Document Report Card

Basic Information

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

DOI: 10.1016/j.bmcl.2014.01.006