Ontology highlight
ABSTRACT:
SUBMITTER: Mallinger A
PROVIDER: S-EPMC4767141 | biostudies-literature | 2015 Feb
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20150213 4
WNT signaling is frequently deregulated in malignancy, particularly in colon cancer, and plays a key role in the generation and maintenance of cancer stem cells. We report the discovery and optimization of a 3,4,5-trisubstituted pyridine 9 using a high-throughput cell-based reporter assay of WNT pathway activity. We demonstrate a twisted conformation about the pyridine-piperidine bond of 9 by small-molecule X-ray crystallography. Medicinal chemistry optimization to maintain this twisted conforma ...[more]