Structure-Activity Relationships of Kadsurenone Analogues

Article abstract of DOI:10.1021/jm00384a023

Kadsurenone, a specific receptor antagonist of platelet-activating factor (PAF), and its analogues were prepared from derivatives of cinnamyl alcohol and (allyloxy)phenol.Racemic kadsurenone, resolvable by a Chiralpak column at low temperatures, has an IC50 value of 2 * 10^-7 M, which is about 50percent of the activity of the natural product (IC50 = 1 * 10^-7 M).The structural specificity of kadsurenone was further demonstrated by the low PAF-receptor-blocking activities of denudatin B, mirandin A, desallylkadsurenone, and the 2-epimer of kadsurenone.