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

Article abstract of DOI:10.1016/0008-6215(92)85036-Y

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.