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Titolo:
Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines
Autore:
van Loevezijn, A; Allen, JD; Schinkel, AH; Koomen, GJ;
Indirizzi:
Univ Amsterdam, Organ Chem Lab, Inst Mol Chem, NL-1018 WS Amsterdam, Netherlands Univ Amsterdam Amsterdam Netherlands NL-1018 WS S Amsterdam, Netherlands Netherlands Canc Inst, Div Expt Therapy, NL-1066 CX Amsterdam, NetherlandsNetherlands Canc Inst Amsterdam Netherlands NL-1066 CX rdam, Netherlands
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 1, volume: 11, anno: 2001,
pagine: 29 - 32
SICI:
0960-894X(20010108)11:1<29:IOBDEB>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
SOLID-PHASE SYNTHESIS; MULTIDRUG-RESISTANCE; CELL-CYCLE; MITOXANTRONE; REVERSAL; GENE; OVEREXPRESSION; TRANSPORTER; TOPOTECAN; GF120918;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
23
Recensione:
Indirizzi per estratti:
Indirizzo: Koomen, GJ Univ Amsterdam, Organ Chem Lab, Inst Mol Chem, Nieuwe Achtergracht 129, NL-1018 WS Amsterdam, Netherlands Univ Amsterdam Nieuwe Achtergracht 129 Amsterdam Netherlands NL-1018 WS
Citazione:
A. van Loevezijn et al., "Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines", BIOORG MED, 11(1), 2001, pp. 29-32

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

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Documento generato il 03/04/20 alle ore 11:12:36