Lim, Jongwon published the artcileDiscovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers, COA of Formula: C6H3ClIN3, the publication is Journal of Medicinal Chemistry (2016), 59(13), 6501-6511, database is CAplus and MEDLINE.
The ERK/MAPK pathway plays a central role in the regulation of critical cellular processes and is activated in more than 30% of human cancers. Specific BRAF and MEK inhibitors have shown clin. efficacy in patients for the treatment of BRAF-mutant melanoma. However, the majority of responses are transient, and resistance is often associated with pathway reactivation of the ERK signal pathway. Acquired resistance to these agents has led to greater interest in ERK, a downstream target of the MAPK pathway. De novo design efforts of a novel scaffold derived from SCH772984 by employing hydrogen bond interactions specific for ERK in the binding pocket identified 1-(1H-pyrazolo[4,3-c]pyridin-6-yl)ureas as a viable lead series. Sequential SAR studies led to the identification of highly potent and selective ERK inhibitors with low mol. weight and high LE. Compound 21 exhibited potent target engagement and strong tumor regression in the BRAFV600E xenograft model.
Journal of Medicinal Chemistry published new progress about 1260672-72-7. 1260672-72-7 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Iodide, name is 6-Chloro-3-iodo-1H-pyrazolo[4,3-c]pyridine, and the molecular formula is C6H3ClIN3, COA of Formula: C6H3ClIN3.
Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com