Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein.
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.
Manna
Fedele
F
Dip. di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Rome, Italy.
Chimenti
Franco
F
Fioravanti
Rossella
R
Bolasco
Adriana
A
Secci
Daniela
D
Chimenti
Paola
P
Ferlini
Cristiano
C
Scambia
Giovanni
G
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
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000970:Antineoplastic Agents; D011720:Pyrazoles