N-cyclohexanolamine arylesters were designed and synthesized. The new compounds were tested on the K562/DOX cell line by three different tests. They behave as P-gp-dependent multidrug resistance (MDR) reversers. The chemical stability of the ester function of the compounds was evaluated. A compound results interesting lead for the development of new P-gp modulators.