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ID: ALA3124810
Journal: Bioorg Med Chem Lett
Title: Synthesis and biological evaluation of novel benzamide derivatives as potent smoothened antagonists.
Authors: Wu TM, Wang DC, Xiang P, Zhang JN, Sang YX, Lin HJ, Chen J, Xie G, Song H, Zhao YL, Xie YM.
Abstract: A series of novel benzamide derivatives were prepared and evaluated using cell-based measurements. Among these compounds, 10f significantly inhibited Hedgehog signaling and showed equivalent or more potency than GDC-0449 in different tests. Furthermore, compound 10f potently inhibited the proliferation of Daoy, a medulloblastoma cell line that is reported to be resistant to GDC-0449, which indicated a promising prospect in the treatment of Hedgehog signaling pathway related cancer in clinical trial.
CiteXplore: 24491459