59425-27-3Relevant academic research and scientific papers
Sc(OTf)3-catalyzed dehydrogenative cyclization for synthesis of N-methylacridones
Li, Xi-An,Wang, Hong-Li,Yang, Shang-Dong
supporting information, p. 1794 - 1797 (2013/05/23)
A novel method has been developed for the synthesis of substituted N-methylacridones from 2-(N-methyl-N-phenylamino)benzaldehydes via dehydrogenative cyclization. This transformation involves two primary processes: the aldehyde first coordinates with Sc(OTf)3 and induces the aromatic electrophilic substitution (SEAr) reaction to form the active intermediate N-methyl-acridin-9-ol, which is then quickly oxidized in situ to afford the acridones. Furthermore, the procedure involved is both environmental friendly and atom efficient; H2O is the only byproduct in this reaction.
Evaluation of synthetic acridones and 4-quinolinones as potent inhibitors of cathepsins L and v
Marques, Emerson F.,Bueno, Mauro A.,Duarte, Patricia D.,Silva, Larissa R.S.P.,Martinelli, Ariani M.,Dos Santos, Caio Y.,Severino, Richele P.,Broemme, Dieter,Vieira, Paulo C.,Correa, Arlene G.
scheme or table, p. 10 - 21 (2012/08/28)
Cathepsins, also known as lysosomal cysteine peptidases, are members of the papain-like peptidase family, involved in different physiological processes. In addition, cathepsins are implicated in many pathological conditions. This report describes the synthesis and evaluation of a series of N-arylanthranilic acids, acridones, and 4-quinolinones as inhibitors of cathepsins V and L. The kinetics revealed that compounds of the classes of acridones are reversible competitive inhibitors of the target enzyme with affinities in the low micromolar range. They represent promising lead candidates for the discovery of novel competitive cathepsin inhibitors with enhanced selectivity and potency. On the other hand, 4-quinolinones were noncompetitive inhibitors and N-arylanthranilic acids were uncompetitive inhibitors.
Structure-activity relationship studies of acridones as potentialantipsoriatic agents.1.Synthesis and antiproliferative activity of simple N-unsubstituted 10H-acridin-9-ones against human keratinocyte growth
Putic, Aleksandar,Stecher, Lambert,Prinz, Helge,Mueller, Klaus
scheme or table, p. 3299 - 3310 (2010/08/19)
A series of N-unsubstituted hydroxy-10H-acridin-9-ones were synthesized and evaluated for inhibitory action against HaCaT keratinocyte growth,in order to explore their potential as antipsoriatic agents. For structureeactivity relationship studies,the numb
