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Bioorg Med Chem Lett. 2008 Sep 1;18(17):4761-3. doi: 10.1016/j.bmcl.2008.07.127. Epub 2008 Aug 3.

A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins.

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Pharmaceutical Institute, University of Bonn, An der Immenburg 4, D-53121 Bonn, Germany.


We present a novel lead for inhibitors of multidrug resistance-associated proteins (MRPs). Compound 1 (4-[(5,6,7,8-tetrahydro-4-oxo-4H-[1]benzothieno[2,3-d][1,3]thiazin-2-yl)amino]benzoic acid) was about six times more potent than the known inhibitor MK571 at MRP1, while at MRP2 its effect was similar to that of MK571. Structural analogs were also evaluated. Among them, compound 2, sharing the 4-aminobenzoic acid substructure with 1, also inhibited MRP1. Both derivatives were inactive against P-gp. It can be concluded that their carboxyl group is needed for inhibition of MRPs and accounts for the selectivity of these compounds.

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