Synthesis and biological evaluation of novel benzamide derivatives as potent smoothened antagonists
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.
According to the present invention, a compound represented by formula (I): wherein Q is: A is a hydrogen atom, a halogen atom, -ORa or a C1-4 alkyl group which may be substituted by one or more halogen atoms; E is independently selected from a
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(2010/11/27)
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