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A novel 3-arylethynyl-substituted pyrido [2, 3,-b] pyrazine derivatives and pharmacophore model as Wnt2/β-catenin pathway inhibitors in non-small-cell lung cancer …

YD Gong, MS Dong, SB Lee, N Kim, MS Bae…

文献索引:Gong, Young-Dae; Dong, Mi-Sook; Lee, Sang-Bum; Kim, Nayeon; Bae, Mi-Seon; Kang, Nam-Sook Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 18 p. 5639 - 5647

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被引用次数: 16

摘要

We developed Wnt/β-catenin inhibitors by identifying 13 number of 3-arylethynyl-substituted pyrido [2, 3,-b] pyrazine derivatives that were able to inhibit the Wnt/β-catenin signal pathway and cancer cell proliferation. In the optimization process, a series of 2, 3, 6- trisubstituted pyrido [2, 3,-b] pyrazine core skeletons showed were shown to higher activity than 2, 3, 6-trisubstituted quinoxaline's and thus hold promise for use as potential small- ...