title: Quinoline carboxamide-type ABCG2 modulators: indole and quinoline moieties as anilide replacements.
abstract: 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.
authors.affiliation: Institut für Pharmazie, Pharmazeutische/Medizinische Chemie II, Universität Regensburg, Universitätsstr. 31, 93053 Regensburg (Germany).
authors.forename: Stefanie
authors.initials: S
authors.lastname: Bauer
authors.forename: Cristian
authors.initials: C
authors.lastname: Ochoa-Puentes
authors.forename: Qiu
authors.initials: Q
authors.lastname: Sun
authors.forename: Manuel
authors.initials: M
authors.lastname: Bause
authors.forename: Günther
authors.initials: G
authors.lastname: Bernhardt
authors.forename: Burkhard
authors.initials: B
authors.lastname: König
authors.forename: Armin
authors.initials: A
authors.lastname: Buschauer
mesh_terms: D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000037:antagonists & inhibitors*; D000620:Aminoimidazole Carboxamide / Q000737:chemistry*; D000813:Anilides / Q000737:chemistry*; D045744:Cell Line, Tumor; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D015394:Molecular Structure; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors*; D010795:Phthalic Acids / Q000737:chemistry*; D055550:Protein Stability; D011804:Quinolines / Q000737:chemistry*
chemical_list: C116614:ABCG2 protein, human; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D000813:Anilides; D007211:Indoles; D009363:Neoplasm Proteins; D010795:Phthalic Acids; D011804:Quinolines; C000594010:UR-COP78; C000594009:UR-ME22-1; D000620:Aminoimidazole Carboxamide
keywords: ABC transporters; breast cancer resistance proteins; inhibitors; sonogashira couplings; syntheses