A new series of P-glycoprotein (Pgp)-dependent multidrug resistance (MDR) inhibitors having a N,N-bis(cyclohexanol)amine scaffold have been designed, following the frozen analog approach. With respect to the parent flexible molecules, the new compounds show improved potency and efficacy. Among them, compound 1d, on anthracycline-resistant erythroleukemia K562 cells, is able to completely reverse Pgp-dependent MDR at low nanomolar concentration.
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 / Teodori, Elisabetta; Martelli, Cecilia; Salerno, M.; Darghal, N.; Dei, Silvia; GARNIER SUILLEROT, A.; Gualtieri, Fulvio; Manetti, Dina; Scapecchi, Serena; Romanelli, MARIA NOVELLA. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 50:(2007), pp. 599-602. [10.1021/jm0614432]
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
TEODORI, ELISABETTA;MARTELLI, CECILIA;DEI, SILVIA;GUALTIERI, FULVIO;MANETTI, DINA;SCAPECCHI, SERENA;ROMANELLI, MARIA NOVELLA
2007
Abstract
A new series of P-glycoprotein (Pgp)-dependent multidrug resistance (MDR) inhibitors having a N,N-bis(cyclohexanol)amine scaffold have been designed, following the frozen analog approach. With respect to the parent flexible molecules, the new compounds show improved potency and efficacy. Among them, compound 1d, on anthracycline-resistant erythroleukemia K562 cells, is able to completely reverse Pgp-dependent MDR at low nanomolar concentration.
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