新型硝基取代三芳基吡唑衍生物作为潜在雌激素受体配体的合成
Synthesis of novel nitro-substituted triaryl pyrazole derivatives as potential estrogen receptor ligands.
作者信息
Naoum Fotini, Kasiotis Konstantinos M, Magiatis Prokopios, Haroutounian Serkos A
机构信息
Chemistry Laboratory, Agricultural University of Athens, Iera odos 75, Athens 11855, Greece.
出版信息
Molecules. 2007 Jul 2;12(7):1259-73. doi: 10.3390/12071259.
Abstract
Novel tetrasubstituted pyrazole derivatives bearing a nitro substituent on their A-phenol ring were synthesized and their binding affinity towards the estrogen receptor (ER) subtypes ERalpha and ERbeta was determined. Among compounds tested, the 2-nitrophenol derivative 5c was found to bind satisfactorily to both estrogen receptor subtypes (RBAalpha=5.17 and RBAbeta=3.27). In general, the introduction of a nitro group into the A ring of these compounds was found to benefit their ERbeta binding abilities.
摘要
合成了在其A-酚环上带有硝基取代基的新型四取代吡唑衍生物，并测定了它们对雌激素受体（ER）亚型ERα和ERβ的结合亲和力。在所测试的化合物中，发现2-硝基苯酚衍生物5c对两种雌激素受体亚型均具有令人满意的结合能力（RBAα = 5.17，RBAβ = 3.27）。一般而言，发现将硝基引入这些化合物的A环有利于它们与ERβ的结合能力。
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