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

J C  BRIGGS; A H  HAINES; R J K  TAYLOR; A P  DAWSON; I  GIBSON; J  HOOK; A  LLOYD; S  MEINERS

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

J C BRIGGS, A H HAINES, R J K TAYLOR, A P DAWSON, I GIBSON, J HOOK, A LLOYD, S MEINERS

Chemistry

Research output: Contribution to journal › Article › peer-review

Abstract

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.

Original language	English
Pages (from-to)	23-35
Number of pages	13
Journal	CARBOHYDRATE RESEARCH
Volume	234
Publication status	Published - 9 Oct 1992

Keywords

ACTIVATION
SN-1,2-DIACYLGLYCEROLS

Cite this

@article{134e0f1ee4464149a26c2e8bea8b6c2f,

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

abstract = "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.",

keywords = "ACTIVATION, SN-1,2-DIACYLGLYCEROLS",

author = "BRIGGS, {J C} and HAINES, {A H} and TAYLOR, {R J K} and DAWSON, {A P} and I GIBSON and J HOOK and A LLOYD and S MEINERS",

year = "1992",

month = oct,

day = "9",

language = "English",

volume = "234",

pages = "23--35",

journal = "CARBOHYDRATE RESEARCH",

issn = "0008-6215",

publisher = "Elsevier",

}

TY - JOUR

T1 - SYNTHESIS OF DIACYLGLYCEROL ANALOGS AS POTENTIAL 2ND-MESSENGER ANTAGONISTS AND INHIBITORS OF PROTEIN-KINASE-C

AU - BRIGGS, J C

AU - HAINES, A H

AU - TAYLOR, R J K

AU - DAWSON, A P

AU - GIBSON, I

AU - HOOK, J

AU - LLOYD, A

AU - MEINERS, S

PY - 1992/10/9

Y1 - 1992/10/9

N2 - 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.

AB - 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.

KW - ACTIVATION

KW - SN-1,2-DIACYLGLYCEROLS

M3 - Article

SN - 0008-6215

VL - 234

SP - 23

EP - 35

JO - CARBOHYDRATE RESEARCH

JF - CARBOHYDRATE RESEARCH

ER -