Synthesis of diacylglycerol analogues as potential second-messenger antagonists and inhibitors of protein kinase C
1992; Elsevier BV; Volume: 234; Linguagem: Inglês
10.1016/0008-6215(92)85036-y
ISSN1873-426X
AutoresJosie C. Briggs, Alan H. Haines, Richard J. K. Taylor, Alan P. Dawson, Ian Gıbson, Jackie Hook, A. C. Lloyd, Silkie Meiners,
Tópico(s)Eicosanoids and Hypertension Pharmacology
ResumoA 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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