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Bioorg Med Chem Lett. 2001 Jan 8;11(1):29-32.

Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines.

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Laboratory of Organic Chemistry, Institute of Molecular Chemistry, University of Amsterdam, The Netherlands.


A library of 42 diastereoisomeric mixtures of fumitremorgin-type indolyl diketopiperazines, prepared by parallel solid-phase synthesis, was screened for Breast Cancer Resistance Protein inhibitory activity and compared with GF120918. Demethoxy-fumitremorgin C was synthesized by solid-phase techniques and tested as well. Structure-activity relationship studies have identified several potent analogues, both in assays using the T6400 mouse and the T8 human cell line, whereas low cytotoxicity was seen at effective concentrations.

[Indexed for MEDLINE]

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