Target-directed enediynes: Designed estramycins

G. B. Jones, G. Hynd, J. M. Wright, A. Purohit, G. W. Plourde, R. S. Huber, J. E. Mathews, A. Li, M. W. Kilgore, G. J. Bubley, M. Yancisin, M. A. Brown

Research output: Contribution to journalArticlepeer-review

59 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)3688-3695
Number of pages8
JournalJournal of Organic Chemistry
Volume66
Issue number11
DOIs
StatePublished - Jun 1 2001

ASJC Scopus subject areas

  • Organic Chemistry

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