Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein |
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| Authors: | Manna Fedele Chimenti Franco Fioravanti Rossella Bolasco Adriana Secci Daniela Chimenti Paola Ferlini Cristiano Scambia Giovanni |
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| Institution: | Dip. di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Rome, Italy. |
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| 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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