Chemistry is an experimental science, Safety of Piperidine-4-carboxamide, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 39546-32-2, Name is Piperidine-4-carboxamide
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 conformation, cognisant of physicochemical properties likely to maintain good cell permeability, led to 74 (CCT251545), a potent small-molecule inhibitor of WNT signaling with good oral pharmacokinetics. We demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing. This work provides a successful example of hypothesis-driven medicinal chemistry optimization from a singleton hit against a cell-based pathway assay without knowledge of the biochemical target.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Safety of Piperidine-4-carboxamide, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 39546-32-2, in my other articles.
Reference：
Piperidine – Wikipedia,
Piperidine | C5H3338N – PubChem