Target-directed enediynes: Designed estramycins

被引：60

作者：

Jones, GB ^{[1
]}

Hynd, G

Wright, JM

Purohit, A

Plourde, GW

Huber, RS

Mathews, JE

Li, AW

Kilgore, MW

Bubley, GJ

Yancisin, M

Brown, MA

机构：

[1] Northeastern Univ, Dept Chem, Boston, MA 02115 USA

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

[3] Harvard Univ, Sch Med, Beth Israel Deaconess Med Ctr, Boston, MA 02215 USA

[4] Clemson Univ, GHS CU Biomed Cooperat, Clemson, SC 29634 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2001年 / 66卷 / 11期

关键词：

D O I：

10.1021/jo0055842

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The goal of selective targeting of enediyne cytotoxins has been investigated using estrogenic delivery vehicles. A series of estrogen-enediyne conjugates were assembled, and affinity for human estrogen receptor [hERα] was determined. The most promising candidate induced receptor degradation following Bergman cycloaromatization and caused inhibition of estrogen-induced transcription in T47-D human breast cancer cells.

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收藏

页码：3688 / 3695

页数：8

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