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

Bioorganic & medicinal chemistry letters (2001-01-05)
A van Loevezijn, J D Allen, A H Schinkel, G J Koomen
ABSTRACT

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.

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Sigma-Aldrich
Fumitremorgin C, from Neosartorya fischeri, film