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

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[12] STAUROSPORINE, A POTENT INHIBITOR OF PHOSPHOLIPID/CA++DEPENDENT PROTEIN-KINASE [J].

TAMAOKI, T ;

NOMOTO, H ;

TAKAHASHI, I ;

KATO, Y ;

MORIMOTO, M ;

TOMITA, F .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1986, 135 (02) :397-402

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