Formula: C3H8ClNOIn 2012 ,《Discovery of Novel Allosteric Mitogen-Activated Protein Kinase Kinase (MEK) 1,2 Inhibitors Possessing Bidentate Ser212 Interactions》 appeared in Journal of Medicinal Chemistry. The author of the article were Heald, Robert A.; Jackson, Philip; Savy, Pascal; Jones, Mark; Gancia, Emanuela; Burton, Brenda; Newman, Richard; Boggs, Jason; Chan, Emily; Chan, Jocelyn; Choo, Edna; Merchant, Mark; Rudewicz, Patrick; Ultsch, Mark; Wiesmann, Christian; Yue, Qin; Belvin, Marcia; Price, Steve. The article conveys some information:
Using structure-based design, two novel series of highly potent biaryl amine mitogen-activated protein kinase kinase (MEK) inhibitors have been discovered. These series contain an H-bond acceptor, in a shifted position compared with previously disclosed compounds, and an adjacent H-bond donor, resulting in a bidentate interaction with the Ser212 residue of MEK1. The most potent compound identified, 1 (G-894), is orally active in in vivo pharmacodynamic and tumor xenograft models.Azetidin-3-ol hydrochloride(cas: 18621-18-6Formula: C3H8ClNO) was used in this study.
Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Formula: C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.
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