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Quinoline Carboxamide‐Type ABCG2 Modulators: Indole and Quinoline Moieties as Anilide Replacements
Author(s) -
Bauer Stefanie,
OchoaPuentes Cristian,
Sun Qiu,
Bause Manuel,
Bernhardt Günther,
König Burkhard,
Buschauer Armin
Publication year - 2013
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201300319
Subject(s) - quinoline , indole test , moiety , chemistry , abcg2 , combinatorial chemistry , potency , stereochemistry , pharmacology , database , computer science , medicine , biochemistry , in vitro , organic chemistry , atp binding cassette transporter , transporter , gene
ABC, it′s easy as 1 2 3! Bioisosteric replacement of the anilide core by an indole moiety considerably increased stability and gave potent and selective ABCG2 (BCRP) inhibitors. Some compounds are superior to the reference substances fumitremorgin C and Ko143 in terms of potency and efficacy and are the most potent ABCG2 modulators reported so far.