title: Activity-lipophilicity relationship studies on P-gp ligands designed as simplified tariquidar bulky fragments.
abstract: A series of alkyloxyquinoline derivatives has been developed to evaluate the relationship between P-gp potency and lipophilicity. The results show a satisfactory lipophilicity-activity correlation although a series of derivatives showing higher P-gp potency is needed in order to confirm this hypothesis.
authors.affiliation: Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari A. Moro, via Orabona 4, 70125 Bari, Italy.
authors.forename: Marialessandra
authors.initials: M
authors.lastname: Contino
authors.forename: Laura
authors.initials: L
authors.lastname: Zinzi
authors.forename: Mariangela
authors.initials: M
authors.lastname: Cantore
authors.forename: Maria Grazia
authors.initials: MG
authors.lastname: Perrone
authors.forename: Marcello
authors.initials: M
authors.lastname: Leopoldo
authors.forename: Francesco
authors.initials: F
authors.lastname: Berardi
authors.forename: Roberto
authors.initials: R
authors.lastname: Perrone
authors.forename: Nicola Antonio
authors.initials: NA
authors.lastname: Colabufo
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors*; D000818:Animals; D002460:Cell Line; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D057927:Hydrophobic and Hydrophilic Interactions; D008024:Ligands; D015394:Molecular Structure; D015125:Oxyquinoline / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D008024:Ligands; D015125:Oxyquinoline