[EN] PYRAZOLE DERIVATIVES AS MODULATORS OF THE WNT/B-CATENIN SIGNALING PATHWAY [FR] DÉRIVÉS DE PYRAZOLE UTILISÉS COMME MODULATEURS DE LA VOIE DE SIGNALISATION WNT/β-CATÉNINE
作为VEGFR-2激酶抑制剂的3-(4,5,6,7-四氢-3 H-咪唑并[4,5 - c ]吡啶-2-基)-1 H-喹啉-2-酮的设计与合成
摘要:
一系列3-(4,5,6,7-四氢-3 H-咪唑并[4,5- c ]吡啶-2-基)-1 H-喹啉-2-酮已被确定为一类新的VEGFR-2激酶抑制剂。合成了多种(4,5,6,7-四氢咪唑并[5,4- c ]吡啶-2-基)-乙酸乙酯,并评估了其对VEGFR-2的抑制活性。本文描述了该系列的制备以及化合物对VEGFR-2激酶活性的影响。
A simple method of synthesizing various 2-imidazol-2-ylacetates is described. Condensation of alpha-aminoketals with imidates, followed by cyclization in refluxing 4 M-HCl/Dioxane, yielded 2-imidazol-2-ylacetates under one-pot and mild reaction conditions. (c) 2006 Elsevier Ltd. All rights reserved.