Phosphoinositide-3-kinase inhibitors: Evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511 was written by Lanman, Brian A.;Reed, Anthony B.;Cee, Victor J.;Hong, Fang-Tsao;Pettus, Liping H.;Wurz, Ryan P.;Andrews, Kristin L.;Jiang, Jian;McCarter, John D.;Mullady, Erin L.;San Miguel, Tisha;Subramanian, Raju;Wang, Ling;Whittington, Douglas A.;Wu, Tian;Zalameda, Leeanne;Zhang, Nancy;Tasker, Andrew S.;Hughes, Paul E.;Norman, Mark H.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.COA of Formula: C5H3Br2NO This article mentions the following:
Replacement of the piperazine sulfonamide portion of the PI3Kα inhibitor AMG 511 (1) with a range of aliphatic alcs. led to the identification of a truncated gem-dimethylbenzylic alc. analog, 2-(5-(4-amino-6-methyl-1,3,5-triazin-2-yl)-6-((5-fluoro-6-methoxypyridin-3-yl)amino)pyridin-3-yl)propan-2-ol (7). This compound possessed good in vitro efficacy and pharmacokinetic parameters and demonstrated an EC50 of 239 ng/mL in a mouse liver pharmacodynamic model measuring the inhibition of hepatocyte growth factor (HGF)-induced Akt Ser473 phosphorylation in CD1 nude mice 6 h post-oral dosing. In the experiment, the researchers used many compounds, for example, 2,6-Dibromo-3-hydroxypyridine (cas: 6602-33-1COA of Formula: C5H3Br2NO).
2,6-Dibromo-3-hydroxypyridine (cas: 6602-33-1) belongs to pyridine derivatives. The ring atoms in the pyridine molecule are sp2-hybridized. The nitrogen is involved in the π-bonding aromatic system using its unhybridized p orbital. The lone pair is in an sp2 orbital, projecting outward from the ring in the same plane as the σ bonds. Many analogues of pyridine are known where N is replaced by other heteroatoms . Substitution of one C–H in pyridine with a second N gives rise to the diazine heterocycles (C4H4N2), with the names pyridazine, pyrimidine, and pyrazine.COA of Formula: C5H3Br2NO