Structure-activity relationships of kadsurenone analogues

MM Ponpipom, RL Bugianesi, DR Brooker…

Index: Ponpipom, Mitree M.; Bugianesi, Robert L.; Brooker, David R.; Yue, Bao-Zhen; Hwang, San-Bao; Shen, Tsung-Ying Journal of Medicinal Chemistry, 1987 , vol. 30, # 1 p. 136 - 142

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Citation Number: 41

Abstract

Kadsurenone, a specific receptor antagonist of platelet-activating factor (PAF), and its analogues were prepared from derivatives of cinnamyl alcohol and (ally1oxy) phenol. Racemic kadsurenone, resolvable by a Chiralpak column at low temperatures, has an IC50 value of 2 X lo-'M, which is about 50% of the activity of the natural product (IC50= 1 XM). The structural specificity of kadsurenone was further demonstrated by the low PAF-receptor- ...