Bifunctional scaffolds as templates for synthetic combinatorial libraries

被引：9
作者：
Krchnak, V
Weichsel, AS
Issakova, O
Lam, KS
Lebl, M
机构：
[1] SELECTIDE CORP,TUCSON,AZ 85737
[2] UNIV ARIZONA,COLL MED,ARIZONA CANC CTR,DEPT MED,TUCSON,AZ 85724
[3] UNIV ARIZONA,COLL MED,ARIZONA CANC CTR,DEPT IMMUNOL,TUCSON,AZ 85724
[4] UNIV ARIZONA,COLL MED,ARIZONA CANC CTR,DEPT MICROBIOL,TUCSON,AZ 85724
来源：
MOLECULAR DIVERSITY | 1996年 / 1卷 / 03期
关键词：
combinatorial chemistry; library; scaffold; solid-phase synthesis; streptavidin;
D O I：
10.1007/BF01544955
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：
A small-molecule synthetic combinatorial library was designed and synthesized that features potential pharmacophores attached to a variety of small cyclic scaffolds. The synthesis of the library involved randomization of three types of building blocks: 20 amino acids, 10 aromatic hydroxy acids and 21 alcohols, totaling a library complexity of 4200 compounds. Mitsunobu polymer-supported etherification was used in the last randomization. The library compounds were attached to beads via an ester-bond linkage enabling both on-bead as well as in-solution screening. When the library was tested against a model target, streptavidin, specific binders were found. The structures of the most active compounds were determined from the fragmentation pattern in MS/MS experiments.
引用
收藏
页码：177 / 182
页数：6
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