Natural product guided compound library development

被引：62

作者：

Breinbauer, R

Manger, M

Scheck, M

Waldmann, H

机构：

[1] Max Planck Inst Mol Physiol, Dept Chem Biol, D-44227 Dortmund, Germany

[2] Univ Dortmund, Fachbereich 3, D-44221 Dortmund, Germany

来源：

CURRENT MEDICINAL CHEMISTRY | 2002年 / 9卷 / 23期

关键词：

combinatorial chemistry; drug discovery; lead optimisation; natural products; organic synthesis; protein domains; solid phase synthesis;

D O I：

10.2174/0929867023368773

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Natural products are biologically validated starting points for the design of combinatorial libraries, as they have a proven record of biological relevance. This special role of natural products in medicinal chemistry and chemical biology can be interpreted in the light of new insights about the domain architecture of proteins gained by structural biology and bioinformatics. In order to fulfil the specific requirements of the individual binding pocket within a domain family it is necessary to optimise the natural product structure by chemical variation. Solid-phase chemistry is becoming an efficient tool for this optimisation process, and recent advances in this field are highlighted in this review article.

引用

页码：2129 / 2145

页数：17

共 90 条

[31] THE ROLE OF THE CHLORINE SUBSTITUENTS IN THE ANTIBIOTIC VANCOMYCIN - PREPARATION AND CHARACTERIZATION OF MONODECHLOROVANCOMYCIN AND DIDECHLOROVANCOMYCIN [J].