HETEROATOM EFFECT IN THE PKC INHIBITORY ACTIVITIES OF PERHYDROAZEPINE ANALOGS OF BALANOL

被引：23

作者：

LAI, YS

STAMPER, M

机构：

[1] 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)00364-Y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Analogs 2-5 of balanol (-)-1, a potent protein kinase C (PKC) inhibitor, were prepared in which the perhydroazepine N atom was replaced with O, S, or C. Compounds 2 and 3 are found to show enhanced isozyme selectivity, despite the general trend of these analogs being less potent PKC inhibitors relative to balanol.

引用

页码：2147 / 2150

页数：4

共 16 条

[1] BASHA A, 1977, TETRAHEDRON LETT, P4171
[2] SEQUENCE AND EXPRESSION OF HUMAN PROTEIN KINASE-C-EPSILON
BASTA, P
STRICKLAND, MB
HOLMES, W
LOOMIS, CR
BALLAS, LM
BURNS, DJ
[J]. BIOCHIMICA ET BIOPHYSICA ACTA, 1992, 1132 (02) : 154 - 160
[3] 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
[4] COREY EJ, 1975, TETRAHEDRON LETT, P3183
[5] A SYNTHESIS OF HOMOALLYLIC ALCOHOLS
CRANDALL, JK
BANKS, DB
COLYER, RA
WATKINS, RJ
ARRINGTO.JP
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1968, 33 (01) : 423 - &
[6] 2 PRACTICAL SYNTHESES OF STERICALLY CONGESTED BENZOPHENONES
HOLLINSHEAD, SP
NICHOLS, JB
WILSON, JW
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1994, 59 (22) : 6703 - 6709
[7] 2 EFFICIENT SYNTHESES OF (+/-)-ANTI-N-BENZYL-3-AMINO-4-HYDROXYHEXAHYDROAZEPINE
HU, H
JAGDMANN, GE
HUGHES, PF
NICHOLS, JB
[J]. TETRAHEDRON LETTERS, 1995, 36 (21) : 3659 - 3662
[8] NEW HEXAHYDROXYBIPHENYL DERIVATIVES AS INHIBITORS OF PROTEIN-KINASE-C
KASHIWADA, Y
HUANG, L
BALLAS, LM
JIANG, JB
JANZEN, WP
LEE, KH
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (01) : 195 - 200
[9] RAPID PURIFICATION OF PROTEIN-KINASE-C BY HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY
KIKKAWA, U
GO, M
KOUMOTO, J
NISHIZUKA, Y
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1986, 135 (02) : 636 - 643
[10] 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

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