期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 1, 期 3, 页码 130-134出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml1000307
关键词
Hedgehog signaling pathway; Smoothened; medulloblastoma
The blockade of aberrant hedgehog (Hh) signaling has shown promise for therapeutic intervention in cancer. A cell-based phenotypic high-throughput screen was performed, and the lead structure (1) was identified as an inhibitor of the Hh pathway via antagonism of the Smoothened receptor (Smo). Structure-activity relationship studies led to the discovery of a potent and specific Smoothened antagonist N-(6-((2S,6R)-2,6-dimethyl morpholino)pyridin-3-yl)-2methy1-4'-(trifluoromethoxy)biphenyl-3-carboxamide (5m, NVP-LDE225), which is currently in clinical development.
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