Design and Synthesis of 1-Indol-1-yl-propan-2-ones as Inhibitors of Human Cytosolic
Phospholipase A<sub>2</sub>α
Joachim Ludwig
Stefanie Bovens
Carsten Brauch
Alwine Schulze Elfringhoff
Matthias Lehr
10.1021/jm051243a.s001
https://acs.figshare.com/articles/journal_contribution/Design_and_Synthesis_of_1_Indol_1_yl_propan_2_ones_as_Inhibitors_of_Human_Cytosolic_Phospholipase_A_sub_2_sub_/3226246
The synthesis and structure−activity relationship study of a series of 1-indol-1-yl-3-phenoxypropan-2-one
inhibitors of cytosolic phospholipase A<sub>2</sub>α (cPLA<sub>2</sub>α) are described. The compounds were evaluated in a
vesicle assay with isolated cPLA<sub>2</sub>α and in cellular assays with intact human platelets. Systematic variation
led to 3-methylhydrogen 1-[3-(4-decyloxyphenoxy)-2-oxopropyl]indole-3,5-dicarboxylate (<b>57</b>), which revealed
the highest activity against the isolated enzyme. With an IC<sub>50</sub> value of 4.3 nM in this assay, it is one of the
most potent in vitro cPLA<sub>2</sub>α inhibitors known today.
2006-04-20 00:00:00
2 α
cPLA 2 α
Human Cytosolic Phospholipase
assay
cPLA 2 α inhibitors
IC 50 value