Inhibitory kinetics of novel 2,3-dihydro-1 H -inden-1-one chalcone-like derivatives on mushroom tyrosinase
摘要:
In this study, novel 2,3-dihydro-1H-inden-1-one chalcone-like compounds and their hydroxyl derivatives were synthesized, and their inhibitory effects on mushroom tyrosinase activity were evaluated. Two of the compounds synthesized inhibited the diphenolase activity of tyrosinase in a dose dependent manner and exhibited much higher tyrosinase inhibitory activities (IC50 values of 12.3 mu M and 8.2 mu M, respectively) than the positive control, kojic acid (IC50: 27.5 mu M). Kinetic analysis showed that their inhibition was reversible. Both the novel compounds displayed competitive inhibition with their K-i values of 10.3 mu M and 8.7 mu M, respectively. This study suggests hydroxy substituted 2,3-dihydro-1H-inden-1-one chalcone-like compounds to serve as promising candidates for use as depigmentation agents. (C) 2015 Elsevier Ltd. All rights reserved.
This invention relates to certain 3-aryl or 3-heteroaryl pyrazoles with 4,5(3,4)-bicyclic ring fusion which are inhibitors of protein kinase activity, of which some are novel compounds, to pharmaceutical compositions containing these pyrazoles and to processes for preparing these pyrazoles.
This invention realtes to compounds formula I
and pharmaceutically acceptable salts thereof, which are inhibitors of protein kinase activity, pharmaceutical compositions thereof and provesses for their preparation.