Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein
F Manna, F Chimenti, R Fioravanti, A Bolasco…
Index: Manna, Fedele; Chimenti, Franco; Fioravanti, Rossella; Bolasco, Adriana; Secci, Daniela; Chimenti, Paola; Ferlini, Cristiano; Scambia, Giovanni Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 20 p. 4632 - 4635
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Citation Number: 134
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.
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