SCH 53823 and SCH 53825, novel fungal metabolites with phospholipase D inhibitory activity

被引：27
作者：
Chu, M
Patel, MG
Pai, JK
Das, PR
Puar, MS
机构：
[1] Schering-Plough Research Institute, Kenilworth, NJ 07033
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 05期
关键词：
D O I：
10.1016/0960-894X(96)00074-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Two novel phospholipase D (PLD) inhibitors, Sch 53823 (1) and Sch 53825 (2), were isolated from a fungal culture. The acetylated derivatives, Sch 53827 (3) and Sch 53829 (4), were prepared for the purpose of structure determination. The extensive NMR studies of 3 and 4 including DEFT, COSY, NOESY, HETCOR, and selective INEPT experiments permitted the establishment of their structures, as well as relative stereochemistries. Among these compounds, 3 exhibited the most potent inhibitory activity in the phospholipase D assay with the IC50 = 17 mu M.
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页码：579 / 584
页数：6
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