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Synthesis of diacylglycerol analogues as potential second-messenger antagonists and inhibitors of protein kinase C

✍ Scribed by Josie C. Briggs; Alan H. Haines; Richard J.K. Taylor; Alan P. Dawson; I. Gibson; Jackie Hook; Alan Lloyd; Silkie Meiners

Book ID: 102990278
Publisher: Elsevier Science
Year: 1992
Tongue: English
Weight: 973 KB
Volume: 234
Category: Article
ISSN: 0008-6215
DOI: 10.1016/0008-6215(92)85036-y

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✦ Synopsis

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-O-acetyl-1-O-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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