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

被引：128

作者：

van Loevezijn, A

Allen, JD

Schinkel, AH

Koomen, GJ

机构：

[1] Univ Amsterdam, Organ Chem Lab, Inst Mol Chem, NL-1018 WS Amsterdam, Netherlands

[2] Netherlands Canc Inst, Div Expt Therapy, NL-1066 CX Amsterdam, Netherlands

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(00)00588-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：29 / 32

页数：4

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