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

Authors
van Loevezijn, A Allen, JD Schinkel, AH Koomen, GJ
Citation
A. Van Loevezijn et al., Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines, BIOORG MED, 11(1), 2001, pp. 29-32
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
1
Year of publication
2001
Pages
29 - 32
Database
ISI
SICI code
0960-894X(20010108)11:1<29:IOBDEB>2.0.ZU;2-6
Abstract
A library of 42 diastereoisomeric mixtures of fumitremorgin-type indolyl di ketopiperazines, prepared by parallel solid-phase synthesis, was screened f or Breast Cancer Resistance Protein inhibitory activity and compared with G F120918. Demethoxy-fumitremorgin C was synthesized by solid-phase technique s and tested as well. Structure-activity relationship studies have identifi ed several potent analogues, both in assays using the T6400 mouse and the T 8 human cell line, whereas low cytotoxicity was seen at effective concentra tions. (C) 2000 Elsevier Science Ltd. All rights reserved.