Target-Directed Enediynes: Designed Estramycins
The Journal of Organic Chemistry2001Vol. 66(11), pp. 3688–3695
Citations Over TimeTop 10% of 2001 papers
Graham B. Jones, George W. Hynd, Justin M. Wright, Ajay Purohit, Gary W. Plourde, Robert S. Huber, Jude E. Mathews, Aiwen Li, Michael W. Kilgore, Glenn J. Bubley, Molly Yancisin, Myles Brown
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 [hERalpha] 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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