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