Abstract

The multifactorial nature of chemotherapy failure in controlling cancer is often associated with the occurrence of multidrug resistance (MDR), a phenomenon likely related to the increased expression of members of the ATP binding cassette (ABC) transporter superfamily. In this respect, the most extensively characterized MDR transporters include ABCB1 (also known as MDR1 or P-glycoprotein) and ABCC1 (also known as MRP1) whose inhibition remains a priority to circumvent drug resistance. Herein, we report how the simple galloyl benzamide scaffold can be easily and properly decorated for the preparation of either MRP1 or P-gp selective inhibitors. In particular, some gallamides and pyrogallol-1-monomethyl ethers congeners showed remarkable affinity and selectivity toward MRP1 (e.g. 15g: IC50 = 9.50 μM, > 100 μM). On the other hand, trimethyl ether galloyl anilides, with few exceptions, exhibited moderate to very high and selective P-gp inhibition (e.g., 11g: IC50 = 0.2 μM, > 100μM).

Autore Pugliese

• Stefanachi Angela , Berardi Francesco , Niso Mauro , Colabufo Nicola Antonio , Nicolotti Orazio , Cellamare Saverio

Tutti gli autori

• STEFANACHI A.;CAROTTI A.;BERARDI F.;LEONETTI F.;NISO M.;COLABUFO N.A.;NICOLOTTI O.;PERRONE R.;CELLAMARE S.

Titolo volume/Rivista

Non Disponibile

Anno di pubblicazione

2012

ISSN

0022-2623

ISBN

Non Disponibile

Numero di citazioni Wos

19

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

24

Ultimo Aggiornamento Citazioni

Non Disponibile

Settori ERC

Non Disponibile

Codici ASJC

Non Disponibile