THE DESIGN OF INHIBITORS OF PROTEIN-KINASE-C - THE SOLUTION CONFORMATION OF STAUROSPORINE

被引：20

作者：

DAVIS, PD ^{[1
]}

HILL, CH ^{[1
]}

THOMAS, WA ^{[1
]}

WHITCOMBE, IWA ^{[1
]}

机构：

[1] ROCHE PROD LTD,POB 8,WELWYN GARDEN CIT AL7 3AY,HERTS,ENGLAND

来源：

JOURNAL OF THE CHEMICAL SOCIETY-CHEMICAL COMMUNICATIONS | 1991年 / 03期

关键词：

D O I：

10.1039/c39910000182

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

NMR spectra in several solvents show that the conformation of the tetrahydropyran ring in staurosporine changes from a chair form in the free base to a boat conformation on protonation, mainly owing to the increased solvation requirement of -NH2Me+ vs. -NHMe; implications for the bioactive conformation are discussed.

引用

页码：182 / 184

页数：3

共 12 条

[11] UCN-01 AND UCN-02, NEW SELECTIVE INHIBITORS OF PROTEIN KINASE-C .2. PURIFICATION, PHYSICOCHEMICAL PROPERTIES, STRUCTURAL DETERMINATION AND BIOLOGICAL-ACTIVITIES
TAKAHASHI, I
SAITOH, Y
YOSHIDA, M
SANO, H
NAKANO, H
MORIMOTO, M
TAMAOKI, T
[J]. JOURNAL OF ANTIBIOTICS, 1989, 42 (04) : 571 - 576
[12] STAUROSPORINE, A POTENT INHIBITOR OF PHOSPHOLIPID/CA++DEPENDENT PROTEIN-KINASE
TAMAOKI, T
NOMOTO, H
TAKAHASHI, I
KATO, Y
MORIMOTO, M
TOMITA, F
[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1986, 135 (02) : 397 - 402

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