Literature DB >> 11140726

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

A van Loevezijn1, 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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Year:  2001        PMID: 11140726     DOI: 10.1016/s0960-894x(00)00588-6

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  18 in total

1.  Investigation of chalcones as selective inhibitors of the breast cancer resistance protein: critical role of methoxylation in both inhibition potency and cytotoxicity.

Authors:  Glaucio Valdameri; Charlotte Gauthier; Raphaël Terreux; Rémy Kachadourian; Brian J Day; Sheila M B Winnischofer; Maria E M Rocha; Véronique Frachet; Xavier Ronot; Attilio Di Pietro; Ahcène Boumendjel
Journal:  J Med Chem       Date:  2012-04-02       Impact factor: 7.446

2.  Establishment and characterization of models of chemotherapy resistance in colorectal cancer: Towards a predictive signature of chemoresistance.

Authors:  Niels F Jensen; Jan Stenvang; Mette K Beck; Barbora Hanáková; Kirstine C Belling; Khoa N Do; Birgitte Viuff; Sune B Nygård; Ramneek Gupta; Mads H Rasmussen; Line S Tarpgaard; Tine P Hansen; Eva Budinská; Per Pfeiffer; Fred Bosman; Sabine Tejpar; Arnaud Roth; Mauro Delorenzi; Claus L Andersen; Maria U Rømer; Nils Brünner; José M A Moreira
Journal:  Mol Oncol       Date:  2015-02-24       Impact factor: 6.603

3.  Role of the breast cancer resistance protein (ABCG2) in drug transport.

Authors:  Qingcheng Mao; Jashvant D Unadkat
Journal:  AAPS J       Date:  2005-05-11       Impact factor: 4.009

Review 4.  Structure and function of the human breast cancer resistance protein (BCRP/ABCG2).

Authors:  Zhanglin Ni; Zsolt Bikadi; Mark F Rosenberg; Qingcheng Mao
Journal:  Curr Drug Metab       Date:  2010-09       Impact factor: 3.731

Review 5.  Role of the breast cancer resistance protein (BCRP/ABCG2) in drug transport--an update.

Authors:  Qingcheng Mao; Jashvant D Unadkat
Journal:  AAPS J       Date:  2014-09-19       Impact factor: 4.009

6.  Human ABCG2: structure, function, and its role in multidrug resistance.

Authors:  Wei Mo; Jian-Ting Zhang
Journal:  Int J Biochem Mol Biol       Date:  2011-03-30

7.  Identification and characterization of the major alternative promoter regulating Bcrp1/Abcg2 expression in the mouse intestine.

Authors:  Karthika Natarajan; Yi Xie; Takeo Nakanishi; William T Beck; Kenneth S Bauer; Douglas D Ross
Journal:  Biochim Biophys Acta       Date:  2011-06-28

8.  Strategies for the synthesis of novel indole alkaloid-based screening libraries for drug discovery.

Authors:  Demosthenes Fokas; Libing Yu; Carmen M Baldino
Journal:  Mol Divers       Date:  2005       Impact factor: 2.943

Review 9.  Structure-activity relationships and quantitative structure-activity relationships for breast cancer resistance protein (ABCG2).

Authors:  Yash A Gandhi; Marilyn E Morris
Journal:  AAPS J       Date:  2009-07-24       Impact factor: 4.009

10.  Knocking down breast cancer resistance protein (Bcrp) by adenoviral vector-mediated RNA interference (RNAi) in sandwich-cultured rat hepatocytes: a novel tool to assess the contribution of Bcrp to drug biliary excretion.

Authors:  Wei Yue; Koji Abe; Kim L R Brouwer
Journal:  Mol Pharm       Date:  2009 Jan-Feb       Impact factor: 4.939

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