The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 3,4,5-Trichloropyridine, is researched, Molecular C5H2Cl3N, CAS is 33216-52-3, about Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen, the main research direction is trisubstituted pyridine preparation bioavailability WNT signaling inhibitor antitumor.Application In Synthesis of 3,4,5-Trichloropyridine.
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. The authors report the discovery and optimization of a 3,4,5-trisubstituted pyridine, 1-(3,5-Dichloropyridin-4-yl)piperidine-4-carboxamide (9), using a high-throughput cell-based reporter assay of WNT pathway activity. The authors demonstrate a twisted conformation about the pyridine-piperidine bond of (9) by small-mol. x-ray crystallog. Medicinal chem. optimization to maintain this twisted conformation, cognisant of physicochem. properties likely to maintain good cell permeability, led to 8-[3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]pyridin-4-yl]-2,8-diazaspiro[4,5]decan-1-one (74) (CCT251545), a potent small-mol. inhibitor of WNT signaling with good oral pharmacokinetics. The authors 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 chem. optimization from a singleton hit against a cell-based pathway assay without knowledge of the biochem. target.
In addition to the literature in the link below, there is a lot of literature about this compound(3,4,5-Trichloropyridine)Application In Synthesis of 3,4,5-Trichloropyridine, illustrating the importance and wide applicability of this compound(33216-52-3).
Reference:
Bromide – Wikipedia,
bromide – Wiktionary