title: Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein.
abstract: A series of substituted pyrazolines were synthesized and evaluated for their anticancer activity and for their ability to inhibit P-glycoprotein-mediated multidrug resistance by direct binding to a purified protein domain containing an ATP-binding site and a modulator interacting region. Compounds 2a and e have been found to bind to P-glycoprotein with greater affinity.
authors.affiliation: Dip. di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Rome, Italy.
authors.forename: Fedele
authors.initials: F
authors.lastname: Manna
authors.forename: Franco
authors.initials: F
authors.lastname: Chimenti
authors.forename: Rossella
authors.initials: R
authors.lastname: Fioravanti
authors.forename: Adriana
authors.initials: A
authors.lastname: Bolasco
authors.forename: Daniela
authors.initials: D
authors.lastname: Secci
authors.forename: Paola
authors.initials: P
authors.lastname: Chimenti
authors.forename: Cristiano
authors.initials: C
authors.lastname: Ferlini
authors.forename: Giovanni
authors.initials: G
authors.lastname: Scambia
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D011485:Protein Binding; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000378:metabolism; D013056:Spectrophotometry, Ultraviolet
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000970:Antineoplastic Agents; D011720:Pyrazoles