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.
Pyrazole Derivatives as Potential Anticancer agents and their Affinity Binding to P-Glycoprotein / F., Manna; Chimenti, Franco; Fioravanti, Rossella; Bolasco, Adriana; Secci, Daniela; Chimenti, Paola; C., Ferlini; G., Scambia. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 15:(2005), pp. 4632-4635. [10.1016/j.bmcl.2005.05.067]
Pyrazole Derivatives as Potential Anticancer agents and their Affinity Binding to P-Glycoprotein
CHIMENTI, Franco;FIORAVANTI, Rossella;BOLASCO, Adriana;SECCI, DANIELA;CHIMENTI, Paola;
2005
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
