The goal of selective targeting of enediyne cytotoxins has been investigated using estrogenic deliveryvehicles. A series of estrogen−enediyne conjugates were assembled, and affinity for human estrogenreceptor [hERα] was determined. The most promising candidate induced receptor degradationfollowing Bergman cycloaromatization and caused inhibition of estrogen-induced transcription inT47-D human breast cancer cells.
