一些吡唑衍生物的合成及其与P-糖蛋白亲和力结合的初步研究。
Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein.
作者信息
Manna Fedele, Chimenti Franco, Fioravanti Rossella, Bolasco Adriana, Secci Daniela, Chimenti Paola, Ferlini Cristiano, Scambia Giovanni
机构信息
Dip. di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Rome, Italy.
出版信息
Bioorg Med Chem Lett. 2005 Oct 15;15(20):4632-5. doi: 10.1016/j.bmcl.2005.05.067.
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.
合成了一系列取代吡唑啉，并对其抗癌活性以及通过直接结合含有ATP结合位点和调节剂相互作用区域的纯化蛋白结构域来抑制P-糖蛋白介导的多药耐药性的能力进行了评估。已发现化合物2a和e与P-糖蛋白的结合亲和力更高。
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