Protein-degrading enediynes: Library screening of Bergman cycloaromatization products

被引：56

作者：

Jones, GB

Wright, JM

Hynd, G

Wyatt, JK

Yancisin, M

Brown, MA

机构：

[1] Northeastern Univ, Dept Chem, Bioorgan & Med Chem Labs, Boston, MA 02115 USA

[2] Harvard Univ, Sch Med, Dana Farber Canc Inst, Dept Adult Oncol, Boston, MA 02115 USA

来源：

ORGANIC LETTERS | 2000年 / 2卷 / 13期

关键词：

D O I：

10.1021/ol005926q

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A screening method based on Bergman cycloaromatization products was applied to a compact library of estrogenic-enediyne hybrids, An enediyne candidate identified from the screen was subsequently synthesized, and it induced temperature- and concentration-dependent degradation of human estrogen receptor a upon cycloaromatization.

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页码：1863 / 1866

页数：4

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