Pyridoimidazolones as Novel Potent Inhibitors of v-Raf Murine Sarcoma Viral Oncogene Homologue B1 (BRAF) was written by Niculescu-Duvaz, Dan;Gaulon, Catherine;Dijkstra, Harmen P.;Niculescu-Duvaz, Ion;Zambon, Alfonso;Menard, Delphine;Suijkerbuijk, Bart M. J. M.;Nourry, Arnaud;Davies, Lawrence;Manne, Helen;Friedlos, Frank;Ogilvie, Lesley;Hedley, Douglas;Whittaker, Steven;Kirk, Ruth;Gill, Adrian;Taylor, Richard D.;Raynaud, Florence I.;Moreno-Farre, Javier;Marais, Richard;Springer, Caroline J.. And the article was included in Journal of Medicinal Chemistry in 2009.SDS of cas: 6834-42-0 This article mentions the following:
BRAF is a serine/threonine kinase that is mutated in a range of cancers, including 50-70% of melanomas, and has been validated as a therapeutic target. The authors have designed and synthesized mutant BRAF inhibitors containing pyridoimidazolone as a new hinge-binding scaffold. Compounds have been obtained which have low nanomolar potency for mutant BRAF (12 nM for compound I) and low micromolar cellular potency against a mutant BRAF melanoma cell line, WM266.4. The series benefits from very low metabolism, and pharmacokinetics (PK) that can be modulated by methylation of the NH groups of the imidazolone, resulting in compounds with fewer H-donors and a better PK profile. These compounds have great potential in the treatment of mutant BRAF melanomas. In the experiment, the researchers used many compounds, for example, 2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0SDS of cas: 6834-42-0).
2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).SDS of cas: 6834-42-0
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics