INCREASING THE CELLULAR PKC INHIBITORY ACTIVITY OF BALANOL - A STUDY OF ESTER ANALOGS

被引：21

作者：

CRANE, HM

MENALDINO, DS

JAGDMANN, GE

DARGES, JW

BUBEN, JA

机构：

[1] Departments of Chemical and Biomolecular Research, Sphinx Pharmaceuticals, A Division of Eli Lilly and Company, Durham, NC 27707

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 18期

关键词：

D O I：

10.1016/0960-894X(95)00361-V

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

As part of an effort to enhance the cellular activity of balanol analogs 2 and 3, we prepared a series of benzophenone ester analogs of varying steric size and hydrolytic stability. These were evaluated for protein kinase C inhibitory activity, with the results showing that both small alkyl esters and the pivaloyloxymethyl ester analogs displayed large increases in cellular PKC inhibition.

引用

页码：2133 / 2138

页数：6

共 15 条

[1] THERAPEUTIC POTENTIAL OF PROTEIN-KINASE-C INHIBITORS
BRADSHAW, D
HILL, CH
NIXON, JS
WILKINSON, SE
[J]. AGENTS AND ACTIONS, 1993, 38 (1-2): : 135 - 147
[2] NEW METHODS FOR OXIDATION OF ALDEHYDES TO CARBOXYLIC ACIDS AND ESTERS
COREY, EJ
GILMAN, NW
GANEM, BE
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1968, 90 (20) : 5616 - &
[3] DAEHNE WV, 1970, J MED CHEM, V13, P607
[4] DEFAUW JM, 1994, 24TH MED CHEM S SALT
[5] 2 PRACTICAL SYNTHESES OF STERICALLY CONGESTED BENZOPHENONES
HOLLINSHEAD, SP
NICHOLS, JB
WILSON, JW
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1994, 59 (22) : 6703 - 6709
[6] JAGDMANN GE, UNPUB
[7] BALANOL - A NOVEL AND POTENT INHIBITOR OF PROTEIN-KINASE-C FROM THE FUNGUS VERTICILLIUM-BALANOIDES
KULANTHAIVEL, P
HALLOCK, YF
BOROS, C
HAMILTON, SM
JANZEN, WP
BALLAS, LM
LOOMIS, CR
JIANG, JB
KATZ, B
STEINER, JR
CLARDY, J
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1993, 115 (14) : 6452 - 6453
[8] RECEPTOR-MEDIATED REGULATION OF SUPEROXIDE PRODUCTION IN HUMAN-NEUTROPHILS STIMULATED BY PHORBOL-MYRISTATE ACETATE
LEHRER, RI
COHEN, L
[J]. JOURNAL OF CLINICAL INVESTIGATION, 1981, 68 (05) : 1314 - 1320
[9] PREPARATION OF CARBOXYLIC-ACIDS FROM ALDEHYDES (INCLUDING HYDROXYLATED BENZALDEHYDES) BY OXIDATION WITH CHLORITE
LINDGREN, BO
NILSSON, T
[J]. ACTA CHEMICA SCANDINAVICA, 1973, 27 (03): : 888 - 890
[10] MENALDINO DS, 1994, 208TH NAT M AM CHEM

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