SYNTHESIS OF DIACYLGLYCEROL ANALOGS AS POTENTIAL 2ND-MESSENGER ANTAGONISTS AND INHIBITORS OF PROTEIN-KINASE-C

被引:9
|
作者
BRIGGS, JC
HAINES, AH
TAYLOR, RJK
DAWSON, AP
GIBSON, I
HOOK, J
LLOYD, A
MEINERS, S
机构
[1] UNIV E ANGLIA,SCH CHEM SCI,NORWICH NR4 7TJ,NORFOLK,ENGLAND
[2] UNIV E ANGLIA,SCH BIOL SCI,NORWICH NR4 7TJ,NORFOLK,ENGLAND
关键词
D O I
10.1016/0008-6215(92)85036-Y
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of analogues of diacylglycerol has been prepared and tested as inhibitors of protein kinase C (PKC). The diketone analogues, 10-hydroxymethyl-8,13-eicosanedione (24), 10-acetoxymethyl-8,13-eicosanedione (25), and 10-methoxymethyl-8,13-eicosanedione (26) each inhibited PKC activated by 2-0-acetyl-1-0-oleoylglycerol. Compound 24 was the most effective inhibitor of the growth of MR4 and HT29 cells in culture, and 26 was more effective than 24 against HL60 cells.
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页码:23 / 35
页数:13
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