BISINDOLYLMALEIMIDE INHIBITORS OF PROTEIN-KINASE-C - FURTHER CONFORMATIONAL RESTRICTION OF A TERTIARY AMINE SIDE-CHAIN

被引：12

作者：

DAVIS, PD ^{[1
]}

HALLAM, TJ ^{[1
]}

HARRIS, W ^{[1
]}

HILL, CH ^{[1
]}

LAWTON, G ^{[1
]}

NIXON, JS ^{[1
]}

SMITH, JL ^{[1
]}

VESEY, DR ^{[1
]}

WILKINSON, SE ^{[1
]}

机构：

[1] ROCHE RES CTR,BROADWATER RD,WELWYN GARDEN CIT AL7 3AY,HERTS,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(01)80349-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A pharmacophore model for the localisation of the cationic binding site of bisindolylmaleimide PKC inhibitors is described. This model has been used to guide selection of further conformationally restricted tertiary amine analogues, culminating in the identification and synthesis of the potent and highly selective PKC inhibitor, Ro 32-0557.

引用

页码：1303 / 1308

页数：6

共 10 条

[1] BIRCHALL AM, IN PRESS J PHARM EXP
[2] INHIBITORS OF PROTEIN-KINASE-C .3. POTENT AND HIGHLY SELECTIVE BISINDOLYLMALEIMIDES BY CONFORMATIONAL RESTRICTION
BIT, RA
DAVIS, PD
ELLIOTT, LH
HARRIS, W
HILL, CH
KEECH, E
KUMAR, H
LAWTON, G
MAW, A
NIXON, JS
VESEY, DR
WADSWORTH, J
WILKINSON, SE
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (01) : 21 - 29
[3] A DIECKMANN/RING EXPANSION APPROACH TO TETRAHYDROPYRIDO[1,2-A]INDOLES AND TETRAHYDROAZEPINO[1,2-A]INDOLES
BIT, RA
DAVIS, PD
HILL, CH
KEECH, E
VESEY, DR
[J]. TETRAHEDRON, 1991, 47 (26) : 4645 - 4664
[4] 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
[5] INHIBITORS OF PROTEIN-KINASE-C .2. SUBSTITUTED BISINDOLYMALEIMIDES WITH IMPROVED POTENCY AND SELECTIVITY
DAVIS, PD
ELLIOTT, LH
HARRIS, W
HILL, CH
HURST, SA
KEECH, E
KUMAR, MKH
LAWTON, G
NIXON, JS
WILKINSON, SE
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (06) : 994 - 1001
[6] DAVIS PD, 1990, TETRAHEDRON LETT, V31, P2353
[7] A MILD CONVERSION OF MALEIC ANHYDRIDES INTO MALEIMIDES
DAVIS, PD
BIT, RA
[J]. TETRAHEDRON LETTERS, 1990, 31 (36) : 5201 - 5204
[8] ON TARGET WITH A NEW MECHANISM FOR THE REGULATION OF PROTEIN-PHOSPHORYLATION
HUBBARD, MJ
COHEN, P
[J]. TRENDS IN BIOCHEMICAL SCIENCES, 1993, 18 (05) : 172 - 177
[9] THE ROLE OF PROTEIN KINASE-C IN CELL-SURFACE SIGNAL TRANSDUCTION AND TUMOR PROMOTION
NISHIZUKA, Y
[J]. NATURE, 1984, 308 (5961) : 693 - 698
[10] ISOENZYME SPECIFICITY OF BISINDOLYLMALEIMIDES, SELECTIVE INHIBITORS OF PROTEIN-KINASE-C
WILKINSON, SE
PARKER, PJ
NIXON, JS
[J]. BIOCHEMICAL JOURNAL, 1993, 294 : 335 - 337

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