Isomeric N,N-Bis(cyclohexanol)amine Aryl Esters: The Discovery of a New Class of Highly Potent P-Glycoprotein (Pgp)-dependent Multidrug Resistance (MDR) Inhibitors
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- 作者：Elisabetta Teodori ; Cecilia Martelli ; Milena Salerno ; Nacira Darghal ; Silvia Dei ; Arlette Garnier-Suillerot ; Fulvio Gualtieri ; Dina Manetti ; Serena Scapecchi ; Maria Novella Romanelli
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：February 22, 2007
- 年：2007
- 卷：50
- 期：4
- 页码：599 - 602
- 全文大小：65K
- 年卷期：v.50,no.4(February 22, 2007)
- ISSN：1520-4804
文摘
A new series of P-glycoprotein (Pgp)-dependent multidrugresistance (MDR) inhibitors having a N,N-bis(cyclohexanol)aminescaffold have been designed, following the frozen analog approach.With respect to the parent flexible molecules, the new compounds showimproved potency and efficacy. Among them, compound 1d, onanthracycline-resistant erythroleukemia K562 cells, is able to completelyreverse Pgp-dependent MDR at low nanomolar concentration.