79950-50-8Relevant academic research and scientific papers
CELL CYCLE PROGRESSION INHIBITOR
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, (2019/09/18)
The present invention provides a cell cycle progression inhibitor, a cytostatic agent, and an anticancer agent. The cell cycle progression inhibitor, the cytostatic agent, and the anticancer agent each contains a Hes1 protein-PHB2 protein binding enhancer.
Facile one-pot transformation of phenols into o-cyanophenols
Nakai, Yuhta,Moriyama, Katsuhiko,Togo, Hideo
, p. 6077 - 6083 (2015/03/30)
The treatment of phenols with paraformaldehyde in the presence of MgCl2 and Et3N in THF at 80 C, followed by reaction with molecular iodine and aq. ammonia at room temperature provided the corresponding o-cyanophenols in moderate to good yields. The present reaction is a one-pot transformation of phenols into o-cyanophenols using much less expensive reagents than are typically used; the reaction is free of both transition-metals and cyanide. The utility of this reaction was highlighted during our preparation of Febuxostat from p-bromophenol.
Synthesis of a 10,000-membered library of molecules resembling carpanone and discovery of vesicular traffic inhibitors
Goess, Brian C.,Hannoush, Rami N.,Chan, Lawrence K.,Kirchhausen, Tomas,Shair, Matthew D.
, p. 5391 - 5403 (2007/10/03)
Split-and-pool synthesis of a 10,000-membered library of molecules resembling the natural product carpanone has been achieved. The synthesis features development of solid-phase multicomponent reactions between nitrogen nucleophiles, enones, and hydroxylamines, and a solid-phase application of the Huisgen cycloaddition affording substituted triazoles. The synthesis was performed in high-capacity (500 μm) polystyrene beads using a one bead-one stock solution strategy that enabled phenotypic screens of the resulting library. Using whole-cell fluorescence imaging, we discovered a series of molecules from the carpanone-based library that inhibit exocytosis from the Golgi apparatus. The most potent member of this series has an IC50 of 14 μM. We also report structure-activity relationships for the molecules exhibiting this interesting phenotype. These inhibitors of exocytosis may be useful reagents for the study of vesicular traffic.
